Therapy Detail
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| Therapy Name | Alpelisib + Tipifarnib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Alpelisib | Piqray | BYL719 | PIK3CA inhibitor 24 | 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 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). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| PIK3CA R88Q | tonsil squamous cell carcinoma | predicted - sensitive | Alpelisib + Tipifarnib | Case Reports/Case Series | Actionable | In a Phase I/II trial (KURRENT-HN), the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) resulted in a partial response with an 84% reduction in the target lesions and a complete response in the lung in a patient with metastatic squamous cell carcinoma of the tonsil harboring PIK3CA R88Q, with response ongoing at 27 weeks (PMID: 37339176; NCT04997902). | 37339176 |
| HRAS over exp | head and neck squamous cell carcinoma | 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 over exp | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited Mtor and Rsk phosphorylation, induced cell cycle arrest and apoptosis, and synergistically inhibited viability of an HRAS-overexpressing head and neck squamous cell carcinoma cell line in culture and inhibited tumor growth in patient-derived xenograft (PDX) models (PMID: 37339176). | 37339176 |
| PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in patient-derived xenograft (PDX) models of PIK3CA-amplified head and neck squamous cell carcinoma (PMID: 37339176). | 37339176 |
| HRAS G12S | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, treatment with the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) resulted in enhanced tumor growth inhibition compared to monotherapy in a patient-derived xenograft (PDX) model of head and neck squamous cell carcinoma harboring HRAS G12S (PMID: 38219706). | 38219706 |
| PIK3CA H1047R | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited Mtor and Rsk phosphorylation, induced cell cycle arrest and apoptosis, and synergistically inhibited viability of head and neck cancer squamous cell carcinoma cell lines harboring PIK3CA H1047R in culture and inhibited Mtor signaling, induced cell cycle arrest and apoptosis, inhibited proliferation, and induced tumor regression in a cell line xenograft model (PMID: 37339176). | 37339176 |
| 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 |
| PIK3CA E545K | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in a patient-derived xenograft (PDX) model of head and neck squamous cell carcinoma harboring PIK3CA E545K (PMID: 37339176). | 37339176 |
| PIK3CA G118D | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in a patient-derived xenograft (PDX) model of head and neck squamous cell carcinoma harboring PIK3CA G118D (PMID: 37339176). | 37339176 |
| PIK3CA H1047L PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Alpelisib + Tipifarnib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited tumor growth in a patient-derived xenograft (PDX) model of PIK3CA-amplified head and neck squamous cell carcinoma harboring PIK3CA H1047L (PMID: 37339176). | 37339176 |
| 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 |
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| 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 |
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