Therapy Detail
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| Therapy Name | Binimetinib |
| Synonyms | |
| 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) 23 MEK1 Inhibitor 25 MEK2 Inhibitor 23 | 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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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF V600E MAP2K1 P306H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P306H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S331R | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S331R in culture (PMID: 36442478). | 36442478 |
| BRAF R239Q BRAF L597S | 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 |
| BRAF S363F BRAF K601E | 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 |
| NRAS Q61K | colorectal cancer | predicted - sensitive | Binimetinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) treatment resulted in stable disease in two patient with colorectal cancer harboring NRAS Q61K, whom remained on treatment for 12 and 17 months until disease progression (PMID: 33637626; NCT02465060). | 33637626 |
| BRAF R506_K507insLLR | Advanced Solid Tumor | predicted - sensitive | Binimetinib | Preclinical - Biochemical | Actionable | In a preclinical study, Mektovi (binimetinib) treatment inhibited Erk signaling in cells expressing BRAF R506_K507insLLR in culture (PMID: 34108213). | 34108213 |
| BRAF V600E MAP2K1 D303N | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D303N in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 W247* | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 W247* in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P293S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P293S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V93F | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V93F in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V258I | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V258I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 N345T | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 N345T in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 D67Y | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D67Y in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Y134C | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Y134C in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S72G | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S72G in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R108Q | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R108Q in culture (PMID: 36442478). | 36442478 |
| 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 MAP2K1 L115P | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L115P was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| 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 |
| 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 |
| 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 |
| MAP2K1 F129L | ovarian serous carcinoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a low grade serous ovarian cancer cell line harboring MAP2K1 F129L was resistant to treatment with Mektovi (binimetinib) in culture (PMID: 36198031). | 36198031 |
| 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 |
| BRAF V600E MAP2K1 G176S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G176S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 D336H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D336H in culture (PMID: 36442478). | 36442478 |
| 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 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 |
| BRAF V600E MAP2K1 F53_Q58delinsL | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 F53_Q58delinsL was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600X | melanoma | sensitive | Binimetinib | Phase II | Actionable | In a Phase II trial, Binimetinib (MEK162) treatment resulted in a partial response in 20% (8/41) of melanoma patients harboring BRAF V600 mutations, including V600E (33/41), V600K (5/41), and V600R (1/41) (PMID: 23414587; NCT01320085). | 23414587 |
| NRAS Q61R | colorectal cancer | predicted - sensitive | Binimetinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) treatment resulted in an unconfirmed partial response in a patient with colorectal cancer harboring NRAS Q61R, with a 48.2% tumor reduction at cycle 4, but the disease progressed at cycle 7 (PMID: 33637626; NCT02465060). | 33637626 |
| BRAF V600E MAP2K1 R349K | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R349K in culture (PMID: 36442478). | 36442478 |
| 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 |
| 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 |
| BRAF V600E MAP2K1 S212N | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S212N in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Q56_G61delinsR | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Q56_G61delinsR was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| NRAS Q61X | Advanced Solid Tumor | unknown | Binimetinib | Phase II | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) therapy led to a nonpromising objective response rate of 2.1% (1/47) in patients (pts) with advanced solid tumors harboring NRAS G12/13 or Q61 mutations, Q61-mutant pts achieved longer overall survival (13.1 vs 5.5 mo, p=0.04) and progression-free survival (5.8 vs 1.8 mo, p=0.006) compared to G12/13-mutant pts examining all tumor types, but not when colorectal caner was excluded (HR 0.84, p=0.70; HR 0.67, p=0.4, respectively) (PMID: 33637626; NCT02465060). | 33637626 |
| NRAS Q61K PIK3CA E545K | melanoma | predicted - resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K was resistant to treatment with Mektovi (binimetinib) in culture (PMID: 29496665). | 29496665 |
| 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 |
| 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 (dabrafenib) resulted in disease progression after two cycles (PMID: 30181415; NCT01885195). | 30181415 |
| BRAF V600E MAP2K1 R201H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R201H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S86A | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S86A in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V127M | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V127M in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R201C | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R201C in culture (PMID: 36442478). | 36442478 |
| NRAS Q61R | ameloblastoma | predicted - sensitive | Binimetinib | Case Reports/Case Series | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) treatment resulted in a partial response in a patient with metastatic malignant ameloblastoma harboring NRAS Q61R, and the patient stayed on treatment for 26 months (PMID: 33637626; NCT02465060). | 33637626 |
| BRAF V600E MAP2K1 S200Y | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S200Y in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R49H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R49H in culture (PMID: 36442478). | 36442478 |
| 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 |
| BRAF V600E MAP2K1 R96K | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R96K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P387S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P387S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 L235H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L235H in culture (PMID: 36442478). | 36442478 |
| 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 |
| BRAF V600E MAP2K1 D136N | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D136N in culture (PMID: 36442478). | 36442478 |
| 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... |
| NRAS mutant | skin melanoma | sensitive | Binimetinib | Guideline | Actionable | Mektovi (binimetinib) is included in guidelines as second-line therapy for patients with metastatic or unresectable cutaneous melanoma harboring an NRAS mutation (NCCN.org). | detail... |
| BRAF V600E MAP2K1 M146I | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 M146I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S231L | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S231L in culture (PMID: 36442478). | 36442478 |
| 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 |
| BRAF V600E MAP2K1 K4N | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 K4N in culture (PMID: 36442478). | 36442478 |
| 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 |
| MAP2K1 V211D | Advanced Solid Tumor | predicted - resistant | Binimetinib | Preclinical - Biochemical | Actionable | In a preclinical study, Mektovi (binimetinib) did not inhibit kinase activity of MAP2K1 V211D in an in vitro assay (PMID: 31227518). | 31227518 |
| BRAF V600E MAP2K1 G79V | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G79V in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S150F | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S150F in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 A106T | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A106T in culture (PMID: 36442478). | 36442478 |
| NRAS G12X | Advanced Solid Tumor | no benefit | Binimetinib | Phase II | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) treatment resulted in an objective response rate of 2.1% (1/47) that was deemed nonpromising in patients with advanced solid tumors harboring NRAS mutations at codon 12 (n=17), 13 (n=8), or 61 (n=22), with a 6-month progression-free survival (PFS) of 29.2%, a median PFS of 3.5 months, and a median overall survival of 10.5 months (PMID: 33637626; NCT02465060). | 33637626 |
| BRAF V600E MAP2K1 P326H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P326H in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 K57T | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 K57T was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P105_A106del | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P105_A106del was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| NRAS G13X | Advanced Solid Tumor | no benefit | Binimetinib | Phase II | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) treatment resulted in an objective response rate of 2.1% (1/47) that was deemed nonpromising in patients with advanced solid tumors harboring NRAS mutations at codon 12 (n=17), 13 (n=8), or 61 (n=22), with a 6-month progression-free survival (PFS) of 29.2%, a median PFS of 3.5 months, and a median overall survival of 10.5 months (PMID: 33637626; NCT02465060). | 33637626 |
| 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 |
| BRAF V600E MAP2K1 A132V | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A132V in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 V154I | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 V154I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R291K | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R291K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Q58* | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Q58* in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 A14S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A14S in culture (PMID: 36442478). | 36442478 |
| BRAF K601E MAP2K1 V211D | colon cancer | resistant | Binimetinib | Preclinical - Pdx | Actionable | In a preclinical study, Mektovi (binimetinib) did not inhibit Rsk and Erk phosphorylation, and had no effect on tumor growth in patient-derived xenograft (PDX) models of metastatic colon cancer harboring BRAF K601E and MAP2K1 V211D (PMID: 31227518). | 31227518 |
| BRAF V600E MAP2K1 I99_K104del | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I99_K104del was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P193S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P193S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 G294E | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G294E in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 G276W | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 G276W in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 P162S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P162S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 A76V | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 A76V in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 S327T | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 S327T in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 N382H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 N382H in culture (PMID: 36442478). | 36442478 |
| 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 |
| BRAF V600E MAP2K1 R49C | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R49C in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 L215F | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L215F in culture (PMID: 36442478). | 36442478 |
| 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 |
| BRAF V600E MAP2K1 L63_D67del | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 L63_D67del in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 R47Q | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 R47Q in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 E367K | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E367K in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 E102_I103del | melanoma | resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring BRAF V600E and expressing MAP2K1 E102_I103del was resistant to Mektovi (binimetinib) in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 Y229H | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 Y229H in culture (PMID: 36442478). | 36442478 |
| NRAS Q61L PIK3CA E545K | melanoma | predicted - resistant | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K was resistant to treatment with Mektovi (binimetinib) in culture (PMID: 29496665). | 29496665 |
| BRAF V600E MAP2K1 M94I | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 M94I in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 D351G | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 D351G in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 C121S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 C121S in culture (PMID: 36442478). | 36442478 |
| BRAF V600E MAP2K1 I310L | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 I310L in culture (PMID: 36442478). | 36442478 |
| NRAS Q61X | colorectal cancer | unknown | Binimetinib | Phase II | Actionable | In a Phase II trial (MATCH), Mektovi (binimetinib) treatment did not demonstrate promising efficacy in patients with advanced solid tumors harboring NRAS mutations at codon 12 (n=17), 13 (n=8), or 61 (n=22), however, colorectal cancer patients harboring NRAS Q61 mutations (n=8) achieved longer overall survival (HR 0.34, p=0.03) and progression-free survival (HR 0.23, p=0.007) compared to those harboring mutations at G12 or G13 (n=16) (PMID: 33637626; NCT02465060). | 33637626 |
| 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 |
| BRAF V600E MAP2K1 P264S | melanoma | sensitive | Binimetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mektovi (binimetinib) inhibited viability of a melanoma cell line harboring BRAF V600E and expressing MAP2K1 P264S in culture (PMID: 36442478). | 36442478 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04801966 | Phase 0 | Palbociclib Alpelisib Atezolizumab Vemurafenib Ribociclib Talazoparib Cobimetinib Trametinib Abemaciclib Dabrafenib Nivolumab Binimetinib Pembrolizumab Encorafenib | Safety and Oversight of the Individually Tailored Treatment Approach: A Novel Pilot Study (TAILOR) | Terminated | AUS | 0 |
| 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 | Completed | USA | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUT | AUS | 9 |
| NCT05203172 | FDA approved | Encorafenib Binimetinib + Encorafenib Binimetinib + Encorafenib + Ribociclib Binimetinib + Cetuximab + Encorafenib Binimetinib | The FLOTILLA Study: Providing Continued Access to The Study Medicines Encorafenib and Binimetinib for Participants in Prior Clinical Trials | Recruiting | USA | ITA | FRA | ESP | CAN | AUS | 6 |
| NCT02285439 | Phase Ib/II | Binimetinib | Study of MEK162 for Children With Low-Grade Gliomas | Active, not recruiting | USA | 0 |
| NCT03231306 | Phase II | Binimetinib | Phase II Study of Binimetinib in Children and Adults With NF1 Plexiform Neurofibromas (NF108-BINI) | Active, not recruiting | USA | 0 |
| 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 | Terminated | USA | 0 |
| NCT01885195 | Phase II | Binimetinib | MEK162 for Patients With RAS/RAF/MEK Activated Tumors | Completed | USA | 0 |
| NCT01801358 | Phase Ib/II | Binimetinib Binimetinib + Sotrastaurin | A Phase Ib/II Study of AEB071 and MEK162 in Adult Patients With Metastatic Uveal Melanoma | Terminated | USA | GBR | FRA | ESP | DEU | 1 |
| NCT05286788 | Phase II | Binimetinib | MEKTOVI for the Treatment of Pediatric Adamantinomatous Craniopharyngioma | Recruiting | USA | GBR | DEU | CAN | AUS | 1 |
| NCT05564377 | Phase II | Selumetinib Olaparib + Selumetinib Binimetinib + Fulvestrant Binimetinib + Palbociclib Nilotinib + Paclitaxel Binimetinib + Fluorouracil + Leucovorin + Oxaliplatin Fluorouracil + Leucovorin + Oxaliplatin Panitumumab + Sotorasib Binimetinib Fulvestrant Sotorasib Ipatasertib + Paclitaxel | Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Registration Trial | Recruiting | USA | 1 |
| NCT01763164 | Phase III | Dacarbazine Binimetinib | Study Comparing the Efficacy of MEK162 Versus Dacarbazine in Unresectable or Metastatic NRAS Mutation-positive Melanoma | Completed | USA | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUT | AUS | 17 |
| 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 | USA | 0 |
| NCT04322383 | Phase II | Binimetinib | Binimetinib for People With Relapsed/Refractory BRAF Wild Type Hairy Cell Leukemia and Variant | Recruiting | USA | 0 |
| 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 | USA | ITA | FRA | ESP | CAN | BEL | 1 |
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