Therapy Detail
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| Therapy Name | RO5126766 |
| Synonyms | |
| 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) 22 MEK1 Inhibitor 20 MEK2 Inhibitor 18 RAF Inhibitor (Pan) 16 | RO5126766 is dual RAF-MEK1/2 inhibitor with effectiveness against both BRAF and RAS mutated cells (PMID: 25422890). |
Filtering
- Case insensitive filtering will display rows where any text in any cell matches the filter term
- Simple literal full or partial string matches
- Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
- Use quotes to match a longer phrase which contains spaces "mtor c1483f"
Sorting
- Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
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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 |
| 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 |
| 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 |
| 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 |
| 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 | 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 |
| 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 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 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 | 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 |
| 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 |
| 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 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 |
Filtering
- Case insensitive filtering will display rows where any text in any cell matches the filter term
- Simple literal full or partial string matches
- Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
- Use quotes to match a longer phrase which contains spaces "mtor c1483f"
Sorting
- Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.
| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|---|---|---|---|
| NCT03681483 | Phase I | RO5126766 | RO5126766 for Patients With Advanced KRAS-Mutant Lung Cancer | Recruiting |
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