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Therapy Name | Pimasertib |
Synonyms | |
Therapy Description |
Pimasertib (MSC1936369B) binds to and inhibits MEK1/2, preventing activation of downstream targets and potentially reducing tumor cell proliferation (PMID: 23587417). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Pimasertib | AS703026|MSC1936369B | MEK inhibitor (Pan) 22 MEK1 Inhibitor 20 MEK2 Inhibitor 18 | Pimasertib (MSC1936369B) binds to and inhibits MEK1/2, preventing activation of downstream targets and potentially reducing tumor cell proliferation (PMID: 23587417, PMID: 31870556). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
BRAF V600E PIK3CA P449T | colorectal cancer | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). | 23629727 |
PIK3CA wild-type | colon cancer | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) treatment inhibited colony formation, and induced cell death and apoptosis in PIK3CA wild-type colon cancer cells in culture (PMID: 30944457). | 30944457 |
CTNNB1 over exp PIK3CA wild-type | colon cancer | resistant | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, overexpression of CTNNB1 in PIK3CA wild-type colon cancer cells suppressed cell death following Pimasertib (MSC1936369B) treatment in culture (PMID: 30944457). | 30944457 |
BRAF V600E | colorectal cancer | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 23629727). | 23629727 |
NRAS Q61K | lung non-small cell carcinoma | sensitive | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) inhibited proliferation of non-small cell lung cancer cells harboring NRAS Q61K in culture (PMID: 23629727). | 23629727 |
Unknown unknown | Advanced Solid Tumor | not applicable | 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... |
PIK3CA mutant | colon cancer | predicted - resistant | Pimasertib | Preclinical - Cell culture | Actionable | In a preclinical study, Pimasertib (MSC1936369B) treatment did not induce cell death, apoptosis, or inhibit colony formation in PIK3CA mutant colon cancer cells in culture (PMID: 30944457). | 30944457 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01992874 | Phase I | Pimasertib | Relative Bioavailability of Pimasertib in Cancer Patients | Completed | USA | 0 |
NCT01693068 | Phase II | Dacarbazine Pimasertib | Phase II Trial of Pimasertib Versus Dacarbazine in N-Ras Mutated Cutaneous Melanoma | Completed | USA | 13 |