Therapy Detail

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Therapy Name Buparlisib + Olaparib
Synonyms
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Buparlisib BKM-120|BKM120 PI3K Inhibitor (Pan) 40 Buparlisib (BKM120) specifically inhibits class I PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, and may result in apoptotic activity and inhibition of cell proliferation (PMID: 22188813).
Olaparib Lynparza AZD2281|KU-0059436 PARP Inhibitor (Pan) 30 Lynparza (olaparib) binds to and inhibits PARP, resulting in inhibition of DNA repair and lethality in homologous-recombination deficient cells, and may be a sensitizing agent for chemotherapy and radiotherapy (PMID: 25028150, PMID: 24225019). Lynparza (olaparib) is FDA approved for treatment of ERBB2 (HER2)-negative breast cancer with deleterious or suspected deleterious germline BRCA mutations, ovarian cancer with deleterious or suspected deleterious germline BRCA mutations and received 3 or more prior therapies, metastatic pancreatic adenocarcinoma with deleterious or suspected deleterious germline BRCA mutations as a maintenance therapy, metastatic castration-resistant prostate cancer (mCRPC) with deleterious or suspected deleterious germline or somatic homologous recombination repair gene mutations who progressed following enzalutamide or abiraterone, in combination with abiraterone in patients with mCRPC harboring deleterious or suspected deleterious BRCA mutations, as a maintenance therapy in recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer and in epithelial ovarian, fallopian tube or primary peritoneal cancer with deleterious or suspected deleterious germline or somatic BRCA mutation, and in combination with Avastin (bevacizumab) as maintenance therapy in HDR defective epithelial ovarian, fallopian tube or primary peritoneal cancer as defined by deleterious or suspected deleterious BRCA mutation, and/or genomic instability (FDA.gov).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA mutant ovarian cancer sensitive Buparlisib + Olaparib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Buparlisib (BKM120) and Lynparza (olaparib) worked synergistically to induce apoptosis and inhibit growth of ovarian cancer cell lines harboring PIK3CA mutations in culture, and induced apoptosis and decreased proliferation of PIK3CA-mutant ovarian cancer cell line xenograft models (PMID: 26909613). 26909613
PTEN negative endometrial carcinoma sensitive Buparlisib + Olaparib Preclinical - Cell culture Actionable In a preclinical study, the combination of Buparlisib (BKM120) and Lynparza (olaparib) resulted in enhanced DNA damage and growth inhibition in PTEN-deficient endometrial carcinoma cell lines in culture (PMID: 28945226). 28945226
PTEN del STK11 del endometrial carcinoma sensitive Buparlisib + Olaparib Preclinical Actionable In a preclinical study, the combination of Buparlisib (BKM120) and Lynparza (olaparib) significantly induced apoptosis and reduced tumor volume by 1.83 fold in a STK11 and PTEN double knock-out mouse model of endometrial carcinoma (PMID: 28945226). 28945226
PTEN del endometrial carcinoma sensitive Buparlisib + Olaparib Preclinical - Cell culture Actionable In a preclinical study, the combination of Buparlisib (BKM120) and Lynparza (olaparib) resulted in enhanced DNA damage and growth inhibition in an endometrial carcinoma cell line with PTEN knocked out via CRISPR/Cas9 system in culture (PMID: 28945226). 28945226

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01623349 Phase I Alpelisib + Olaparib Buparlisib + Olaparib Phase I Study of the Oral PI3kinase Inhibitor BKM120 or BYL719 and the Oral PARP Inhibitor Olaparib in Patients With Recurrent Triple Negative Breast Cancer or High Grade Serous Ovarian Cancer Completed USA 0


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