Therapy Detail

Therapy Name RO4987655
Therapy Description

RO4987655 is a dual MEK1/2 inhibitor, which blocks RAS/RAF/MEK/ERK signaling to prevent cell proliferation (PMID: 21316218).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RO4987655 CH4987655 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 RO4987655 is a dual MEK1/2 inhibitor, which blocks RAS/RAF/MEK/ERK signaling to prevent cell proliferation (PMID: 21316218).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 S252W endometrial carcinoma decreased response RO4987655 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 S252W demonstrated decreased response to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 K310R FGFR2 N549K endometrial carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring both FGFR2 K310R and N549K were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR3 Y373C myeloid neoplasm no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
KRAS mutant non-small cell lung carcinoma sensitive RO4987655 Phase I Actionable In a Phase I trial, 11% (2/11) of NSCLC patients with Kras mutations achieved partial response after treatment with RO4987655 (PMID: 24947927). 24947927
FGFR2 N549K endometrial carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 N549K were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
KRAS G13D colorectal adenocarcinoma sensitive RO4987655 Preclinical - Cell culture Actionable In a preclinical study, RO4987655 inhibited proliferation of colorectal adenocarcinoma cells harboring KRAS G13D in culture (PMID: 26438159). 26438159
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
BRAF V600E melanoma sensitive RO4987655 Preclinical - Cell culture Actionable In a preclinical study, RO4987655 inhibited proliferation of melanoma cells harboring BRAF V600E in culture (PMID: 26438159). 26438159
FGFR1 amp lung squamous cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 amp stomach carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified gastric carcinoma cell lines were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
FGFR2 amp colorectal adenocarcinoma decreased response RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified colorectal adenocarcinoma cells demonstrated decreased response to RO4987655 in culture (PMID: 26438159). 26438159
Unknown unknown Advanced Solid Tumor not applicable RO4987655 Phase I Actionable In a Phase I trial, RO4987655 demonstrated safety and preliminary clinical activity in Japanese patients with advanced solid tumors, including 1 partial response in a patient with esophageal cancer and 7 patients achieving progression-free survival for greater than 16 weeks (PMID: 25809858). 25809858
Unknown unknown Advanced Solid Tumor not applicable RO4987655 Phase I Actionable In a Phase I trial, RO4987655 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (PMID: 22767668). 22767668
FGFR1 amp non-small cell lung carcinoma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
KRAS mutant colorectal cancer no benefit RO4987655 Phase I Actionable In a Phase I trial, none of 30 colorectal cancer patients with KRAS mutations achieved favorable response after treatment with RO4987655 (PMID: 24947927). 24947927
FGFR3-TACC3 bladder transitional cell papilloma no benefit RO4987655 Preclinical - Cell culture Actionable In a preclinical study, bladder transitional cell papilloma cells harboring FGFR3-TACC3 were not sensitive to RO4987655 in culture (PMID: 26438159). 26438159
Clinical Trial Phase Therapies Title Recruitment Status