Therapy Detail

Therapy Name Alpelisib
Therapy Description

Alpelisib (BYL719) is a selective PIK3CA inhibitor that blocks activation of the PI3K signaling pathway and inhibits tumor growth (PMID: 23726034).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Alpelisib BYL719 PIK3CA inhibitor 14 Alpelisib (BYL719) is a selective PIK3CA inhibitor that blocks activation of the PI3K signaling pathway and inhibits tumor growth (PMID: 23726034).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PTEN A126G prostate cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) inhibited Akt signaling and cell migration in prostate cancer cells expressing PTEN A126G in culture (PMID: 26504226). 26504226
FGFR1 amp estrogen-receptor positive breast cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring an FGFR1 amplification demonstrated resistance to Alpelisib (BYL719) in culture (PMID: 27126994). 27126994
KRAS G12V colorectal cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) decreased viability of a colorectal cancer cell line harboring KRAS G12V in culture (PMID: 27602501). 27602501
BRAF mut PTEN inact mut melanoma decreased response Alpelisib Preclinical Actionable In a preclincal study, melanoma cell lines harboring BRAF mutations and PTEN inactivating mutations were less sensitive to Alpelisib (BYL719)-induced growth inhibition in culture (PMID: 26577700). 26577700
PTEN loss breast cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells harboring PTEN loss demonstrated resistance to Alpelisib (BYL719) in culture (PMID: 27604488). 27604488
PTEN C136Y breast cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells harboring PTEN C136Y demonstrated resistance to Alpelisib (BYL719) in culture (PMID: 27604488). 27604488
KRAS amp MET del exon14 non-small cell lung carcinoma no benefit Alpelisib Preclinical - Patient cell culture Actionable In a preclinical study, Alpelisib (BYL719) treatment did not result in apoptotic induction or inhibition of cell proliferation in non-small cell lung carcinoma patient-derived cells harboring KRAS amplification and a MET exon 14 splice site mutation (PMID: 30072474). 30072474
Unknown unknown Advanced Solid Tumor not applicable Alpelisib Phase I Actionable In a Phase I clinical trial, Alpelisib (BYL719) demonstrated safety and some efficacy in patients with advanced solid tumors (PMID: 24617631). 24617631
Unknown unknown Advanced Solid Tumor not applicable Alpelisib Phase I Actionable In a Phase I clinical trial, Alpelisib (BYL719) treatment was well tolerated in Japanese patients with advanced solid tumors and resulted in a 3% (1/33) objective response rate and a disease control rate of 57.6% (19/33, 1 partial response, 18 stable disease) in Japanese patients with advanced solid tumors; disease control rates of 75.0% (6/8) in patients with PIK3CA mutations or amplification vs. 78.6% (11/14) in all patients were observed (PMID: 30588709; NCT01387321). 30588709
Clinical Trial Phase Therapies Title Recruitment Status
NCT03601507 Phase II Alpelisib Alpelisib in Treating Participants With Transorally Resectable HPV-Associated Stage I-IVA Oropharyngeal Cancer Recruiting
NCT03138070 Phase I Alpelisib A Window of Opportunity Study to Assess the Modulation of Biomarkers in Head and Neck Squamous Cell Cancer (HNSCC) By Preoperative Treatment With BYL719 Recruiting
NCT01219699 Phase I Alpelisib Fulvestrant A Study of BYL719 in Adult Patients With Advanced Solid Malignancies, Whose Tumors Have an Alteration of the PIK3CA Gene Active, not recruiting
NCT02537223 Phase I Alpelisib Cisplatin Phase I Study of BYL719 in Combination With Cisplatin and Radiotherapy in Patients With Squamous Cell Head and Neck Cancer Recruiting
NCT02437318 Phase III Alpelisib Fulvestrant Study Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant in Men and Postmenopausal Women With Advanced Breast Cancer Which Progressed on or After Aromatase Inhibitor Treatment. Active, not recruiting