Therapy Detail

Therapy Name AEB071 + Binimetinib
Synonym
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AEB071 Sotrastaurin PKC Inhibitor (Pan) 9 Sotrastaurin (AEB071) is a pan-PKC inhibitor, which induces cell cycle arrest and apoptosis (PMID: 19491325).
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
GNA11 Q209L uveal melanoma sensitive AEB071 + Binimetinib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Binimetinib (MEK162) and Sotrastaurin (AEB071) synergized to inhibit growth in a human uveal melanoma cancer cell line harboring a GNA11 Q209L mutation in culture and in xenograft models, and demonstrated improved efficacy over either agent alone (PMID: 24141786). 24141786
GNAQ mutant uveal melanoma predicted - sensitive AEB071 + Binimetinib Preclinical - Pdx & cell culture Actionable In a preclinical study, the combination of Binimetinib (MEK162) and Sotrastaurin (AEB071) inhibited tumor growth in patient-derived xenograft (PDX) models of uveal melanoma harboring GNAQ mutations, and inhibited growth of GNAQ-mutant uveal melanoma cell lines in culture (PMID: 27507190). 27507190
GNA11 mutant uveal melanoma predicted - sensitive AEB071 + Binimetinib Preclinical - Pdx & cell culture Actionable In a preclinical study, the combination of Binimetinib (MEK162) and Sotrastaurin (AEB071) inhibited tumor growth in patient-derived xenograft (PDX) models of uveal melanoma harboring GNA11 mutations, and inhibited growth of GNA11-mutant uveal melanoma cell lines in culture (PMID: 27507190). 27507190
Clinical Trial Phase Therapies Title Recruitment Status
NCT01801358 Phase Ib/II Binimetinib AEB071 + Binimetinib A Phase Ib/II Study of AEB071 and MEK162 in Adult Patients With Metastatic Uveal Melanoma Terminated