Therapy Detail

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Therapy Name RO5126766
Synonyms
Therapy Description

RO5126766 (VS-6766) is a RAF/MEK inhibitor, which potentially leads to decreased tumor cell growth and inhibition of tumor growth (PMID: 34288272).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RO5126766 Avutometinib|VS-6766|VS6766|VS 6766|CH5126766|CH-5126766|R-7304|RG-7304 MEK inhibitor (Pan) 24 MEK1 Inhibitor 26 MEK2 Inhibitor 24 RAF Inhibitor (Pan) 27 RO5126766 (VS-6766) is a RAF/MEK inhibitor, which potentially leads to decreased tumor cell growth and inhibition of tumor growth (PMID: 34288272).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 N549K endometrial carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 N549K were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR2 S252W endometrial carcinoma sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 inhibited proliferation of endometrial carcinoma cells harboring FGFR2 S252W in culture (PMID: 26438159). 26438159
BRAF V600E melanoma sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 (VS-6766) treatment induced cell cycle arrest, decreased Mek and Erk phosphorylation, and inhibited growth of melanoma cells harboring BRAF V600E in culture (PMID: 25422890). 25422890
BRAF V600E melanoma sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 inhibited proliferation of melanoma cells harboring BRAF V600E in culture (PMID: 26438159). 26438159
FGFR3 Y373C myeloid neoplasm no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR2 amp colorectal adenocarcinoma predicted - sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 inhibited proliferation of FGFR2 amplified colorectal adenocarcinoma cells in culture (PMID: 26438159). 26438159
FGFR2 amp stomach carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified gastric carcinoma cell lines were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
BRAF V600E colorectal adenocarcinoma sensitive RO5126766 Preclinical - Cell line xenograft Actionable In a preclinical study, RO5126766 (VS-6766) inhibited tumor growth in a cell line xenograft model of colorectal adenocarcinoma harboring BRAF V600E (PMID: 23667175). 23667175
FGFR1 amp lung non-small cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR2 K310R FGFR2 N549K endometrial carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring both FGFR2 K310R and N549K were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
NRAS Q61R melanoma sensitive RO5126766 Preclinical - Cell line xenograft Actionable In a preclinical study, RO5126766 (VS-6766) treatment induced cell cycle arrest, decreased Mek and Erk phosphorylation, and inhibited growth of melanoma cells harboring NRAS Q61R in culture, and inhibited tumor growth in cell line xenograft models (PMID: 25422890). 25422890
BRAF V600E thyroid gland papillary carcinoma sensitive RO5126766 Preclinical Actionable In a preclinical study, RO5126766 inhibited Mek signaling and increased radioiodide uptake and response in transgenic animal models of papillary thyroid carcinoma driven by BRAF V600E (PMID: 27669459). 27669459
FGFR1 amp lung squamous cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03681483 Phase I RO5126766 RO5126766 for Patients With Advanced KRAS-Mutant Lung Cancer Active, not recruiting USA 0
NCT04625270 Phase II Defactinib + RO5126766 RO5126766 A Study of Avutometinib (VS-6766) v. Avutometinib (VS-6766) + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation (RAMP 201) Active, not recruiting USA | ITA | GBR | FRA | ESP | CAN | BEL 0
NCT06104488 Phase I RO5126766 A Study of Avutometinib for People With Solid Tumor Cancers Recruiting USA 0
NCT04620330 Phase II Defactinib + RO5126766 RO5126766 A Study of Avutometinib (VS-6766) + Defactinib in Recurrent KRAS G12V, Other KRAS and BRAF Non-Small Cell Lung Cancer (RAMP202) Completed USA | ITA | FRA | ESP | DEU 0
NCT05798507 Phase I RO5126766 Defactinib Identification of Treatment Concentrations of Defactinib or VS-6766 for the Treatment of Patients With Glioblastoma Recruiting USA 0
NCT02407509 Phase I RO5126766 Everolimus + RO5126766 Phase I Trial of VS-6766 Alone and in Combination With Everolimus (RAF/MEK) Recruiting GBR 0


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