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Profile Name | FLT3 L610_E611insCSSDNEYFYVDFREYEYDLKWEFPRENL |
Gene Variant Detail |
FLT3 L610_E611insCSSDNEYFYVDFREYEYDLKWEFPRENL (gain of function) |
Relevant Treatment Approaches | FLT3 Inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Relevant Treatment Approaches | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|---|
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Navitoclax + TAK-901 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of TAK-901 and ABT-263 demonstrated synergy in inhibiting proliferation of colorectal cancer cell lines in culture (PMID: 25667100). | 25667100 |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Navitoclax + TAK-901 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of TAK-901 and Navitoclax (ABT-263) resulted in a synergistic effect, demonstrating reduced cell viability of non-small cell lung cancer cells in culture (PMID: 28179288). | 28179288 |
Unknown unknown | prostate cancer | not applicable | FLT3 Inhibitor | Navitoclax + TAK-901 | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of TAK-901 and Navitoclax (ABT-263) resulted in a synergistic effect, demonstrating reduced cell viability of prostate cancer cells in culture (PMID: 28179288). | 28179288 |
Unknown unknown | lung non-squamous non-small cell carcinoma | not applicable | FLT3 Inhibitor | Carboplatin + Linifanib + Paclitaxel | Phase II | Actionable | In a Phase II clinical, Linifanib (ABT-869), in combination with Taxol (paclitaxel) and Paraplatin (carboplatin), increased progression free survival in patients with nonsquamous non-small cell lung cancer (PMID: 25559798). | 25559798 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Linifanib | Phase II | Actionable | In a Phase II clinical trial, single-agent linifanib was found safe and efficacious in patients with advanced hepatocellular carcinoma (PMID: 22833179). | 22833179 |
Unknown unknown | glioblastoma | not applicable | FLT3 Inhibitor | Pexidartinib | Phase II | Actionable | In a Phase II trial, Pexidartinib (PLX3397) in combination with radiation therapy and Temodar (temozolomide) demonstrated safety and improved efficacy over standard therapy, resulting in a median progression-free survival of 9.7 months and an estimated overall survival of 25.1 months in newly diagnosed glioblastoma multiforme patients (Neuro Oncol (2016) 18 (suppl 6): vi6). | detail... |
Unknown unknown | tenosynovial giant cell tumor | not applicable | FLT3 Inhibitor | Pexidartinib | FDA approved | Actionable | In a Phase III trial (ENLIVEN) that supported FDA approval, Turalio (pexidartinib) treatment resulted in improved overall response rate at week 25 (24/61, 39% vs 0/59, 0%, p<0.0001) compared to placebo in patients with advanced tenosynovial giant cell tumour (PMID: 31229240; NCT02371369). | detail... 31229240 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Pexidartinib + PLX9486 | Phase I | Actionable | In a Phase I trial, PLX9486 and Pexidartinib (PLX3397) combination therapy demonstrated safety and preliminary efficacy, resulted in a partial response rate of 8.3% (1/12) and progression-free survival not yet reached in patients with advanced solid tumors, 11 of these patients had gastrointestinal stromal tumor that progressed on Gleevec (imatinib mesylate), and most harbored KIT exon 11 and exon 17 mutations (Journal of Clinical Oncology 36, no. 15_suppl (May 20 2018) 11509-11509; NCT02401815). | detail... |
Unknown unknown | diffuse large B-cell lymphoma | not applicable | FLT3 Inhibitor | Ibrutinib + SEL24-B489 | Preclinical | Actionable | In a preclinical study, SEL24-B489 demonstrated a synergistic effect when combined with Ibruvica (ibrutinib) in diffuse large B-cell lymphoma cells in culture, resulting in cell growth inhibition ((Blood 126 (23):706.December 2015). | detail... |
Unknown unknown | diffuse large B-cell lymphoma | not applicable | FLT3 Inhibitor | SEL24-B489 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, SEL24-B489 treatment induced apoptosis in diffuse large B-cell lymphoma cells in both culture and xenograft models (Blood 126 (23):706.December 2015). | detail... |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Debio 0617B | Preclinical - Patient cell culture | Actionable | In a preclinical study, Debio 0617B inhibited survival of a variety of patient-derived tumor cells in culture (PMID: 27439479). | 27439479 |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Merestinib | Phase I | Actionable | In a Phase I trial, LY2801653 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including patients with colorectal cancer (Cancer Res October 1, 2014 74:CT237). | detail... |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Merestinib | Preclinical | Actionable | In a preclinical study, LY2801653 inhibited tumor growth in mouse xenograft models of non-small cell lung cancer (PMID: 24305878). | 24305878 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Merestinib | Phase I | Actionable | In a Phase I trial, LY2801653 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (Cancer Res October 1, 2014 74:CT237). | detail... |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Merestinib + Ramucirumab | Phase I | Actionable | In a Phase I trial, the combination of Merestinib (LY2801653) and Cyramza (ramucirumab) demonstrated tolerability and resulted in a median overall survival of 8.9 months, median progression-free survival of 3.3 months, and stable disease in 52% (12/23) of patients with previously treated metastatic colorectal cancer (PMID: 32537847; NCT02745769). | 32537847 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Amuvatinib + Carboplatin + Paclitaxel | Phase I | Actionable | In a Phase I clinical trial, Amuvatinib (MP470) in combination with chemotherapeutic agents, demonstrated safety and some efficacy in patients with advanced solid tumors (PMID: 24849582). | 24849582 |
Unknown unknown | multiple myeloma | not applicable | FLT3 Inhibitor | Carfilzomib + Zotiraciclib | Phase I | Actionable | In a Phase I trial, Zotiraciclib (TG02) in combination with Kyprolis (carfilzomib) resulted in an overall response rate of 27% (3/11) and durable stable disease in 27% (3/11) of multiple myeloma patients (Blood 2015 126:3052). | detail... |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | Zotiraciclib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Zotiraciclib (TG02) inhibited growth of acute myeloid leukemia cell lines and patient-derived acute myeloid leukemia cells in culture (PMID: 21860433). | 21860433 |
Unknown unknown | acute lymphoblastic leukemia | not applicable | FLT3 Inhibitor | Zotiraciclib | Preclinical - Cell culture | Actionable | In a preclinical study, TG02 inhibited growth of acute lymphocytic leukemia cells in culture (PMID: 21860433). | 21860433 |
Unknown unknown | lymphoid leukemia | not applicable | FLT3 Inhibitor | Ponatinib | FDA approved | Actionable | In a Phase II clinical trial which supported FDA approval, Iclusig (ponatinib) was effective in promoting disease regression in 52% of patients with accelerated phase chronic myeloid leukemia, 31% of patients with blast phase chronic myeloid leukemia, and 41% of patients with Philadelphia chromosome positive acute lymphoblastic leukemia (PMID: 23935038). | 23935038 detail... |
Unknown unknown | gastrointestinal stromal tumor | not applicable | FLT3 Inhibitor | Ponatinib | Phase II | Actionable | In a Phase II trial, Iclusig (ponatinib) demonstrated preliminary activity in patients with advanced gastrointestinal stromal tumor (J Clin Oncol (Meeting Abstracts) 2014 32: 10506). | detail... |
Unknown unknown | glioblastoma | not applicable | FLT3 Inhibitor | Ponatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Iclusig (ponatinib) induced apoptosis and inhibited growth in glioblastoma cells in culture and in cell line xenograft models (PMID: 25378936). | 25378936 |
Unknown unknown | chronic myeloid leukemia | not applicable | FLT3 Inhibitor | Ponatinib | Clinical Study | Actionable | In a meta-analysis, Iclusig (ponatinib) treatment was associated with increased rate of major molecular response compared with Gleevec (imatinib) (Odds Ratio (OR): 4.95 [0.97-25.19]), but not improved overall survival (OR: 2.00 [0.21-19.33]), and was associated with increased risk of vascular occlusive events (OR: 3.47 [1.23-9.78]) in patients with chronic myeloid leukemia (PMID: 26847662). | 26847662 |
Unknown unknown | chronic myeloid leukemia | not applicable | FLT3 Inhibitor | Ponatinib | FDA approved | Actionable | In a Phase II clinical trial which supported FDA approval, Iclusig (ponatinib) was effective in promoting disease regression in 52% of patients with accelerated phase chronic myeloid leukemia, 31% of patients with blast phase chronic myeloid leukemia, and 41% of patients with Philadelphia chromosome positive acute lymphoblastic leukemia (PMID: 23935038). | 23935038 detail... |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | AKN-028 | Preclinical - Cell culture | Actionable | In a preclinical study, AKN-028 treatment induced apoptosis in acute myeloid leukemia cells in culture and inhibited growth and resulted in decreased tumor mass in acute myeloid leukemia cell line xenograft models (PMID: 22864397). | 22864397 |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | AKN-028 + Cytarabine | Preclinical - Cell culture | Actionable | In a preclinical study, the sequential treatment of Cytosar-U (cytarabine) and AKN-028 resulted in a syntergistic effect in acute myeloid leukemia cells in culture, demonstrating antileukemic activity (PMID: 22864397). | 22864397 |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | AKN-028 + Daunorubicin | Preclinical - Cell culture | Actionable | In a preclinical study, the sequential treatment of Cerubidine (daunorubicin) and AKN-028 resulted in a syntergistic effect in acute myeloid leukemia cells in culture, demonstrating antileukemic activity (PMID: 22864397). | 22864397 |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | Cytarabine + Daunorubicin + Quizartinib | Phase I | Actionable | In a Phase I trial (QuANTUM-First), the combination therapy, Quizartinib (AC220) with Cytosar-U (cytarabine) and Cerubidine (daunorubicin), resulted in a response in 84% (16/19) of patients with acute myeloid leukemia, including fourteen patients with a composite complete response and two patients achieving morphologic leukemia-free state (PMID: 29139135; NCT01390337). | 29139135 |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | Quizartinib | Phase II | Actionable | In a Phase II trial, Quizartinib (AC220) treatment resulted in a composite complete remission (CCR) in 36% (16/44; 1 complete remission (CR)) of FLT3-ITD-negative patients vs. 56% (63/112; 3 CR) of FLT3-ITD-positive patients with relapsed/refractory acute myeloid leukemia (AML) after first-line therapy, and CCR in 30% (12/40; 1 CR) of FLT3-ITD-negative vs. 46% (62/136; 5 CR) in FLT3-ITD-positive patients with relapsed/refractory AML after salvage chemotherapy or transplant (PMID: 29859851; NCT00989261). | 29859851 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | SU14813 | Phase I | Actionable | In a Phase I trial, SU14813 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, with an objective response rate of 20% (13/65), including 1 complete response and 12 partial responses (PMID: 20605934). | 20605934 |
Unknown unknown | prostate cancer | not applicable | FLT3 Inhibitor | Atezolizumab + Cabozantinib | Phase I | Actionable | In a Phase I trial (COSMIC-021), Tecentriq (atezolizumab) and Cometriq (Cabometyx, cabozantinib) combination therapy was tolerated, resulted in an objective response rate of 32% (14/44, 2 complete responses, 12 partial responses) and stable disease in 48% (21/44) of patients with metastatic castration-resistant prostate cancer whose disease progressed after Xtandi (enzalutamide) or Zytiga (abiraterone) treatment (J Clin Oncol 38, no. 15_suppl (May 20, 2020) 5564-5564; NCT03170960). | detail... |
Unknown unknown | thyroid gland medullary carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | FDA approved | Actionable | In a Phase III trial that supported FDA approval, treatment with Cometriq (cabozantinib) significantly improved median progression free survival (11.2 vs 4.0, HR 0.28, p<0.001) compared to placebo in patients with metastatic medullary thyroid cancer (PMID: 24002501; NCT00704730). | detail... 24002501 |
Unknown unknown | uveal melanoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, Cometriq (cabozantinib) treatment resulted in stable disease in 61% (14/23) of patients with metastatic uveal melanoma, with a median progression free survival of 4.8 months and an overall survival of 12.6 months (PMID: 28103611; NCT00940225). | 28103611 |
Unknown unknown | uveal melanoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, treatment with Cometriq (Cabometyx, cabozantinib) did not result in an improved progression-free survival at 4 months (32.3% vs 26.7%, P=0.35) and median overall survival (6.4 mo vs 7.3 mo, P=0.58) when compared to treatment with Temodar (temozolomide) or Deticene (dacarbazine) in patients with uveal melanoma (PMID: 31558480; NCT01835145). | 31558480 |
Unknown unknown | breast cancer | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical | Actionable | In a preclinical study, Cometriq (cabozantinib) suppressed metastasis, angiogenesis, and tumor growth in mouse models of breast cancer (PMID: 21926191). | 21926191 |
Unknown unknown | gastrointestinal system cancer | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical - Pdx | Actionable | In a preclinical study, Cometriq (cabozantinib) demonstrated efficacy in colorectal cancer patient-derived tumor explant models (Cancer Research: April 15, 2013; Volume 73, Issue 8, Supplement 1). | detail... |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical | Actionable | In a preclinical study, Cometriq (cabozantinib) showed anti-tumor activity in human colorectal cancer explants (PMID: 25242168). | 25242168 |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical - Pdx | Actionable | In a preclinical study, Cometriq (Cabometyx, cabozantinib) treatment inhibited activation of PI3K/AKT/MTOR signaling pathway, reduced phosphorylation of Met, Ret, and Axl, and induced autophagy in colorectal cancer cells in culture, and decreased tumor vascularity, reduced tumor growth, and induced regression in patient-derived xenograft (PDX) models (PMID: 30026382). | 30026382 |
Unknown unknown | multiple myeloma | no benefit | FLT3 Inhibitor | Cabozantinib | Phase I | Actionable | In a Phase Ib trial, Cometriq (Cabometyx, cabozantinib) treatment did not demonstrate significant efficacy, resulting in a minimal response in 9% (1/11), stable disease in 73% (8/11), and progression in 18% (2/11) of patients with relapsed and/or refractory multiple myeloma (PMID: 27020089; NCT01866293). | 27020089 |
Unknown unknown | renal carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, renal cancer patients treated with Cabozantinib demonstrated a 28 % objective response rate, a 62 % stable disease rate, and a median progression free survival of 14.7 months (PMID: 23292795). | 23292795 |
Unknown unknown | ovarian cancer | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II clinical trial, Cometriq (cabozantinib ) demonstrated safety and efficacy in patients with ovarian cancers (J Clin Oncol 29: 2011 (suppl; abstr 5008)). | detail... |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | FDA approved | Actionable | In a Phase III trial (CELESTIAL) that supported FDA approval, Cabometyx (cabozantinib) significantly improved overall survival (10.2 vs 8.0 months, HR=0.76, p=0.005) and progression-free survival (5.2 vs 1.9 months, HR=0.44, p<0.001) compared to placebo in patients with previously treated advanced hepatocellular carcinoma (PMID: 29972759; NCT01908426). | 29972759 detail... |
Unknown unknown | uterine carcinosarcoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II (NCI9322/PHL86) trial, Cometriq (Cabometyx, cabozantinib) treatment resulted in a partial response in 5% (1/19) and progression-free survival (PFS) at 12 weeks in 42% (8/19) of patients with endometrial carcinosarcoma, with a median PFS of 3.0 months (PMID: 31992589; NCT01935934). | 31992589 |
Unknown unknown | brain glioma | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical | Actionable | In a preclinical study, Cometriq (cabozantinib) decreased cell proliferation and induced apoptosis in mouse models of glioma (PMID: 21926191). | 21926191 |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase Ib/II | Actionable | In a Phase Ib/II trial, Cometriq (cabozantinib) treatment resulted in partial response in 6.7% (1/15) of patients with non-small cell lung carcinoma that had progressed during treatment with Tarceva (erlotinib), with a median progression free survival of 1.9 months (PMID: 28352985). | 28352985 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II clinical trial, Cometriq (cabozantinib) showed safety and anti-tumor activity in several advanced solid tumor types (J Clin Oncol 29: 2011 (suppl; abstr 3010)). | detail... |
Unknown unknown | transitional cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, Cometriq (cabozantinib) treatment resulted in complete response in 2% (1/41), partial response in 17% (7/41), stable disease in 44% (18/41) of urothelial carcinoma patients, with a median progression-free survival of 3.7 months and median overall survival of 8.2 months (J Clin Oncol 34, 2016 (suppl; abstr 4534)). | detail... |
Unknown unknown | endometrial cancer | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II (NCI9322/PHL86) trial, Cometriq (Cabometyx, cabozantinib) treatment resulted in a response rate (RR) of 14% (5/36), a 12-week progression-free survival (PFS) rate of 67%, and a mPFS of 4.8 mo in patients with recurrent/metastatic endometrial cancer of endometrioid histology, and a RR of 12% (4/34), a 12-week PFS of 56%, and a mPFS of 4.0 mo in patients of serous histology, and a RR of 6% (2/32) and a 12-week PFS of 47% in patients of uncommon histology (PMID: 31992589; NCT01935934). | 31992589 |
Unknown unknown | cholangiocarcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, Cometriq (cabozantinib) treatment resulted in a median progression free survival of 1.8 months, and a median overall survival of 5.2 months in patients with advanced cholangiocarcinoma, but also induced grade 3/4 adverse events in 89% (17/19) of the patients (PMID: 28192597). | 28192597 |
Unknown unknown | pancreatic adenocarcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical | Actionable | In a preclinical trial, Cometriq (cabozantinib) promoted apoptosis of pancreactic ductal adenocarcinoma cells (PMID: 23661005). | 23661005 |
Unknown unknown | melanoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, Cometriq (cabozantinib) treatment resulted in partial response in 5% (4/77) and sttable disease in 39% (30/77) of patients with metastatic melanoma, with a median overall progression free survival of 3.8 months (PMID: 28103611). | 28103611 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | FDA approved | Actionable | In a Phase II trial (CABOSUN) that supported FDA approval, Cabometyx (cabozantinib) treatment resulted in improved progression free survival (8.2 v 5.6 months) and objective response rate (46% vs 18%) compared to Sutent (sunitinib) in patients with untreated metastatic renal cell carcinoma, with a 34% reduction in rate of progression or death (HR=0.66, p=0.012) (PMID: 28199818; NCT01835158). | 28199818 detail... |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | FDA approved | Actionable | In a Phase III clinical trial (METEOR) that supported FDA approval, treatment with Cabometyx (cabozantinib) resulted in a median progression-free survival of 7.4 months in patients with renal cell carcinoma, compared to 3.8 months with Afinitor (everolimus), and an objective response rate of 22% (17/76) versus 3% (2/77) with Afinitor (everolimus) (PMID: 26406150; NCT01865747). | detail... 26406150 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | FDA approved | Actionable | In a Phase III trial, final results extending those that supported FDA approval demonstrated Cabometyx (cabozantinib) improved median overall survival compared to Afinitor (everolimus) (21.4 m vs. 16.5 m) and progression-free survival (7.4 m vs. 3.9 m), and led to a 17% (57/330) objective response rate vs. 3% (11/328) with Afinitor (everolimus) in renal cell carcinoma patients (PMID: 27279544). | 27279544 detail... |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Phase II | Actionable | In a Phase II trial, Cabometyx (cabozantinib) treatment demonstrated improved median progression-free survival (8.2 vs 5.6 months) and overall response rate (46% vs 18%) over Sutent (sunitinib) in untreated patients with metastatic renal cell carcinoma (ESMO 2016 Congress in Copenhagen, Abstract LBA30_PR). | detail... |
Unknown unknown | pancreatic endocrine carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib | Preclinical | Actionable | In a preclinical study, Cometriq (cabozantinib) inhibited pancreatic neuroendocrine tumor growth and invasion in transgenic mouse models (PMID: 22585997). | 22585997 |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Cabozantinib + Chloroquine | Preclinical - Cell culture | Actionable | In a preclinical study, Cometriq (Cabometyx, cabozantinib) treatment in combination with Chloroquine enhanced apoptosis in a colorectal cancer cell line in culture (PMID: 30026382). | 30026382 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib + CT-707 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Cometriq (Cabometyx, cabozantinib) and CT-707 resulted in synergism in hepatocellular carcinoma cells, demonstrating increased apoptosis and inhibition of colony formation in culture and decreased tumor weight in xenograft models (PMID: 27638856). | 27638856 |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib + Erlotinib | Phase Ib/II | Actionable | In a Phase Ib/II trial, Cometriq (cabozantinib) and Tarceva (erlotinib) combination treatment resulted in no response (0/13) in patients with non-small cell lung carcinoma that had progressed during treatment with Tarceva (erlotinib) in Phase II, despite an objective response rate of 8.2% (5/61) in Phase I (PMID: 28352985). | 28352985 |
Unknown unknown | triple-receptor negative breast cancer | not applicable | FLT3 Inhibitor | Cabozantinib + Navitoclax | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Navitoclax (ABT-263) and Cometriq (cabozantinib) resulted in a synergistic effect and inhibited the growth of triple-receptor negative breast cancer cells in culture (PMID: 27872098). | 27872098 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Cabozantinib + Nivolumab | FDA approved | Actionable | In a Phase III trial (CHECKMATE-9ER) that supported FDA approval, Opdivo (nivolumab) in combination with Cabometyx (cabozantinib) significantly improved median progression-free survival (16.6 vs 8.3 mo, HR 0.51, P < 0.0001), overall survival (HR 0.60, p<0.0010), and objective response rate (55.7% vs 27.1%, P < 0.0001) compared to Sutent (sunitinib) in patients with advanced real cell carcinoma (Annals of Oncology (2020) 31 (suppl_4): S1142-S1215. 10.1016/annonc/annonc325; NCT03141177). | detail... detail... detail... |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Cabozantinib + SBI-0206965 | Preclinical - Cell culture | Actionable | In a preclinical study, Cometriq (Cabometyx, cabozantinib) treatment in combination with SBI-0206965 enhanced apoptosis in colorectal cancer cells in culture (PMID: 30026382). | 30026382 |
Unknown unknown | prostate cancer | not applicable | FLT3 Inhibitor | Cabozantinib + unspecified CTLA4 antibody + unspecified PD-1 antibody | Preclinical | Actionable | In a preclinical study, combination of myeloid-derived suppressor cell-targeting with Cometriq (cabozantinib) and immune checkpoint blockade with anti-CTLA4 and anti-PD-1 antibodies resulted in synergistic inhibition of tumor growth and metastasis in transgenic mouse models of metastatic castration-resistant prostate cancer (PMID: 28321130). | 28321130 |
Unknown unknown | chronic myelomonocytic leukemia | not applicable | FLT3 Inhibitor | TG101209 | Preclinical - Patient cell culture | Actionable | In a preclinical study, TG101209 inhibited colony formation of granulocytes and macrophages cultured from patients with chronic myelomonocytic leukemia (PMID: 27157043). | 27157043 |
Unknown unknown | adenoid cystic carcinoma | not applicable | FLT3 Inhibitor | Dovitinib | Phase II | Actionable | In a Phase II trial, Dovitinib (TKI258) treatment was tolerated and demonstrated limited clinical activity in patients with adenoid cystic carcinoma, resulting in partial response in 5.9% (2/34) of patients, suppression of overall tumor growth rate, and a median progression-free survival of 8.2 months (PMID: 28377480). | 28377480 |
Unknown unknown | glioblastoma | not applicable | FLT3 Inhibitor | Dovitinib | Phase I | Actionable | In a Phase I trial, Dovitinib (TKI258) treatment resulted in a progression free survival rate at 6 months of 16.7% (2/12) in patients with recurrent glioblastoma (PMID: 27100354). | 27100354 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Dovitinib | Phase III | Actionable | In a Phase III clinical trial, Dovitinib (TKI258) demonstrated efficacy equivalent to Nexavar (sorafenib) in metastatic renal cell carcinoma patients (PMID: 24556040). | 24556040 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Dovitinib | Phase I | Actionable | In a Phase I trial, Dovitinib (TKI258) demonstrated safety and efficacy resulting in 10% (2/20) partial response and 60% (12/20) stable disease in renal cell carcinoma patients (PMID: 23339124). | 23339124 |
Unknown unknown | melanoma | not applicable | FLT3 Inhibitor | Dovitinib | Phase Ib/II | Actionable | In a Phase I/II study, Dovitinib (TKI258) was demonstrated safe, but of limited clinical benefit in patients with advanced melanoma (PMID: 21976540). | 21976540 |
Unknown unknown | gastrointestinal stromal tumor | not applicable | FLT3 Inhibitor | Dovitinib | Phase II | Actionable | In a Phase II clinical trial, Dovitinib (TKI258) demonstrated safety and efficacy in heavily pretreated patients with advanced GISTs (PMID: 24084771). | 24084771 |
Unknown unknown | pancreatic ductal adenocarcinoma | not applicable | FLT3 Inhibitor | Lestaurtinib | Preclinical | Actionable | In preclinical studies, lestaurtinib has been shown to have an antitumor effect in xenograft models of pancreatic ductal adenocarcinoma (PMID: 10473107). | 10473107 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Famitinib | Phase I | Actionable | In a Phase I trial, patients with advanced solid tumors had antitumor activity in response to the receptor tyrosine kinase inhibitor, famitinib (PMID: 24043137). | 24043137 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Famitinib | Phase I | Actionable | In a Phase I trial, renal carcinoma patients treated with Famitinib demonstrated a disease control rate of 87.5%, which included 50% (12/24) with a partial response and 37.5% (9/24) with stable disease, and a PFS of 10.7 mo and an OS of 33 mo (PMID: 24238512). | 24238512 |
Unknown unknown | clear cell renal cell carcinoma | no benefit | FLT3 Inhibitor | Bevacizumab + Sorafenib | Phase III | Actionable | In a Phase II clinical trial, treatment with the combination of Nexavar (sorafenib) and Avastin (bevacizumab) did not result in a significant improvement in progression-free survival compared to treatment with Avastin (bevacizumab) as a single agent (9.2 months vs 7.4 months) in patients with renal clear cell carcinoma (PMID: 26077237). | 26077237 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Bevacizumab + Sorafenib | Phase I | Actionable | In a Phase I trial, the treatment combination of Avastin (bevacizumab) and Nexavar (sorafenib) in patients with advanced solid tumors resulted in stable disease in 25% (29/115) of patients and a partial response in 5% (6/115) of patients (PMID: 25363205). | 25363205 |
Unknown unknown | invasive bladder transitional cell carcinoma | not applicable | FLT3 Inhibitor | Cisplatin + Gemcitabine + Sorafenib | Phase II | Actionable | In a Phase II trial, Nexavar (sorafenib) in combination with Platinol (cisplatin) and Gemzar (gemcitabine) resulted in pathologic complete response in 42.2% (19/45) of patients with muscle-invasive urothelial bladder cancer (J Clin Oncol 35, 2017 (suppl 6S; abstract 345)). | detail... |
Unknown unknown | colon cancer | not applicable | FLT3 Inhibitor | CVX-060 + Sorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of CVX-060 and Nexavar (sorafenib) resulted in increased tumor growth inhibition compared to either agent alone in a colon cancer cell line xenograft model (PMID: 21233403). | 21233403 |
Unknown unknown | hepatocellular carcinoma | no benefit | FLT3 Inhibitor | Dalantercept + Sorafenib | Phase I | Actionable | In a Phase Ib trial, addition of Dalantercept (ACE-041) to Nexavar (sorafenib) was well tolerated, but did not improve the efficacy of Nexavar (sorafenib) in patients with advanced hepatocellular carcinoma, with overall survival ranged from 1.9 to 23.3 months and stable disease as best overall response in 53.3% (11/21) of the patients (PMID: 30352941; NCT02024087). | 30352941 |
Unknown unknown | hepatocellular carcinoma | no benefit | FLT3 Inhibitor | Erlotinib + Sorafenib | Phase III | Actionable | In a Phase III trial, the combination treatment of Nexavar (sorafenib) with Tarceva (erlotinib) compared to Nexavar (sorafenib) plus placebo did not demonstrate an improved overall survival and time to progression in patients with hepatocellular carcinoma (PMID: 25547503). | 25547503 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Fingolimod + Sorafenib | Preclinical | Actionable | In a preclinical study, Gilenya (fingolimod) worked synergistically with Nexavar (sorafenib) to inhibit growth and induce apoptosis in hepatocellular carcinoma cell lines in culture (PMID: 26516583). | 26516583 |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Fluorouracil + Quinacrine + Sorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Acrichine (quinacrine) and Adrucil (5-fluorouracil) synergistically enhanced the cytotoxicity of Nexavar (sorafenib) in human colorectal cancer cell lines in culture (PMID: 21725213). | 21725213 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Fluorouracil + Sorafenib | Phase I | Actionable | In a Phase I trial, Nexavar (sorafenib) in combination with Adrucil (fluorouracil) displayed safety and efficacy in advanced solid tumors, including colon cancer (PMID: 22232731). | 22232731 |
Unknown unknown | colon cancer | not applicable | FLT3 Inhibitor | Fluorouracil + Sorafenib | Phase I | Actionable | In a Phase I trial, Nexavar (sorafenib) in combination with Adrucil (fluorouracil) displayed safety and efficacy in advanced solid tumors, including colon cancer (PMID: 22232731). | 22232731 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | GW5074 + Sorafenib | Preclinical | Actionable | In a preclinical study, the combination of GW5074 and Nexavar (sorafenib) induced cell death in several tumor cell lines, and phosphorylation of DAPK at amino acid S308 correlated positively with response to therapy (PMID: 26100670). | 26100670 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | GW5074 + Sorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of GW5074 and Nexavar (sorafenib) worked synergistically to induce cell death in renal cell carcinoma cells in culture and inhibited tumor growth in xenograft and spontaneous mouse models of renal cell carcinoma (PMID: 26100670). | 26100670 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Intuvax + Sorafenib | Case Reports/Case Series | Actionable | In a Phase I trial, Intuvax (ilixadencel) alone or in combination with Nexavar (sorafenib) demonstrated safety in hepatocellular carcinoma patients, and resulted in one partial response (Intuvax monotherapy), stable disease in 5 patients, increased circulating tumor-specific CD8-positive T-cells in 82% (9/11) of patients receiving Intuvax alone and 50% (2/4) of patients also receiving Nexavar, median time to progression of 5.5 months, and median overall survival of 7.5 months (PMID: 30719425; NCT01974661). | 30719425 |
Unknown unknown | hepatocellular carcinoma | no benefit | FLT3 Inhibitor | Lenalidomide + Sorafenib | Phase I | Actionable | In a Phase I clinical trial, the combination of Revlimid (lenalidomide) and Nexavar (sorafenib) was not well-tolerated and did not demonstrate clinical activity in patients with hepatocellular carcinoma, and the study was terminated early due to toxicity (PMID: 27256874). | 27256874 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Metformin + Sorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, addition of Glucophage (metformin) sensitized hepatocellular carcinoma cells to Nexavar (sorafenib) induced apoptosis in culture, resulted in suppression of postoperative intrahepatic recurrence and lung metastasis in cell line xenograft models (PMID: 26957312). | 26957312 |
Unknown unknown | breast cancer | not applicable | FLT3 Inhibitor | Pemetrexed Disodium + Sorafenib | Phase I | Actionable | In a Phase I clinical trial in patients with advanced solid tumors, the combination of Alimta (pemetrexed) and Nexavar (sorafenib) demonstrated safety and preliminary efficacy in patients with breast cancer, with 58% (7/12) of breast cancer patients achieving objective response or stable disease (PMID: 27213589). | 27213589 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Pemetrexed Disodium + Sorafenib | Phase I | Actionable | In a Phase I clinical trial, the combination of Alimta (pemetrexed) and Nexavar (sorafenib) demonstrated safety and some preliminary efficacy in patients with advanced solid tumors, with an objective response rate of 15% (5/33) and stable disease in 45% (15/33) of patients (PMID: 27213589). | 27213589 |
Unknown unknown | triple-receptor negative breast cancer | not applicable | FLT3 Inhibitor | Pemetrexed Disodium + Sorafenib | Phase I | Actionable | In a Phase I clinical trial in patients with advanced solid tumors, the combination of Alimta (pemetrexed) and Nexavar (sorafenib) demonstrated safety and preliminary efficacy in patients with triple-receptor breast cancer (TNBC), with 60% (3/5) of TNBC patients demonstrating an objective response and 100% (5/5) of patients achieving stable disease or better (PMID: 27213589). | 27213589 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | PX-866 + Sorafenib | Preclinical | Actionable | In a preclinical study, treatment with the combination of Stivarga (regorafenib) PK-866 resulted in increased cell death in a variety of solid tumor cell lines in culture (PMID: 23877009). | 23877009 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Refametinib + Sorafenib | Phase I | Actionable | In a Phase I trial, 43.8% (7/16) of hepatocellular carcinoma patients treated with a combination of Refametinib (BAY86-9766) and Nexavar (sorafenib) demonstrated stable disease (PMID: 26644411). | 26644411 |
Unknown unknown | colorectal cancer | not applicable | FLT3 Inhibitor | Refametinib + Sorafenib | Phase I | Actionable | In a Phase I trial, a patient with colorectal cancer demonstrated a durable partial response for 358 days when treated with the combination of Refametinib (BAY86-9766) and Nexavar (sorafenib) (PMID: 26644411). | 26644411 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Refametinib + Sorafenib | Phase I | Actionable | In a Phase I trial, the combination treatment of Refametinib (BAY86-9766) and Nexavar (sorafenib) in patients with advanced solid tumors resulted in a disease control rate of 65.8% (25/38), specifically, 2.6% (1/38) experienced a partial response and 63.2% (24/38) demonstrated stable disease (PMID: 26644411). | 26644411 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Resminostat + Sorafenib | Phase Ib/II | Actionable | In a Phase I/II trial, the combination of Resminostat (4SC-201) and Nexavar (sorafenib) demonstrated increased efficacy compared to Resminostat (4SC-201) alone in advanced hepatocellular carcinoma patients, resulting in an improved progression-free survival rate of 62.5% vs. 12.5%, a median time to progression of 4.1 vs. 1.8 months, and an overall survival of 8.0 vs. 6.5 months (PMID: 26952006). | 26952006 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Selumetinib + Sorafenib | Phase II | Actionable | In a Phase II trial, Nexavar (sorafenib) and Selumetinib (AZD6244) combination treatment resulted in partial response in 15% (4/27) and stable disease in 48% (13/27) of hepatocellular carcinoma patients (PMID: 27681866). | 27681866 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | SF1126 + Sorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of SF1126 and Nexavar (sorafenib) was synergistic or additive in inhibiting proliferation of hepatocellular carcinoma cell lines in culture, and demonstrated increased efficacy in hepatocellular carcinoma cell line xenograft models compared to SF1126 alone (PMID: 23355037). | 23355037 |
Unknown unknown | endometrial carcinoma | not applicable | FLT3 Inhibitor | Sorafenib | Preclinical | Actionable | In preclinical studies, Nexavar (sorafenib) promoted apoptosis of endometrial carcinoma cells (PMID: 23463670). | 23463670 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Sorafenib | FDA approved | Actionable | In a Phase III trial that supported FDA approval, treatment with Nexavar (sorafenib) resulted in an improved median progression-free survival of 167 days in patients with renal cell carcinoma (PMID: 17189398). | detail... 17189398 |
Unknown unknown | gastrointestinal stromal tumor | not applicable | FLT3 Inhibitor | Sorafenib | Phase II | Actionable | In a Phase II trial, Nexavar (sorafenib) treatment resulted in partial response in 13% (4/31), stable disease in 52% (16/31), a median progression-free survival of 4.9 months and an overall survivals of 9.7 months in gastrointestinal stromal tumor patients who failed prior tyrosine kinase inhibitors (PMID: 22270258). | 22270258 |
Unknown unknown | lung non-small cell carcinoma | no benefit | FLT3 Inhibitor | Sorafenib | Phase III | Actionable | In a Phase III trial (MISSION), Nexavar (sorafenib) treatment in non-small cell lung carcinoma patients did not reach its primary endpoint, resulting in an overall survival similar to that when treated with placebo (8.2 vs 8.3 mo, HR=0.99, p=0.47), however, did meet its secondary endpoint, demonstrating a greater progression free survival (2.8 vs 1.4 mo, HR=0.61, p<0.0001) and time to progression (2.9 vs 1.4 mo, HR=0.54, p<0.0001) when compared to placebo (PMID: 26743856; NCT00863746). | 26743856 |
Unknown unknown | thyroid gland carcinoma | not applicable | FLT3 Inhibitor | Sorafenib | Clinical Study | Actionable | In a clinical case report, Nexavar (sorafenib) therapy based on in vitro efficacy testing using patient-derived tumor cells resulted in 43 months of disease-free in a patient with anaplastic thyroid carcinoma (PMID: 27379749). | 27379749 |
Unknown unknown | adult T-cell leukemia | no benefit | FLT3 Inhibitor | Sorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, adult T cell leukemia cells were not sensitive to treatment with Nexavar (sorafenib) in culture (PMID: 32907612). | 32907612 |
Unknown unknown | Her2-receptor negative breast cancer | not applicable | FLT3 Inhibitor | Sorafenib | Clinical Study | Actionable | In a meta-analysis of 844 ERBB2 (HER2)-negative breast cancer patients, Nexavar (sorafenib) increased progression-free survival time, but not overall survival or objective response rate (PMID: 24940450). | 24940450 |
Unknown unknown | desmoid tumor | not applicable | FLT3 Inhibitor | Sorafenib | Phase III | Actionable | In a Phase III trial, Nexavar (sorafenib) treatment resulted in an increased 2-year progression-free survival compared to placebo (81% vs 36%), an objective response rate of 33% (16/49; 1 complete response and 15 partial responses (PR)) compared in 20% (7/25; all PR) with placebo, and a median time to objective response of 9.6 months, compared to 13.3 months with placebo, in patients with refractory desmoid tumors (PMID: 30575484; NCT02066181). | 30575484 |
Unknown unknown | thyroid gland cancer | not applicable | FLT3 Inhibitor | Sorafenib | FDA approved | Actionable | In a Phase III trial that supported FDA approval, treatment with Nexavar (sorafenib) improved median progression free survival to 10.8 months in metastatic differentiated thyroid cancer patients (PMID: 24768112). | detail... 24768112 |
Unknown unknown | thyroid gland medullary carcinoma | not applicable | FLT3 Inhibitor | Sorafenib | Phase II | Actionable | In a Phase II trial, Nexavar (sorafenib) treatment resulted in partial response in 6.3% (1/16) and stable disease in 87.5% (14/16) of patients with sporadic medullary thyroid carcinoma, with a median progression free survival of 17.9 months (PMID: 20368568). | 20368568 |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Sorafenib | FDA approved | Actionable | In a Phase III trial that supported FDA approval, treatment with Nexavar (sorafenib) improved median progression free survival to 10.7 months in patients with unresectable hepatocellular carcinoma (PMID: 19144678). | 19144678 detail... |
Unknown unknown | hepatocellular carcinoma | not applicable | FLT3 Inhibitor | Sorafenib | Case Reports/Case Series | Actionable | In a Phase I trial, three hepatocellular carcinoma patients treated with Nexavar (sorafenib) following CEBPA-51 (MTL-CEBPA) treatment achieved complete radiological response, 1 with complete radiological response in the liver that was sustained at 9 months, 1 with complete radiological response in the liver and lung lesions that was sustained at 12 months, and 1 with complete radiologcial response in the liver and lungs that was sustained at 7 months (PMID: 32357963; NCT02716012). | 32357963 |
Unknown unknown | clear cell renal cell carcinoma | no benefit | FLT3 Inhibitor | Sorafenib + Temsirolimus | Phase II | Actionable | In a Phase II clinical trial, treatment with the combination of Nexavar (sorafenib) and Torisel (temsirolimus) did not prolong progression-free survival compared to treatment with Avastin (bevacizumab) monotherapy (7.4 months vs 7.5 months) in patients with renal clear cell carcinoma (PMID: 26077237). | 26077237 |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | Bortezomib + Cytarabine + Etoposide + Midostaurin + Mitoxantrone | Phase I | Actionable | In a Phase I trial, Rydapt (midostaurin), in combination with Velcade (bortezomib) and mitoxantrone, Vepesid (etoposide), and Cytosar-U (cytarabine) (MEC), resulted in an overall response rate of 82.5% (19/23) in patients with relapsed or refractory acute myeloid leukemia receiving dose level 3 and above, with complete responses in 56.5% (13/23) of patients (PMID: 26784138). | 26784138 |
Unknown unknown | mast-cell leukemia | not applicable | FLT3 Inhibitor | Midostaurin | FDA approved | Actionable | In a Phase II trial that supported FDA approval, Rydapt (midostaurin) treatment resulted in an overall response rate of 60% (53/89), a median overall survival of 28.7 months, and a median progression-free survival of 14.1 months in patients with systemic mastocytosis including aggressive systemic mastocytosis, systemic mastocytosis with an associated hematologic neoplasm, and mast-cell leukemia (PMID: 27355533; NCT00782067). | detail... 27355533 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Midostaurin | Phase I | Actionable | In a Phase I trial, Rydapt (midostaurin) demonstrated safety in patients with advanced solid tumors (PMID: 11230495). | 11230495 |
Unknown unknown | colon cancer | not applicable | FLT3 Inhibitor | FN-1501 | Preclinical - Cell culture | Actionable | In a preclinical study, FN-1501 induced cell-cycle arrest decreased proliferation in a colon cancer cell line in culture (PMID: 29357250). | 29357250 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | XL999 | Phase II | Actionable | In six Phase II clinical trials, XL999 demonstrated anti-tumor activity in patients with advanced solid tumors, but also resulted in significant cardiotoxicity, which improved after discontinuation of the drug (J Clin Oncol, 25:18s, 2007 (Suppl; abstr 3591)). | detail... |
Unknown unknown | renal cell carcinoma | no benefit | FLT3 Inhibitor | AGS-003 + Sunitinib | Phase II | Actionable | In a Phase II clinical trial, treatment with the combination of AGS-003 and Sutent (sunitinib) resulted in clinical benefit in 62% (13/21) of patients with advanced renal cell carcinoma, with 9 partial responses and 4 patients achieving stable disease, a median overall survival of 30.2 months, and median progression-free survival of 11.2 months (PMID: 25901286; NCT00678119). | 25901286 |
Unknown unknown | renal cell carcinoma | no benefit | FLT3 Inhibitor | AGS-003 + Sunitinib | Phase III | Actionable | In a Phase III trial (ADAPT), the combination of AGS-003 (Rocapuldencel-T) and Sutent (sunitinib) did not demonstrate improved efficacy compared to Sutent alone in metastatic renal cell carcinoma patients, resulting in median overall survival of 27.7 v 32.4 months, progression-free survival of 6.0 v 7.83 months, and objective response rate of 42.7% (131/307, 9 complete, 122 partial) v 39.4% (61/155, 3 complete, 58 partial) in the combination or monotherapy groups, respectively (PMID: 32034074; NCT01582672). | 32034074 |
Unknown unknown | kidney cancer | not applicable | FLT3 Inhibitor | CVX-060 + Sunitinib | Preclinical | Actionable | In a preclinical study, the combination of CVX-060 and Sutent (sunitinib) demonstrated a trend improved overall survival compared to single agent Sutent (sunitinib) in mouse models of unresected and resected renal cancer, however, also demonstrated increased toxicity (PMID: 27651308). | 27651308 |
Unknown unknown | colon cancer | not applicable | FLT3 Inhibitor | CVX-060 + Sunitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, treatment with the combination of CVX-060 and Sutent (suntinib) resulted in increased tumor growth inhibition compared to either agent alone in a colon cancer cell line xenograft model (PMID: 21233403). | 21233403 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Everolimus + Sunitinib | Phase II | Actionable | In a Phase II trial, Sutent (sunitinib) as first line therapy followed by second line therapy, Afinitor (everolimus), resulted in a greater overall survival (29.5 mo vs 22.4 mo) compared to the reverse treatment of the two therapies in patients with metastatic renal cell carcinoma (PMID: 28327953). | 28327953 |
Unknown unknown | brain glioblastoma multiforme | not applicable | FLT3 Inhibitor | Irinotecan + Sirolimus + Sunitinib + Temozolomide | Clinical Study | Actionable | In two clinical case studies, RIST (rapamycin, irinotecan, sunitinib, temozolomide) resulted in anti-tumor activity in patients with glioblastoma (PMID: 25123598). | 25123598 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Ixabepilone + Sunitinib | Phase I | Actionable | In a Phase I trial, Ixabepilone and Sutent (sunitinib) combination therapy resulted in partial response in 15% (4/27) and stable disease in 48% (13/27) of patients with advanced solid tumors (PMID: 26864210). | 26864210 |
Unknown unknown | glioblastoma | not applicable | FLT3 Inhibitor | PRX177561 + Sunitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of PRX177561 and Sutent (sunitinib) decreased tumor growth and improved time-to-progression, disease-free survival, and overall survival over either agent alone in glioblastoma cell line xenograft models (PMID: 28057017). | 28057017 |
Unknown unknown | thyroid gland cancer | not applicable | FLT3 Inhibitor | SL327 + Sunitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of SL327 and Sutent (sunitinib) worked additively to decrease viability, induce apoptosis, and decrease migration of Taxotere (docetaxel)-resistant anaplastic thyroid cancer cell lines in culture, and to inhibit tumor growth in xenograft models (PMID: 28178630) | 28178630 |
Unknown unknown | endometrial cancer | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In Phase II clinical trials, Sutent (sunitinib) demonstrated efficacy in patients with metastatic or recurrent endometrial carcinoma (PMID: 24882554). | 24882554 |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase III | Actionable | In a Phase III clinical trial, treatment with Sutent (sunitinib) resulted in prolonged disease free survival (HR = 0.761) compared to placebo in post-nephrectomy patients with renal cell carcinoma (ESMO 2016 Congress in Copenhagen, Abstract LBA11_PR). | detail... |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | FDA approved | Actionable | In a Phase III clinical trial that supported FDA approval, treatment with Sutent (sunitinib) resulted in improved median progression free survival (47.3 weeks) and objective response rate (27.5%) in patients with renal cell carcinoma (PMID: 19707433). | 19707433 detail... |
Unknown unknown | high grade ependymoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II clinical trial, Sutent (sunitinib) was well-tolerated in young patients with ependymoma, but did not demonstrate sufficient anti-tumor activity as a single agent, with no patients achieving a sustained objective response (PMID: 27109549). | 27109549 |
Unknown unknown | gastrointestinal stromal tumor | not applicable | FLT3 Inhibitor | Sunitinib | FDA approved | Actionable | In a Phase III clinical trial that supported FDA approval, treatment with Sutent (sunitinib) improved median progression free survival to 27.3 weeks in GIST patients (PMID: 17332278). | 17332278 detail... |
Unknown unknown | colon cancer | not applicable | FLT3 Inhibitor | Sunitinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Sutent (sunitinib) induced apoptosis in colon cancer cells in culture and in cell line xenograft models (PMID: 22912816). | 22912816 |
Unknown unknown | glioblastoma | no benefit | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In multiple Phase II clinical trials, Sutent (sunitinib) failed to demonstrate any benefit in patients with glioblastoma with or without concurrent bevacizumab treatment (PMID: 24424564, PMID: 23086433). | 23086433 24424564 |
Unknown unknown | lung small cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II trial, Sutent (sunitinib) treatment in small cell lung cancer patients resulted in a partial response of 11% (1/9) and stable disease in 30% (3/9) (PMID: 26716400). | 26716400 |
Unknown unknown | paraganglioma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II trial (SNIPP), Sutent (sunitinib) treatment in patients with paraganglioma (PGL, n=11) or pheochromocytoma (PCC, n=14) resulted in an overall response rate of 13% (3/23), including partial responses in one PGL patient and two PCC patients, a disease control rate of 83% (19/23), and median progression-free survival of 13.4 months (PMID: 31105270). | 31105270 |
Unknown unknown | high grade glioma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II clinical trial, Sutent (sunitinib) was well-tolerated in young patients with high grade glioma, but did not demonstrate sufficient anti-tumor activity as a single agent, with no patients achieving a sustained objective response (PMID: 27109549). | 27109549 |
Unknown unknown | high grade glioma | not applicable | FLT3 Inhibitor | Sunitinib | Preclinical | Actionable | In a preclinical study, Sutent (sunitinb) induced cell death and decreased proliferation of glioma cells in culture (PMID: 25458015). | 25458015 |
Unknown unknown | pheochromocytoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II trial (SNIPP), Sutent (sunitinib) treatment in patients with pheochromocytoma (PCC, n=14) or paraganglioma (PGL, n=11) resulted in an overall response rate of 13% (3/23), including partial responses in two PCC patients and one PGL patient, a disease control rate of 83% (19/23), and median progression-free survival of 13.4 months (PMID: 31105270). | 31105270 |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II trial, Sutent (sunitinib) treatment in non-small cell lung cancer patients resulted in an objective response rate of 11.1% (7/63), stable disease in 28.6% (18/63), and a PFS of 12 weeks and OS of 23.4 weeks (PMID: 18235126). | 18235126 |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase III | Actionable | In a Phase III trial, Sutent (sunitinib) as maintenance therapy resulted in improved progression free survival (4.3 vs 2.6 months) but not overall survival (11.7 vs 12.1 months) compared to placebo in patients with stage IIIB/IV non-small cell lung cancer (PMID: 28161554). | 28161554 |
Unknown unknown | lung non-small cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | Phase II | Actionable | In a Phase II trial, Sutent (sunitinib) treatment resulted in an objective response rate of 8% (1/13, partial response) and stable disease as the best response in 69% (9/13) of non-small cell lung carcinoma patients (PMID: 32312893; NCT01829217). | 32312893 |
Unknown unknown | ovarian cancer | not applicable | FLT3 Inhibitor | Sunitinib | Phase Ib/II | Actionable | In a Phase II trial, Sutent (sunitinib) treatment in ovarian cancer patients resulted in an increased PFS and a response rate of 16.7% (6/36) in those that received Sutent (sunitinib) continuously and a a response rate of 5.4% (2/37) in those that received the drug non-continuously (PMID: 22377563, PMID: 24070205). | 22377563 24070205 |
Unknown unknown | pancreatic endocrine carcinoma | not applicable | FLT3 Inhibitor | Sunitinib | FDA approved | Actionable | In a Phase III clinical trial that supported FDA approval, Sutent (sunitinib) demonstrated safety and improved progression free survival in patients with pancreatic neuroendocrine tumors (PMID: 21306237). | 21306237 detail... |
Unknown unknown | renal cell carcinoma | not applicable | FLT3 Inhibitor | Sunitinib + Trametinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, combination of Mekinist (trametinib) and Sutent (sunitinib) effectively inhibited tumor angiogenesis and growth in cell line xenograft models of Sutent (sunitinib)-refractory renal cell carcinoma (PMID: 26487278). | 26487278 |
Unknown unknown | myelofibrosis | not applicable | FLT3 Inhibitor | Fedratinib | FDA approved | Actionable | In a Phase III trial (JAKARTA) that supported FDA approval, Inrebic (fedratinib) demonstrated both clinical benefits and toxicity in myelofibrosis patients, resulting in symptom response rates at week 24 of 36% (33/91), 34% (31/91), and 7% (6/85) in the Fedratinib (SAR302503) 400 mg, 500 mg, and placebo groups, respectively (P<.001) (PMID: 26181658; NCT01437787). | 26181658 detail... |
Unknown unknown | ovarian cancer | not applicable | FLT3 Inhibitor | ENMD-2076 | Phase II | Actionable | In a Phase II clinical trial, ENMD-2076 demonstrated efficacy in patients with recurrent, platinum-resistant ovarian, fallopian tube or peritoneal cancers (PMID: 22921155). | 22921155 |
Unknown unknown | ovarian clear cell carcinoma | no benefit | FLT3 Inhibitor | ENMD-2076 | Phase II | Actionable | In a Phase II trial, ENMD-2076 did not meet efficacy standard, resulted in partial response in 7.9% (3/38) and stable disease in 68.4% (26/38) of patients with recurrent ovarian clear cell carcinoma, with an overall 6-month progression-free survival rate of 22% (PMID: 30108107). | 30108107 |
Unknown unknown | peritoneum cancer | not applicable | FLT3 Inhibitor | ENMD-2076 | Phase II | Actionable | In a Phase II clinical trial, ENMD-2076 demonstrated efficacy in patients with recurrent, platinum-resistant ovarian, fallopian tube or peritoneal cancers (PMID: 22921155). | 22921155 |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | ENMD-2076 | Phase I | Actionable | In a Phase I trial, treatment with ENMD-2076 resulted in a 25% (4/16) overall response rate in patients with acute myeloid leukemia as well as three patients achieving a complete response (with incomplete count recovery) and one patient with a morphological leukemia free state (PMID: 27406088). | 27406088 |
Unknown unknown | fallopian tube cancer | not applicable | FLT3 Inhibitor | ENMD-2076 | Phase II | Actionable | In a Phase II clinical trial, ENMD-2076 demonstrated efficacy in patients with recurrent, platinum-resistant ovarian, fallopian tube or peritoneal cancers (PMID: 22921155). | 22921155 |
Unknown unknown | Advanced Solid Tumor | not applicable | FLT3 Inhibitor | Carboplatin + Rebastinib | Phase Ib/II | Actionable | In a Phase I/II trial, Rebastinib (DCC-2036) and Paraplatin (carboplatin) combination therapy demonstrated acceptable safety, resulted in a partial response in 4.8% (1/21) and stable disease in 48% (10/21) of patients with advanced solid tumors (Annals of Oncology (2020) 31 (suppl_4): S481-S482; NCT03717415). | detail... |
Unknown unknown | ovarian cancer | not applicable | FLT3 Inhibitor | Paclitaxel + Rebastinib | Phase Ib/II | Actionable | In a Phase I/II trial, Rebastinib (DCC-2036) and Taxol (paclitaxel) combination therapy demonstrated acceptable safety, resulted in an objective response rate of 29% (5/17, 5 partial responses) and a clinical benefit rate of 82% in patients with advanced or metastatic platinum-resistant ovarian cancer, 62% (8/13) of patients had a CA-125 response (Annals of Oncology (2020) 31 (suppl_4): S629-S630; NCT03717415). | detail... |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | HM43239 | Preclinical - Cell culture | Actionable | In a preclinical study, HM43239 treatment inhibited downstream signaling, reduced proliferation, and induced apoptosis in an acute myeloid leukemia cell line expressing leukemic stem cell marker in culture (Cancer Res 2019;79(13 Suppl):Abstract nr 1293). | detail... |
Unknown unknown | melanoma | not applicable | FLT3 Inhibitor | SKI-G-801 | Preclinical | Actionable | In a preclinical study, SKI-G-801 treatment reduced tumor burden in a metastatic mouse model of melanoma (Cancer Res 2019;79(13 Suppl):Abstract nr 2010). | detail... |
Unknown unknown | acute myeloid leukemia | not applicable | FLT3 Inhibitor | SKI-G-801 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, SKI-G-801 treatment induced tumor regression in a cell line xenograft model of acute myeloid leukemia (Mol Cancer Ther 2011;10(11 Suppl):Abstract nr C196). | detail... |
Unknown unknown | breast cancer | not applicable | FLT3 Inhibitor | SKI-G-801 | Preclinical | Actionable | In a preclinical study, SKI-G-801 treatment reduced tumor growth in a syngeneic mouse model of breast cancer (Cancer Res 2019;79(13 Suppl):Abstract nr 2010). | detail... |
Unknown unknown | lung cancer | not applicable | FLT3 Inhibitor | SKI-G-801 | Preclinical | Actionable | In a preclinical study, SKI-G-801 treatment reduced tumor growth in a syngeneic mouse model of lung cancer (Cancer Res 2019;79(13 Suppl):Abstract nr 2010). | detail... |
Unknown unknown | hematologic cancer | not applicable | FLT3 Inhibitor | Cenisertib | Phase I | Actionable | In a Phase I clinical trial, Cenisertib (AS703569) demonstrated safety and preliminary efficacy in patients with advanced hematological malignancies (Blood 2008 112:2963). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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