Therapy Detail
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| Therapy Name | Tipifarnib + Trametinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Tipifarnib | Zarnestra|R115777 | Farnesyltransferase Inhibitor 4 | Zarnestra (tipifarnib) is a farnesyltransferase inhibitor, which alters post-translational modification and activation of Ras proteins, and may result in decreased tumor cell proliferation and reduced tumor growth (PMID: 11196150, PMID: 25323927, PMID: 32557577). | |
| Trametinib | Mekinist | GSK1120212 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Mekinist (trametinib) inhibits MEK 1 and 2, which potentially leads to reduced tumor cell proliferation (PMID: 27956260). Mekinist (trametinib) is FDA approved for melanoma patients harboring BRAF V600E or BRAF V600K mutations, and in combination with Tafinlar (dabrafenib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, BRAF V600E-mutant anaplastic thyroid cancer, for adult and pediatric patients of 6 years or older with unresectable or metastatic solid tumors harboring BRAF V600E, and for pediatric patients of 1 year or older with low-grade glioma harboring BRAF V600E (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| HRAS G13R | Advanced Solid Tumor | sensitive | Tipifarnib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Zarnestra (tipifarnib) and Mekinist (trametinib) decreased viability of HRAS-null, NRAS-null, and KRAS knockout cells expressing HRAS G13R compared to Zarnestra (tipifarnib) treatment alone in culture (PMID: 39152269). | 39152269 |
| BRAF G466E HRAS G13R | Advanced Solid Tumor | sensitive | Tipifarnib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, combination treatment with Zarnestra (tipifarnib) and Mekinist (trametinib) resulted in decreased viability of HRAS-null, NRAS-null, and KRAS knockout cells expressing HRAS G13R and BRAF G466E in culture (PMID: 39152269). | 39152269 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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