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 |
|---|---|---|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 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 |
| 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 |
| 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 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| 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 |
| NCT02407509 | Phase I | RO5126766 Everolimus + RO5126766 | Phase I Trial of VS-6766 Alone and in Combination With Everolimus (RAF/MEK) | Recruiting | GBR | 0 |
| 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 |
| NCT05798507 | Phase I | RO5126766 Defactinib | Identification of Treatment Concentrations of Defactinib or VS-6766 for the Treatment of Patients With Glioblastoma | Recruiting | USA | 0 |
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