Molecular Profile Detail

Profile Name BRAF G469L
Gene Variant Detail

BRAF G469L (unknown)

Relevant Treatment Approaches MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor LY3009120

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor WX-554 Phase I Actionable In a Phase I trial, WX-554 was well-tolerated and resulted in stable disease in 59% (20/34) and prolonged stable disease for greater than 6 months in 6% (2/34) of patients with advanced solid tumors (PMID: 27693888). 27693888
Unknown unknown pancreatic cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Gemcitabine + Refametinib Phase Ib/II Actionable In a Phase I/II trial, Refametinib (BAY86-9766) and Gemzar (gemcitabine) combination treatment resulted in an objective response rate of 23% and a disease control rate of 73% in patients with advanced pancreatic cancer (PMID: 27975152). 27975152
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Refametinib Phase I Actionable In a Phase I trial, Refametinib (BAY 86-9766) was well-tolerated and displayed some evidence of clinical benefit across several tumor types (PMID: 23434733). 23434733
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 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 colorectal cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 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 hepatocellular carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 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 Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor BI-847325 Phase I Actionable In a Phase I trial, BI-847325 treatment resulted in stable disease in 30% (21/69) of patients with advanced solid tumors, and one partial response for 67 days in a patient with esophageal cancer (PMID: 26650227). 26650227
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor BI-847325 Phase I Actionable In a Phase I trial, BI-847325 demonstrated safety and some efficacy in a variety of advanced solid tumors (Mol Cancer Ther 2013;12(11 Suppl):B281). detail...
Unknown unknown esophageal cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor BI-847325 Phase I Actionable In a Phase I trial, BI-847325 treatment resulted in stable disease in 30% (21/69) of patients with advanced solid tumors, and one partial response for 67 days in a patient with esophageal cancer (PMID: 26650227). 26650227
Unknown unknown ovarian cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor ABT-737 + AZD8055 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD8055 and Mekinist (trametinib) enhanced the sensitivity of ovarian cancer cells to ABT-737 in culture, resulting in greater apoptotic activity and cell cycle arrest when compared to Mekinist (trametinib) alone (PMID: 27980105). 27980105
Unknown unknown ovarian cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor ABT-737 + BEZ235 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of BEZ235 and Mekinist (trametinib) enhanced the sensitivity of ovarian cancer cells to ABT-737 in culture, resulting in decreased cell viability (PMID: 27980105). 27980105
Unknown unknown ovarian cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor ABT-737 + MK2206 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of MK2206 and Mekinist (trametinib) enhanced the sensitivity of ovarian cancer cells to ABT-737 in culture, resulting in decreased cell viability (PMID: 27980105). 27980105
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Afuresertib + Trametinib Phase I Actionable In a Phase I trial, the combination of Mekinist (trametinib) and Afuresertib (GSK2110183) was not well-tolerated in patients with advanced solid tumors (PMID: 25417902). 25417902
Unknown unknown melanoma sensitive MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor AMG 232 + Trametinib Phase I Actionable In a Phase I trial, the combination therapy of AMG 232 and Mekinist (trametinib) in 15 patients with metastatic cutaneous melanoma without a BRAF V600 mutation resulted in a partial response in 2 patients, stable disease in 11 patients, and progressive disease in 2 patients, and of the 15 patients, 11 experienced tumor reduction (J Clin Oncol 35, 2017 (suppl; abstr 2575)). detail...
Unknown unknown lung cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor AZ628 + Trametinib Preclinical - Cell culture Actionable In a preclinical study, the combination of Mekinist (trametinib) and AZ628 resulted in greater inhibition of Mek and apoptosis in a non-BRAF V600 mutant lung cancer cell line in culture compared to the combination of Mekinist (trametinib) and Tafinlar (dabrafenib) (J Clin Oncol 35, 2017 (suppl; abstr e23154)). detail...
Unknown unknown ovarian cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Buparlisib + Trametinib Phase Ib/II Actionable In a Phase Ib trial, ovarian cancer patients demonstrated an objective response rate of 21% (6/21), including 1 complete response and 5 partial responses, to treatment with Buparlisib (BKM120) in combination with Mekinist (trametinib) (PMID: 25500057) 25500057
Unknown unknown lung non-small cell carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Docetaxel + Trametinib Phase I Actionable In a Phase I/Ib trial, treatment with the combination of Mekinist (trametinib) and Taxotere (docetaxel) resulted in an overall response rate (ORR) of 21% (10/47, all partial responses) and stable disease in 43% (20/47) of patients with non-small cell lung cancer (PMID: 27876675). 27876675
Unknown unknown lung squamous cell carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Docetaxel + Trametinib Phase I Actionable In a Phase I/Ib trial, treatment with the combination of Mekinist (trametinib) and Taxotere (docetaxel) resulted in partial response in 1 patient and stable disease in 3 patients within the subset of 5 evaluable patients with squamous non-small cell lung cancer patients (PMID: 27876675). 27876675
Unknown unknown colorectal cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Fluorouracil + Trametinib Preclinical Actionable In preclinical studies, Mekinist (trametinib) enhanced the efficacy of Adrucil (fluorouracil) in colorectal cancer cells in culture (PMID: 23438367). 23438367
Unknown unknown breast cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Gemcitabine + Trametinib Phase Ib/II Actionable In a Phase Ib clinical trial, the combination of Mekinist (trametinib) and Gemzar (gemcitabine) demonstrated safety and preliminary anti-tumor activity in patients with advanced solid tumors, including one complete response in a patient with breast cancer (PMID: 23583440). 23583440
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Gemcitabine + Trametinib Phase Ib/II Actionable In a Phase Ib trial, the combination of Mekinist (trametinib) and Gemzar (gemcitabine) demonstrated safety and preliminary anti-tumor activity in patients with advanced solid tumors (PMID: 23583440). 23583440
Unknown unknown pancreatic cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Gemcitabine + Trametinib Phase Ib/II Actionable In a Phase Ib trial, a partial response was seen in 30% (3/11) of patients with pancreatic cancer after treatment with Mekinist (trametinib) in combination with Gemzar (gemcitabine) (PMID: 23583440). 23583440
Unknown unknown renal cell carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Pazopanib + Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, combination of Mekinist (trametinib) and Votrient (pazopanib) effectively inhibited tumor angiogenesis and growth in cell line xenograft models of renal cell carcinoma (PMID: 26487278). 26487278
Unknown unknown sarcoma no benefit MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Pazopanib + Trametinib Phase Ib/II Actionable In a Phase Ib/II trial, the combination of Votrient (pazopanib) and Mekinist (trametinib) demonstrated safety and resulted in partial response in 8% (2/25) and stable disease in 48% (12/25) of patients with advanced soft tissue sarcomas, but did not improve the 4 month progression-free survival rate over Votrient (pazopanib) alone (PMID: 28377484). 28377484
Unknown unknown lung non-small cell carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Pemetrexed + Trametinib Phase I Actionable In a Phase I/Ib trial, treatment with the combination of Mekinist (trametinib) and Alimta (pemetrexed) resulted in an overall response rate of 14% (6/42, all partial responses) and stable disease in 55% (23/42) of patients with non-small cell lung cancer (PMID: 27876675). 27876675
Unknown unknown renal cell carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 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 uveal melanoma no benefit MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Trametinib Phase I Actionable In a Phase I trial, Mekinist (trametinib) treatment resulted in stable disease as best response in 50% (8/16) of patients with uveal melanoma (PMID: 22805292; NCT00687622). 22805292
Unknown unknown oral squamous cell carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Trametinib Phase II Actionable In a Phase II trial, Mekinist (trametinib) treatment in patients with oral cavity squamous cell carcinoma was associated with decreased phosphorylation of Erk1/2 and reduced CD44 expression, and resulted in a partial response in 65% (11/17), stable disease in 29% (5/17), and progressive disease in 1 patient (6%) (PMID: 28151720). 28151720
Unknown unknown pancreatic cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Trametinib Phase I Actionable In a Phase I trial, 42% (11/26) of pancreatic cancer patients demonstrated a decrease in tumor formation when treated with Mekinist (trametinib) (PMID: 22805291). 22805291
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Trametinib + Uprosertib Phase I Actionable In a Phase I trial, the combination of Trametinib (GSK1120212) and Uprosertib (GSK2141795) demonstrated safety and preliminary efficacy in patients with advanced solid tumors (J Clin Oncol (Meeting Abstracts) 2011 29: 3085). detail...
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor RO4987655 Phase I Actionable In a Phase I trial, RO4987655 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (PMID: 22767668). 22767668
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor RO4987655 Phase I Actionable In a Phase I trial, RO4987655 demonstrated safety and preliminary clinical activity in Japanese patients with advanced solid tumors, including 1 partial response in a patient with esophageal cancer and 7 patients achieving progression-free survival for greater than 16 weeks (PMID: 25809858). 25809858
Unknown unknown biliary tract cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Binimetinib Phase I Actionable In a Phase I trial, Binimetinib (MEK162) treatment resulted in complete response in 3.3% (1/30) and partial response in 6.7% (2/30) of patients with biliary tract cancer, with estimated progression free survival of 2.1 months and overall survival of 4.8 months (PMID: 28152546). 28152546
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Binimetinib Phase I Actionable In a Phase I trial, Binimetinib (MEK162) treatment resulted in complete response in 1% (1/91), partial response in 2% (2/91), and stable disease with median duration of 3.94 months in 36% (33/91) of patients with advanced solid tumors (PMID: 28152546). 28152546
Unknown unknown colorectal cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Binimetinib + Fluorouracil + Leucovorin + Oxaliplatin Phase I Actionable In a Phase I clinical trial, the combination of Binimetinib (MEK162) and FOLFOX chemotherapy demonstrated manageable toxicity and preliminary efficacy in metastatic colorectal cancer patients with chemotherapy resistance (J Clin Oncol 34, 2016 (suppl; abstr 2544)). detail...
Unknown unknown ovary epithelial cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Binimetinib + Paclitaxel Phase Ib/II Actionable In a Phase Ib trial, combination therapy with Taxol (paclitaxel) and Mektovi (binimetinib) was tolerable and resulted in an objective response rate of 18% (5/28, 1 complete response, 4 partial responses) and a clinical benefit rate of 57% (16/28, best overall response of stable disease or better) in patients with platinum resistant/refractory epithelial ovarian cancer, and clinical benefit was observed in all patients with MAPK pathway alterations (n=4) (PMID: 29844129; NCT01649336). 29844129
Unknown unknown rhabdomyosarcoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor AZD8055 + Selumetinib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Selumetinib (AZD6244) and AZD8055 worked synergistically to inhibit tumor growth in xenograft models of rhabdomyosarcoma (PMID: 23918606). 23918606
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Dacarbazine + Selumetinib Phase I Actionable In a Phase I trial, the combination of Selumetinib (AZD6244) and Deticene (dacarbazine) demonstrated safety and preliminary efficacy in patients with advanced solid tumors, with partial responses in 17% (4/23) and stable disease for greater than 6 weeks in 65% (15/23) of patients (PMID: 28264648). 28264648
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Docetaxel + Selumetinib Phase I Actionable In a Phase I trial, the combination of Selumetinib (AZD6244) and Taxotere (docetaxel) demonstrated safety and preliminary efficacy in patients with advanced solid tumors, with partial responses in 22% (6/27) and stable disease for greater than 6 weeks in 52% (14/27) of patients (PMID: 28264648). 28264648
Unknown unknown triple-receptor negative breast cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor KW-2450 + Selumetinib Preclinical Actionable In a preclinical study, the combination of KW-2450 and Selumetinib worked synergistically to inhibit growth of triple-negative breast cancer cells in culture (PMID: 26443806). 26443806
Unknown unknown pancreatic adenocarcinoma no benefit MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor MK2206 + Selumetinib Phase II Actionable In a Phase II trial, the combination of Selumetinib (AZD6244) and MK2206 did not result in improved median overall survival compared to mFOLFOX therapy (3.9 mo vs. 6.7 mo) or improved median progression-free survival (1.9 mo vs 2.0 mo) in patients with pancreatic adenocarcinoma (PMID: 27978579). 27978579
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib Clinical Study Actionable In a meta-analysis, Selumetinib (AZD6244) was shown to have modest clinical efficacy as a monotherapy in a variety of solid tumors (PMID: 24716986). 24716986
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib Phase I Actionable In a Phase I trial, treatment with Selumetinib (AZD6244) demonstrated safety and preliminary efficacy patients with advanced solid tumors, with several patients achieving prolonged stable disease (PMID: 18390968). 18390968
Unknown unknown uveal melanoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib Phase II Actionable In a Phase II trial, Selumetinib (AZD6244) improved median progression-free survival (15.9 vs 7 weeks, HR=0.46, p<0.001) but not overall survival (11.8 vs 9.1 months, HR=0.66, p=0.09) compared to chemotherapy in patients with uveal melanoma, but also caused high adverse event rate (PMID: 24938562; NCT01143402). 24938562
Unknown unknown breast cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib Phase I Actionable In a Phase I trial, treatment with Selumetinib (AZD6244) demonstrated safety and preliminary efficacy patients with advanced solid tumors, including patients with breast cancer, with several patients achieving prolonged stable disease (PMID: 18390968). 18390968
Unknown unknown triple-receptor negative breast cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib Preclinical - Cell line xenograft Actionable In a preclinical study, the Mek inhibitor Selumetinib (AZD6244) inhibited tumorigenicity and invasiveness of triple-receptor negative breast cancer cell lines in culture and in cell line xenograft models (PMID: 26384399). 26384399
Unknown unknown multiple myeloma no benefit MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib Phase II Actionable In a Phase II clinical trial, Selumetinib (AZD6244) demonstrated safety and tolerability but had minimal activity with a complete response achieved in 5.6% (2/36) of refractory multiple myeloma patients (PMID: 26446942). 26446942
Unknown unknown pancreatic ductal adenocarcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib + SHP099 Preclinical - Pdx & cell culture Actionable In a preclinical study, the combination of SHP099 and Selumetinib (AZD6244) resulted in greater sensitivity compared to either agent alone in pancreatic ductal adenocarcinoma cells, demonstrating decreased cell viability and reduced colony formation in culture and decreased tumor growth in patient-derived xenograft (PDX) models (PMID: 30045908). 30045908
Unknown unknown triple-receptor negative breast cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib + SHP099 Preclinical - Cell line xenograft Actionable In a preclinical study, the combination therapy of SHP099 and Selumetinib (AZD6244) led to decreased cell viability and reduced colony formation in triple-receptor negative breast cancer cells in culture and tumor regression in xenograft models (PMID: 30045908). 30045908
Unknown unknown ovarian cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Selumetinib + SHP099 Preclinical - Cell culture Actionable In a preclinical study, the combination therapy of Selumetinib (AZD6244) and SHP099 resulted in decreased colony formation and reduced cell viability in ovarian cancer cells in culture and inhibition of tumor growth and reduced tumor angiogenesis in a patient-derived xenograft (PDX) model of ovarian cancer (PMID: 30045908). 30045908
Unknown unknown hepatocellular carcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 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 Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor AZD8330 Phase I Actionable In a Phase I trial, AZD8330 demonstrated safety and some preliminary clinical activity in patients with advanced solid tumors (PMID: 23433846). 23433846
Unknown unknown pancreatic adenocarcinoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Gemcitabine + Pimasertib Phase I Actionable In a Phase I trial, Pimasertib in combination with Gemzar (gemcitabine) demonstrated safety and efficacy in metastatic pancreatic adenocarcinoma patients (PMID: 23846936). 23846936
Unknown unknown pancreatic cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Gemcitabine + Pimasertib Preclinical Actionable In a preclinical study, treatment with Pimasertib (MSC1936369B) followed by Gemzar (gemcitabine) resulted in enhanced inhibition of proliferation and induction of apoptosis in pancreatic cell lines in culture (PMID: 26228206). 26228206
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Pimasertib Phase I Actionable In a Phase I trial, Pimasertib (MSC1936369B) demonstrated safety and some preliminary anti-tumor activity in patients with advanced solid tumors (J Clin Oncol 28:15s, 2010 (suppl; abstr 2504)). detail...
Unknown unknown thyroid cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 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 Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor TAK-733 Phase I Actionable In a Phase I clinical trial, TAK-733 demonstrated safety and some preliminary efficacy in patients with advanced solid tumors with partial response in 5% (2/41) and stable disease in 37% (15/41) of patients (PMID: 27650277). 27650277 detail...
Unknown unknown colorectal cancer no benefit MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Atezolizumab + Cobimetinib Phase III Actionable In a Phase III trial (IMblaze370), Tecentriq (atezolizumab) and Cotellic (cobimetinib) combination treatment did not improve median overall survival (8.9 vs 8.5 months, HR=1.00, p=0.987) compared to Stivarga (regorafenib) in patients with chemotherapy-refractory metastatic colorectal cancer, 91.7% of whom were microsatellite stable or microsatellite instability-low (Annals of Oncology, Volume 29, Issue suppl_5, 1 June 2018; NCT02788279). detail...
Unknown unknown colorectal cancer no benefit MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Atezolizumab + Cobimetinib Phase I Actionable In a Phase Ib trial, Tecentriq (atezolizumab) and Cotellic (cobimetinib) combination treatment resulted in partial response in 7% (7/84) of patients with metastatic colorectal cancer, with a median duration of response of 14.8 months, a disease control rate of 31% (26/84), a median progression-free survival of 1.9 months, and a median overall survival of 10.0 months (Journal of Clinical Oncology 36, no. 4_suppl (February 1 2018) 560-560; NCT01988896). detail...
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Cobimetinib Phase I Actionable In a Phase I trial, Cotellic (cobimetinib) treatment resulted in stable disease for five months or more in five patients with advanced solid tumors (PMID: 27424159). 27424159 detail...
Unknown unknown lymphatic system cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Cobimetinib Phase II Actionable In a Phase II trial, treatment with Cotellic (cobimetinib) in patients with histiocytic neoplasms resulted in a PET overall response rate of 89% (16/18), with complete response in 72% (13/18) and partial response in 17% (3/18), and resulted in stable disease in 6% (1/18) of patients, and at 11.9 months the median duration of response and progression-free survival were not yet reached (PMID: 30867592; NCT01953926). 30867592
Unknown unknown melanoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Cobimetinib Preclinical - Cell line xenograft Actionable In a preclinical study, Cobimetinib (GDC-0973) induced cell death in several human melanoma cell lines in culture and inhibited tumor growth in xenograft models (PMID: 22084396). 22084396
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor Cobimetinib + Ipatasertib Phase I Actionable In a Phase I clinical trial Ipatasertib (GDC-0068), in combination with the Mek inhibitor Cobimetinib (GDC-0973) demonstrated safety and preliminary efficacy in patients with advanced solid tumors (Cancer Res, October 1, 2014 74; CT328). detail...
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor CI-1040 Phase I Actionable In a Phase I trial, CI-1040 treatment resulted in median stable disease for 5.5 months in 28% (19/66) of patients with advanced solid tumors (including colorectal, non-small-cell lung, pancreatic, melanoma, and kidney) and partial response in 1 pancreatic cancer patient (PMID: 16009947). 16009947
Unknown unknown glioblastoma multiforme not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor BI2536 + PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, the combination of BI 2536 and PD-0325901 resulted in greater inhibition of cell proliferation in glioblastoma cells in culture compared to treatment with either agent alone (PMID: 26573800). 26573800
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor PD-0325901 Phase I Actionable In a Phase I clinical trial, PD-0325901 demonstrated preliminary clinical activity in patients with advanced solid tumors, however late-onset dose-limiting toxicities were encountered (PMID: 20215549). 20215549
Unknown unknown colorectal cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor PD-0325901 Phase I Actionable In a Phase I study, PD-325901 demonstrated efficacy but toxicity at current dose was unacceptable (PMID: 21516509). 21516509
Unknown unknown melanoma not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor PD-0325901 Phase I Actionable In a Phase I trial, PD-0325901 demonstrated some efficacy in previously treated melanoma patients, however, there was significant toxicity above 10 mg BID (PMID: 21516509). 21516509
Unknown unknown breast cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor PD-0325901 Phase I Actionable In a Phase I trial, PD-0325901 demonstrated some efficacy, however, the dose administered resulted in a significant degree of toxicity (PMID: 21516509). 21516509
Unknown unknown urinary bladder cancer not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor PD-0325901 + PF-04691502 Preclinical - Pdx Actionable In a preclinical study, PD-0325901, in combination with PF-04691502, delayed tumor growth in patient-derived xenograft models of bladder cancer (PMID: 24442130). 24442130
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor RO5126766 Phase I Actionable In a Phase I trial, RO5126766 demonstrated safety and some preliminary activity in Japanese patients with advanced solid tumors, with 42% (5/12) of patients achieving stable disease (PMID: 23860959). 23860959
Unknown unknown Advanced Solid Tumor not applicable MEK inhibitor (Pan) MEK1 Inhibitor MEK2 Inhibitor RO5126766 Phase I Actionable In a Phase I trial, RO5126766 demonstrated safety and preliminary efficacy in patients with a variety of solid tumors (PMID: 22761467). 22761467
Clinical Trial Phase Therapies Title Recruitment Status