Therapy Detail
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| Therapy Name | TAK-632 |
| Synonyms | |
| Therapy Description |
TAK-632 is an inhibitor of Raf, which has been shown to suppress the kinase activity of the Raf dimer thereby resulting in diminished paradoxical activation of Raf (PMID: 24121489, PMID: 31734178). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| TAK-632 | TAK 632|TAK632 | RAF Inhibitor (Pan) 27 | TAK-632 is an inhibitor of Raf, which has been shown to suppress the kinase activity of the Raf dimer thereby resulting in diminished paradoxical activation of Raf (PMID: 24121489, PMID: 31734178). |
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| BRAF L514V BRAF V600E | melanoma | decreased response | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, melanoma cells expressing BRAF L514V in cis with V600E demonstrated decreased response to TAK-632-induced inhibition of Erk phosphorylation and colony formation compared to cells expressing BRAF V600E in culture (PMID: 29880583). | 29880583 |
| BRAF V600E | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 treatment inhibited Erk phosphorylation and reduced proliferation of a melanoma cells harboring either monomeric BRAF V600E or dimeric isoform (p61) of V600E in culture (PMID: 30559419). | 30559419 |
| BRAF V600E | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of melanoma cell lines harboring either monomeric BRAF V600E or dimeric isoform of V600E which conferred Zelboraf (vemurafenib)-resistance in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | colorectal cancer | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture (PMID: 27523909). | 27523909 |
| BRAF D594G NRAS G12D | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of melanoma cell lines harboring both BRAF D594G and NRAS G12D in culture (PMID: 27523909). | 27523909 |
| BRAF G466V | lung non-small cell carcinoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of non-small cell lung cancer cells harboring BRAF G466V in culture (PMID: 27523909). | 27523909 |
| BRAF L485_P490delinsFS | Advanced Solid Tumor | predicted - sensitive | TAK-632 | Preclinical - Biochemical | Actionable | In a preclinical study, TAK-632 inhibited Mek and Erk phosphorylation in cells expressing BRAF L485_P490delinsFS in culture (PMID: 37656784). | 37656784 |
| BRAF V600D | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of melanoma cell lines harboring BRAF V600D in culture (PMID: 27523909). | 27523909 |
| BRAF L597V NRAS Q61K | lung non-small cell carcinoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of non-small cell lung cancer cells harboring both BRAF L597V and NRAS Q61K in culture (PMID: 27523909). | 27523909 |
| BRAF V600R | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of melanoma cell lines harboring BRAF V600R in culture (PMID: 27523909). | 27523909 |
| BRAF wild-type NRAS wild-type | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of BRAF and NRAS wild-type melanoma cells in culture (PMID: 27523909). | 27523909 |
| NRAS Q61R | melanoma | predicted - sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 treatment inhibited Erk activation and reduced proliferation of melanoma cells harboring NRAS Q61R and wild-type RAF in culture, but at a higher concentration than was required to inhibit melanoma cells harboring BRAF V600E (PMID: 30559419). | 30559419 |
| BRAF G466E | melanoma | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of melanoma cell lines harboring BRAF G466E in culture (PMID: 27523909). | 27523909 |
| BRAF V600E | thyroid cancer | sensitive | TAK-632 | Preclinical - Cell culture | Actionable | In a preclinical study, TAK-632 inhibited proliferation of thyroid cancer cells harboring BRAF V600E in culture (PMID: 27523909). | 27523909 |
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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