Therapy Detail
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| Therapy Name | Binimetinib + Ribociclib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Binimetinib | Mektovi | ARRY-162|ARRY-438162|MEK162 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | 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). |
| Ribociclib | Kisqali | LEE011|LEE-011|LEE 011 | CDK4/6 Inhibitor 14 | Kisqali (ribociclib) is a dual CDK4/6 inhibitor, which may induce cell cycle arrest and reduce proliferation in cancer cells (PMID: 24045179). Kisqali (ribociclib) is FDA-approved in combination with an aromatase inhibitor in women with hormone receptor-positive, ERBB2 (HER2)-negative breast cancer, and in combination with Faslodex (fulvestrant) in postmenopausal women with hormone receptor-positive, ERBB2 (HER2)-negative breast cancer (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| NRAS Q61K | melanoma | sensitive | Binimetinib + Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) resulted in greater inhibition cell growth compared to either agent alone in a melanoma cell line harboring NRAS Q61K in culture (PMID: 29496665). | 29496665 |
| NRAS Q61K PIK3CA E545K | melanoma | predicted - resistant | Binimetinib + Ribociclib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61K and expressing PIK3CA E545K was resistant to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture and in a cell line xenograft model, demonstrating lack of tumor regression and continued tumor growth (PMID: 29496665). | 29496665 |
| NRAS act mut | melanoma | predicted - sensitive | Binimetinib + Ribociclib | Phase Ib/II | Actionable | In a Phase Ib/II trial, Kisqali (ribociclib) plus Mektovi (binimetinib) was well tolerated in NRAS-mutant melanoma patients and resulted in an overall response rate of 19.5% (8/41; all PR), disease control rate of 70.7% (29/41), median duration of response of 10.3mo, median progression-free survival of 3.7mo, and median overall survival of 11.3mo in phase II, and a response rate of 22.9% (16/70) in patients with an NRAS Q61 mutation, and 12.5% (1/8) with NRAS G12/G13 mutation (PMID: 35294522; NCT01781572). | 35294522 |
| NRAS G13R | melanoma | predicted - sensitive | Binimetinib + Ribociclib | Case Reports/Case Series | Actionable | In a Phase Ib/II trial, combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) resulted in a partial response lasting 119 days in a patient with melanoma harboring NRAS G13R (PMID: 29496665; NCT01781572). | 29496665 |
| NRAS mutant | melanoma | sensitive | Binimetinib + Ribociclib | Phase Ib/II | Actionable | In a Phase Ib/II trial, the combination of Binimetinib (MEK162) and Kisqali (ribociclib) resulted in a partial response in 43% (6/14) and stable disease in 43% (6/14) of NRAS mutant melanoma patients (J Clin Oncol 32:5s, 2014 (Suppl;abstr 9009)). | detail... |
| NRAS mutant | melanoma | sensitive | Binimetinib + Ribociclib | Phase Ib/II | Actionable | In a Phase Ib trial, the combination of Binimetinib (MEK162) and Kisqali (ribociclib) resulted in a median progression-free survival of 6.7 months, a partial response in 25% (4/16), and stable disease in 44% (7/16) of NRAS mutant melanoma patients (J Clin Oncol 35, 2017 (suppl; abstr 9519)). | detail... |
| NRAS Q61L PIK3CA E545K | melanoma | predicted - resistant | Binimetinib + Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, a melanoma cell line harboring NRAS Q61L and expressing PIK3CA E545K was resistant to combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) in culture (PMID: 29496665). | 29496665 |
| NRAS Q61X | melanoma | sensitive | Binimetinib + Ribociclib | Phase Ib/II | Actionable | In a Phase Ib/II trial, Kisqali (ribociclib) plus Mektovi (binimetinib) was well tolerated in NRAS-mutant melanoma patients and resulted in an overall response rate (ORR) of 19.5% (8/41; all PR), disease control rate of 70.7% (29/41), median duration of response of 10.3 months, median progression-free survival of 3.7 months, and median overall survival (OS) of 11.3 months in the phase II cohort, and a response rate of 22.9% (16/70) in patients with an NRAS Q61 mutation overall (PMID: 35294522; NCT01781572). | 35294522 |
| NRAS G13R PIK3CA E545K | melanoma | predicted - resistant | Binimetinib + Ribociclib | Case Reports/Case Series | Actionable | In a Phase Ib/II trial, a patient with melanoma harboring NRAS G13R experienced disease progression on combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib), likely due to the acquisition of PIK3CA E545K (PMID: 29496665; NCT01781572). | 29496665 |
| NRAS Q61L | melanoma | sensitive | Binimetinib + Ribociclib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Mektovi (binimetinib) and Kisqali (ribociclib) resulted in greater inhibition cell growth compared to either agent alone in a melanoma cell line harboring NRAS Q61L in culture (PMID: 29496665). | 29496665 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT01781572 | Phase Ib/II | Binimetinib + Ribociclib | A Phase Ib/II Study of LEE011 in Combination With MEK162 in Patients With NRAS Mutant Melanoma | Completed | USA | NLD | ITA | DEU | AUS | 0 |
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