Therapy Detail

Therapy Name Binimetinib
Synonym
Therapy Description

Mektovi (binimetinib) inhibits MEK1 and MEK2 resulting in inhibition of growth factor-mediated signaling and decreased tumor cell proliferation (PMID: 23587417). Mektovi (binimetinib) in combination with Braftovi (encorafenib) is FDA approved for use in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation (FDA.gov).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Binimetinib Mektovi ARRY-162|ARRY-438162|MEK162 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 Mektovi (binimetinib) inhibits MEK1 and MEK2 resulting in inhibition of growth factor-mediated signaling and decreased tumor cell proliferation (PMID: 23587417). Mektovi (binimetinib) in combination with Braftovi (encorafenib) is FDA approved for use in patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation (FDA.gov).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
NRAS Q61K melanoma sensitive Binimetinib Phase II Actionable In a Phase II trial, Binimetinib (MEK162) treatment resulted in partial response in 20% (6/30), and stable disease in 43% (13/30) of melanoma patients harboring NRAS mutations, including Q61L (1/30), Q61K (9/30), and Q61R (15/30) (PMID: 23414587). 23414587
NRAS Q61R melanoma sensitive Binimetinib Phase II Actionable In a Phase II trial, Binimetinib (MEK162) treatment resulted in partial response in 20% (6/30), and stable disease in 43% (13/30) of melanoma patients harboring NRAS mutations, including Q61L (1/30), Q61K (9/30), and Q61R (15/30) (PMID: 23414587). 23414587
BRAF L597S melanoma sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Mektovi (binimetinib) inhibited growth of melanoma cell lines harboring BRAF L597S in culture (PMID: 29903896). 29903896
KRAS Q61H lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS Q61H mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
KRAS G12S lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12S mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
KRAS G12C lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12C mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
NRAS mutant biliary tract cancer predicted - sensitive Binimetinib Phase I Actionable In a Phase I trial, Binimetinib (MEK162) treatment resulted in partial response in a biliary tract cancer patient harboring NRAS mutation (PMID: 28152546) 28152546
KRAS G12V lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12V mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
BRAF V600X melanoma sensitive Binimetinib Phase II Actionable In a Phase II trial, 20% (8/41) of melanoma patients with BRAF V600 mutations had a partial response to Binimetinib (MEK162) (PMID: 23414587). 23414587
HRAS Q61R Advanced Solid Tumor sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing HRAS Q61R demonstrated sensitivity to growth inhibition by Binimetinib (MEK162) in culture (PMID: 26544513). 26544513
NRAS mutant skin melanoma sensitive Binimetinib Phase III Actionable In a Phase III trial, Binimetinib (MEK162) treatment resulted in improved progression free survival (2.8 months), objective response rate (15%, 40/269) and disease control rate (58%, 156/269) compared to Deticene (dacarbazine) (1.5 months, 7%, 25%, respectively) in NRAS-mutant cutaneous melanoma patients (J Clin Oncol 34, 2016 (suppl; abstr 9500)). detail...
BRAF mutant colorectal cancer predicted - sensitive Binimetinib Phase I Actionable In a Phase I trial, Binimetinib (MEK162) treatment resulted in an estimated progression free survival of 1.4 months and overall survival of 7.1 months in colorectal cancer patients harboring BRAF mutations (PMID: 28152546). 28152546
NRAS G12D acute myeloid leukemia sensitive Binimetinib Preclinical Actionable In a preclinical study, Binimetinib (MEK162) inhibited growth of acute myeloid leukemia cells that have been demonstrated to harbor NRAS G12D in culture and decreased disease burden in xenograft models with NRAS G12D (PMID: 24569456, PMID: 11238126). 24569456 11238126
NRAS mutant melanoma conflicting Binimetinib Phase II Actionable In a Phase II trial, Binimetinib (MEK162) treatment resulted in partial response in 20% (6/30), and stable disease in 43% (13/30) of melanoma patients harboring NRAS mutations, including Q61L (1/30), Q61K (9/30), and Q61R (15/30) (PMID: 23414587). 23414587
NRAS mutant melanoma conflicting Binimetinib Phase III Actionable In a Phase III clinical trial, treatment with Binimetinib (MEK162) improved median progression-free survival compared to treatment with Deticene (dacarbazine) (2.8 mo. vs. 1.5 mo.), but did not improve overall survival in patients with NRAS-mutant melanoma (PMID: 28284557). 28284557
BRAF L597S BRAF R239Q melanoma sensitive Binimetinib Preclinical - Pdx & cell culture Actionable In a preclinical study, Mektovi (binimetinib) inhibited growth of patient-derived melanoma cells harboring BRAF L597S, as well as BRAF R239Q, in culture, and induced tumor shrinkage in 25% (3/12) of tumors and delayed tumor growth in a patient-derived xenograft (PDX) model (PMID: 29903896). 29903896
KRAS G12X pancreatic cancer sensitive Binimetinib Preclinical Actionable In a preclinical study, pancreatic cell lines with KRAS codon 12 mutations had increased sensitivity to Binimetinib (MEK162) (PMID: 25167228). 25167228
KRAS mutant colorectal cancer predicted - sensitive Binimetinib Phase I Actionable In a Phase I trial, Binimetinib (MEK162) treatment resulted in an estimated progression free survival (PFS) of 1.5 months and overall survival (OS) of 4.7 months when dosed at 45mg, and PFS of 3.5 months and OS of 9.1 months when dosed at 60mg, in colorectal cancer patients harboring KRAS mutations (PMID: 28152546). 28152546
NRAS amp melanoma predicted - sensitive Binimetinib Preclinical - Pdx Actionable In a preclinical study, Mektovi (binimetinib) treatment resulted in reduced tumor growth and proliferation in two patient-derived xenograft (PDX) melanoma models with NRAS copy number gain and without BRAF or NRAS mutations (PMID: 29245078). 29245078
KRAS G13C lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G13C mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
APC inact mut KRAS G12D PTEN inact mut colorectal cancer no benefit Binimetinib Preclinical Actionable In a preclinical study, Binimetinib (MEK162) increased both apoptosis and proliferation in tumors, resulted in no improvement in survival in transgenic animal models of colorectal cancer driven by APC and PTEN inactivation and KRAS G12D (PMID: 26206338). 26206338
HRAS G12V Advanced Solid Tumor sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing HRAS G12V demonstrated sensitivity to growth inhibition by Binimetinib (MEK162) in culture (PMID: 26544513). 26544513
BRAF V600E colon neuroendocrine neoplasm no benefit Binimetinib Case Reports/Case Series Actionable In Phase II trial, Mektovi (binimetinib) therapy in a patient with recurrent neuroendocrine carcinoma of the colon harboring a BRAF V600E mutation who had previously progressed on Tafinlar (dabrafinib) resulted in disease progression after two cycles (PMID: 30181415; NCT01885195). 30181415
KRAS mutant lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS mutations due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
APC inact mut PTEN inact mut colorectal cancer no benefit Binimetinib Preclinical Actionable In a preclinical study, Binimetinib (MEK162) reduced proliferation in tumors acutely but did not improve survival in transgenic animal models of colorectal cancer driven by APC and PTEN inactivation (PMID: 26206338). 26206338
KRAS Q61K lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS Q61K mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
APC inact mut KRAS G12D colorectal cancer sensitive Binimetinib Preclinical Actionable In a preclinical study, Binimetinib (MEK162) increased apoptosis in tumors and improved survival in transgenic animal models of colorectal cancer driven by APC inactivation and KRAS G12D (PMID: 26206338). 26206338
HRAS mutant Advanced Solid Tumor predicted - sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) inhibited growth and induced apoptosis in human solid tumor cell lines harboring HRAS mutations in culture (PMID: 26544513). 26544513
NRAS Q61L melanoma sensitive Binimetinib Phase II Actionable In a Phase II trial, Binimetinib (MEK162) treatment resulted in partial response in 20% (6/30), and stable disease in 43% (13/30) of melanoma patients harboring NRAS mutations, including Q61L (1/30), Q61K (9/30), and Q61R (15/30) (PMID: 23414587). 23414587
Unknown unknown biliary tract cancer not applicable 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
BRAF V600D NRAS dec exp melanoma no benefit Binimetinib Preclinical - Cell culture Actionable In a preclinical study, a melanoma cell line harboring BRAF V600D and knockdown of NRAS demonstrated a decreased response to Mektovi (binimetinib) relative to cells without NRAS knockdown in culture (PMID: 29245078). 29245078
KRAS G12S pancreatic cancer sensitive Binimetinib Preclinical Actionable In a preclinical study, pancreatic cell lines with KRAS codon 12 mutations had increased sensitivity to Binimetinib (MEK162) (PMID: 25167228). 25167228
KRAS G12R lung adenocarcinoma decreased response Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Binimetinib (MEK162) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12R mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
Unknown unknown Advanced Solid Tumor not applicable 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
BRAF V600E melanoma sensitive Binimetinib Phase II Actionable In a Phase II trial, 20% (8/41) of melanoma patients with BRAF V600 mutations had a partial response to Binimetinib (MEK162) (PMID: 23414587). 23414587
BRAF K601E BRAF S363F melanoma sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Mektovi (binimetinib) inhibited growth of a melanoma cell line harboring BRAF K601E, as well as BRAF S363F, in culture (PMID: 29903896). 29903896
HRAS Q61L Advanced Solid Tumor sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing HRAS Q61L demonstrated sensitivity to growth inhibition by Binimetinib (MEK162) in culture (PMID: 26544513). 26544513
NRAS over exp melanoma predicted - sensitive Binimetinib Preclinical - Cell culture Actionable In a preclinical study, Mektovi (binimetinib) treatment in melanoma cell lines with NRAS overexpression, but without NRAS or BRAF mutations, resulted in reduced downstream signaling and proliferation in cultured cells (PMID: 29245078). 29245078
ATM mut NRAS Q61R melanoma predicted - sensitive Binimetinib Case Reports/Case Series Actionable In a clinical case study, a melanoma patient harboring an ATM mutation and NRAS Q61R demonstrated a partial response and 16 month progression free survival when treated with Binimetinib (MEK162) (PMID: 28514312). 28514312
Clinical Trial Phase Therapies Title Recruitment Status
NCT02089230 Phase Ib/II Binimetinib MEK Inhibitor 162 Relapsed and/or Refractory Acute Myeloid Leukemia (AML) and Poor Prognosis, Not Suitable for or Unwilling to Receive Standard Therapy Active, not recruiting
NCT03231306 Phase II Binimetinib Phase II Study of Binimetinib in Children and Adults With NF1 Plexiform Neurofibromas (NF108-BINI) Recruiting
NCT03170206 Phase Ib/II Palbociclib Binimetinib Binimetinib + Palbociclib Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the MEK Inhibitor Binimetinib (MEK162) for Patients With Advanced KRAS Mutant Non-Small Cell Lung Cancer Recruiting
NCT01763164 Phase III Dacarbazine Binimetinib Study Comparing the Efficacy of MEK162 Versus Dacarbazine in Unresectable or Metastatic NRAS Mutation-positive Melanoma Active, not recruiting
NCT01801358 Phase Ib/II Binimetinib AEB071 + Binimetinib A Phase Ib/II Study of AEB071 and MEK162 in Adult Patients With Metastatic Uveal Melanoma Terminated
NCT01885195 Phase II Binimetinib MEK162 for Patients With RAS/RAF/MEK Activated Tumors Completed
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
NCT01849874 Phase III Binimetinib A Study of MEK162 vs. Physician's Choice Chemotherapy in Patients With Low-grade Serous Ovarian, Fallopian Tube or Peritoneal Cancer Active, not recruiting
NCT02285439 Phase Ib/II Binimetinib Phase I/II Study of MEK162 for Children With Ras/Raf Pathway Activated Tumors Recruiting
NCT01927341 Phase Ib/II Binimetinib Panitumumab Phase Ib/II Study of Efficacy and Safety of MEK162 and Panitumumab, in Adult mCRC Patients With Mutant or Wild-type RAS Tumors Completed