Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
Therapy Name | Alpelisib + Tipifarnib |
Synonyms | |
Therapy Description | |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Alpelisib | Piqray | BYL719 | PIK3CA inhibitor 18 | Piqray (alpelisib) is a selective PIK3CA inhibitor that blocks activation of the PI3K signaling pathway and inhibits tumor growth (PMID: 23726034). Piqray (alpelisib) is FDA approved in combination with fulvestrant for use in postmenopausal women, and men, with advanced or metastatic hormone receptor (HR)-positive, ERBB2 (HER2)-negative, PIK3CA-mutant breast cancer (FDA.gov). |
Tipifarnib | Zarnestra|R115777 | Farnesyltransferase Inhibitor 3 | 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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
HRAS G12V | head and neck squamous cell carcinoma | predicted - sensitive | Alpelisib + Tipifarnib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Piqray (alpelisib) sensitized head and neck squamous cell carcinoma cell lines harboring HRAS G12V to treatment with Zarnestra (tipifarnib), resulting in enhanced growth inhibition and apoptosis in culture (PMID: 35247914). | 35247914 |
HRAS over exp | head and neck squamous cell carcinoma | predicted - sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, Zarnestra (tipifarnib) and Piqray (Alpelisib) combination treatment resulted in enhanced tumor regression in patient-derived xenograft (PDX) models of head and neck squamous cell carcinoma overexpressing wild-type Hras (J Clin Oncol 38: 2020 (suppl; abstr e15658)). | detail... |
HRAS G12D | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Cell culture | Actionable | In a preclinical study, the addition of Piqray (alpelisib) sensitized head and neck squamous cell carcinoma cell lines harboring HRAS G12D to treatment with Zarnestra (tipifarnib), resulting in enhanced growth inhibition and increased apoptosis in culture (PMID: 35247914). | 35247914 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT04997902 | Phase Ib/II | Alpelisib + Tipifarnib | Combination Trial of Tipifarnib and Alpelisib in Adult Recurrent/ Metastatic Head and Neck Squamous Cell Carcinoma (R/M HNSCC) | Recruiting | USA | 0 |