Therapy Detail

Therapy Name AZD4547
Synonym
Therapy Description

AZD4547 selectively binds and inhibits FGFR1, 2, and 3, which may result in the inhibition of FGFR-mediated signal transduction pathways and inhibition of tumor cell proliferation (PMID: 22369928).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AZD4547 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 FGFR3 Inhibitor 12 AZD4547 selectively binds and inhibits FGFR1, 2, and 3, which may result in the inhibition of FGFR-mediated signal transduction pathways and inhibition of tumor cell proliferation (PMID: 22369928).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
ETV6-FGFR1 Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, treatment with AZD4547 decreased Myc expression and inhibited growth of transformed cells expressing ETV6-FGFR1 (TEL-FGFR1) in culture (PMID: 27401245). 27401245
FGFR1 amp synovial sarcoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR1 wild-type lung cancer decreased response AZD4547 Preclinical Actionable In a preclinical study, FGFR1 non-amplified lung cancer cell lines demonstrated reduced sensitivity to AZD4547 induced growth inhibition in culture and in xenograft models (PMID: 23082000). 23082000
FGFR1 amp lung cancer sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of lung cancer cell lines harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR1 amp lung small cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a small cell lung cancer cell line harboring FGFR1 amplification in culture (PMID: 23082000). 23082000
FGFR3 amp Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 59% (10/17) of patients with advanced solid tumors harboring FGFR amplification, with a 6-month progression-free survival rate of 15% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR3 N540K Advanced Solid Tumor resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K were reistant to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR1 amp MET amp lung cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, MET amplification was identified as the mechanism mediating acquired AZD4547 resistance in a FGFR1 amplified lung cancer cell line in culture (PMID: 27429073). 27429073
FGFR1 fusion Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in 22% (2/9) and stable disease in 55% (5/9) of patients with advanced solid tumors harboring FGFR fusions, with a 6-month progression-free survival rate of 42% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 V561M non-small cell lung carcinoma resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells expressing FGFR1 V561M demonstrated resistance to AZD4547 in culture (PMID: 30257990). 30257990
FGFR2 S252W endometrial cancer decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells harboring Fgfr2 S252W were less sensitive to the anti-proliferative effects of AZD4547 than the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR1 over exp uterus leiomyosarcoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR2 V564F Advanced Solid Tumor resistant AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells over expressing FGFR2 V564F were resistant to AZD4547 in culture and in cell line xenograft models (PMID: 25169980). 25169980
FGFR3 mutant urinary bladder cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 mutation in culture (PMID: 27550940). 27550940
FGFR1-TACC1 malignant glioma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Fgfr1 kinase activity and cell growth in transformed cells expressing the FGFR1-TACC1 fusion in culture (PMID: 22837387). 22837387
FGFR3 S249C urinary system cancer sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture and in xenograft models (PMID: 27401245). 27401245
FGFR2 amp stomach cancer sensitive AZD4547 Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a 33% (3/9) response rate in patients with FGFR2-amplified gastroesophageal cancer, and high-level amplification was associated with clinical response (PMID: 27179038). 27179038
FGFR2 amp stomach cancer sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited FGFR signaling, and decreased proliferation and induced cell-cycle arrest in gastric cancer cells with amplification and over expression of FGFR2 in culture (PMID: 22869148). 22869148
FGFR3 K650E Advanced Solid Tumor decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR2 amp endometrial cancer sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified endometrial cancer cells in cell line xenograft models (PMID: 27550940). 27550940
FGFR3-BAIAP2L1 urinary bladder cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of a bladder cancer cell line harboring FGFR3-BAIAP2L1 in culture (PMID: 25589496). 25589496
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response AZD4547 Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZD4547 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR2 K660N Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR3-TACC3 Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of transformed cells expressing FGFR3-TACC3 in culture (PMID: 26992226). 26992226
FGFR1 amp non-small cell lung carcinoma sensitive AZD4547 Preclinical - Pdx Actionable In a preclinical study, AZD4547 inhibited FGFR1 signaling and resulted in tumor regression in patient-derived xenograft models of non-small cell lung carcinoma harboring FGFR1 amplification, wild-type for EGFR, K-Ras and negative for EML4-ALK fusion (PMID: 23082000). 23082000
FGFR2 wild-type endometrial cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells with Fgfr2 wild-type were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). 26294741
ETV6-FGFR3 Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, treatment with AZD4547 decreased Myc expression and inhibited growth of transformed cells expressing ETV6-FGFR3 (TEL-FGFR3) in culture (PMID: 27401245). 27401245
FGFR1 positive uterus leiomyosarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR3-TACC3 cervical squamous cell carcinoma predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with squamous cell carcinoma of the cervix harboring FGFR3-TACC3 (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR2 amp colon cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified colon cancer cells in culture (PMID: 27550940). 27550940
FGFR3 over exp transitional cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). 22869148
FGFR1 positive leiomyosarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR3 L608V Advanced Solid Tumor decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to AZD4547 in culture (PMID: 28034880). 28034880
FGFR2 fusion Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in 22% (2/9) and stable disease in 55% (5/9) of patients with advanced solid tumors harboring FGFR fusions, with a 6-month progression-free survival rate of 42% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 amp lung squamous cell carcinoma no benefit AZD4547 Phase I Actionable In a Phase Ib trial, AZD4547 demonstrated limited efficacy in patients with squamous cell lung cancer with FGFR1 amplification, resulting in an overall response rate of 8% (1/15) and a median overall survival of 4.9 months (PMID: 28615371; NCT00979134). 28615371
FGFR2 amp gastric adenocarcinoma no benefit AZD4547 Phase II Actionable In a Phase II trial (SHINE), AZD4547 treatment did not improve progression-free survival compared to Taxol (paclitaxel) (1.8 vs 3.5 months, p=0.9581) in advanced gastric adenocarcinoma patients with FGFR2 amplification (PMID: 29177434; NCT01457846). 29177434
FGFR1 amp Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 59% (10/17) of patients with advanced solid tumors harboring FGFR amplification, with a 6-month progression-free survival rate of 15% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR3 V555M Advanced Solid Tumor resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to AZD4547 in culture (PMID: 28034880). 28034880
FGFR2 over exp breast cancer sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). 22869148
FGFR1 rearrange lung small cell carcinoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of small cell lung cancer cells harboring FGFR1 translocation in culture (PMID: 27550940). 27550940
FGFR2 mutant Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 40% (6/16) of patients with advanced solid tumors harboring FGFR single nucleotide variants, with a 6-month progression-free survival rate of 8% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR2 amp FGFR2 over exp stomach cancer sensitive AZD4547 Preclinical - Pdx Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited tumor growth in patient-derived xenograft (PDX) models of gastric cancer with FGFR2 amplification and over expression (PMID: 27401245). 27401245
FGFR1 mutant Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 40% (6/16) of patients with advanced solid tumors harboring FGFR single nucleotide variants, with a 6-month progression-free survival rate of 8% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR2 over exp endometrial cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells with Fgfr2 overexpression were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). 26294741
FGFR2 amp Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 59% (10/17) of patients with advanced solid tumors harboring FGFR amplification, with a 6-month progression-free survival rate of 15% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 amp MET dec exp lung cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Erk signaling and proliferation of FGFR1-amplified lung cancer cell lines with undetectable Met expression in culture (PMID: 27429073). 27429073
FGFR2 wild-type ERBB2 amp stomach cancer resistant AZD4547 Preclinical Actionable In a preclinical study, gastric cancer cells with wild-type FGFR2 and ERBB2 (HER2) amplification were resistant to treatment with AZD4547 in culture (PMID: 22869148). 22869148
ETV6-FGFR4 Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, treatment with AZD4547 decreased Myc expression and inhibited growth of transformed cells expressing ETV6-FGFR4 (TEL-FGFR4) in culture (PMID: 27401245). 27401245
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive AZD4547 Preclinical - Pdx & cell culture Actionable In a preclinical study, AZD4547 inhibited proliferation of endometrial cells and delayed tumor growth in cell-line derived xenografts harboring the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR1 amp MET pos lung cancer resistant AZD4547 Preclinical - Cell culture Actionable In a preclinical study, FGFR1-amplified lung cancer cell lines with Met expression were resistant to AZD4547 in culture (PMID: 27429073). 27429073
FGFR1 amp breast cancer no benefit AZD4547 Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a response rate of 12.5% (1/8) in patients with FGFR1-amplified breast cancer, and did not meet the predetermined criteria for efficacy (PMID: 27179038). 27179038
FGFR2 N550K endometrial cancer decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, endometrial cells harboring Fgfr2 N550K were less sensitive to the anti-proliferative effects of AZD4547 than the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR3 rearrange myeloid neoplasm sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of myeloma cells harboring FGFR3 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR2 K660E Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR2 amp breast cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified breast cancer cells in culture (PMID: 27550940). 27550940
FGFR3 fusion urinary bladder cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 fusion in culture (PMID: 27550940). 27550940
FGFR3-TACC3 transitional cell carcinoma predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in a patient with urothelial transitional cell carcinoma harboring FGFR3-TACC3 (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR3 wild-type FGFR3 dec exp HRAS G12V transitional cell carcinoma resistant AZD4547 Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZD4547 in culture (PMID: 22869148). 22869148
FGFR2 W290C Advanced Solid Tumor sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR3 mutant Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 40% (6/16) of patients with advanced solid tumors harboring FGFR single nucleotide variants, with a 6-month progression-free survival rate of 8% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
FGFR1 amp lung large cell carcinoma sensitive AZD4547 Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a large cell lung cancer cell line harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR3 amp urinary system cancer sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). 27401245
FGFR3-TACC3 malignant glioma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited Fgfr3 kinase activity in transformed astrocytes expressing the FGFR3-TACC3 fusion in culture (PMID: 22837387). 22837387
FGFR1 rearrange leukemia sensitive AZD4547 Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of leukemia cells harboring FGFR1 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR1 positive synovial sarcoma decreased response AZD4547 Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 pos FGFR2 pos hepatocellular carcinoma sensitive AZD4547 Preclinical - Cell culture Actionable In a preclinical study, hepatocellular carcinoma cell lines treated with AZD4547 demonstrated decreased phosphorylation of FGFR1 and FGFR2, reduced colony formation, and evidence of apoptotic activity in culture (PMID: 26351320). 26351320
FGFR3 fusion Advanced Solid Tumor predicted - sensitive AZD4547 Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in partial response in 22% (2/9) and stable disease in 55% (5/9) of patients with advanced solid tumors harboring FGFR fusions, with a 6-month progression-free survival rate of 42% (J Clin Oncol 36, 2018 (suppl; abstr 2503); NCT02465060). detail...
Clinical Trial Phase Therapies Title Recruitment Status
NCT02465060 Phase II Erdafitinib Copanlisib Trametinib Crizotinib Sunitinib Sapanisertib Nivolumab AZD4547 Dasatinib Pertuzumab + Trastuzumab Dabrafenib + Trametinib Binimetinib Adavosertib Osimertinib Palbociclib Afatinib Capivasertib Defactinib GSK2636771 Vismodegib Ado-trastuzumab emtansine Larotrectinib Taselisib Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) Recruiting
NCT02546661 Phase I AZD9150 + Durvalumab Durvalumab + Selumetinib AZD4547 Durvalumab + Olaparib Durvalumab AZD4547 + Durvalumab Durvalumab + Vistusertib Adavosertib + Durvalumab Open-Label, Randomised, Multi-Drug, Biomarker-Directed, Phase 1b Study in Pts w/ Muscle Invasive Bladder Cancer (BISCAY) Active, not recruiting
NCT02154490 Phase II Docetaxel Palbociclib Durvalumab AZD4547 Taselisib Erlotinib Rilotumumab Lung-MAP: S1400 Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IIIB-IV Squamous Cell Lung Cancer Recruiting