Therapy Detail

Therapy Name RO5126766
Therapy Description

RO5126766 is dual RAF-MEK1/2 inhibitor with effectiveness against both BRAF and RAS mutated cells (PMID: 25422890).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RO5126766 CH5126766 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 RAF Inhibitor (Pan) 17 RO5126766 is dual RAF-MEK1/2 inhibitor with effectiveness against both BRAF and RAS mutated cells (PMID: 25422890).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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 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
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
FGFR1 amp non-small cell lung 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 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
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 papillary thyroid 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
Unknown unknown Advanced Solid Tumor not applicable RO5126766 Phase I Actionable In a Phase I trial, RO5126766 demonstrated safety and preliminary efficacy in patients with a variety of solid tumors (PMID: 22761467). 22761467
Unknown unknown Advanced Solid Tumor not applicable RO5126766 Phase I Actionable In a Phase I trial, RO5126766 demonstrated safety and some preliminary activity in Japanese patients with advanced solid tumors, with 42% (5/12) of patients achieving stable disease (PMID: 23860959). 23860959
FGFR3-TACC3 bladder transitional cell papilloma no benefit RO5126766 Preclinical - Cell culture Actionable In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO5126766 in culture (PMID: 26438159). 26438159
KRAS G13D colorectal adenocarcinoma sensitive RO5126766 Preclinical - Cell culture Actionable In a preclinical study, RO5126766 inhibited proliferation of colorectal adenocarcinoma cells harboring KRAS G13D in culture (PMID: 26438159). 26438159
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
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
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
Clinical Trial Phase Therapies Title Recruitment Status
NCT03681483 Phase I RO5126766 RO5126766 for Patients With Advanced KRAS-Mutant Lung Cancer Recruiting