Therapy Detail

Therapy Name Buparlisib
Therapy Description

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).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Buparlisib BKM-120|BKM120 PI3K Inhibitor (Pan) 34 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).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
HRAS Q61L lung squamous cell carcinoma no benefit Buparlisib Preclinical - Cell culture Actionable In a preclinical study, BKM120 did not inhibit growth of a lung squamous cell carcinoma cell line harboring HRAS Q61L in culture (PMID: 26544513) 26544513
Unknown unknown glioblastoma multiforme no benefit Buparlisib Preclinical Actionable In a preclinical study, treatment with BKM120 demonstrated a survival similar to vehicle in transgenic mouse models of glioblastoma and therefore, resulted in no benefit (PMID: 27199435). 27199435
NRAS mutant melanoma sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, Buparlisib (BKM120) treatment in human melanoma cell line xenograft models with brain metastases and harboring an NRAS mutation resulted in inhibition of brain tumor growth and an improved survival benefit (PMID: 27307593). 27307593
ERBB2 amp breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model harboring ERBB2 (HER2) amplification demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
KRAS G13D colon cancer no benefit Buparlisib Preclinical Actionable In a preclinical studu, BKM120 alone failed to induce tumor regression in mouse xenograft models of Kras G13D mutant colorectal cancer (PMID: 24576621). 24576621
Unknown unknown head and neck squamous cell carcinoma not applicable Buparlisib Preclinical Actionable In a preclinical study, Buparlisib (BKM-120) reduced viability of head and neck squamous cell carcinoma (HNSSC) cells in culture and demonstrated anti-tumor activity in HNSSC xenograft models (PMID: 22116303). 22116303
BRAF mutant melanoma sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, Buparlisib (BKM120) treatment in human melanoma cell line xenograft models with brain metastases and harboring a BRAF mutation resulted in inhibition of brain tumor growth (PMID: 27307593). 27307593
PTEN negative lung squamous cell carcinoma sensitive Buparlisib Phase II Actionable In a Phase II trial, one patient with Pten negative squamous NSCLC had a partial response to Buparlisib (BKM120) however, stage 2 of the study was not initiated due to failure of meeting overall stage 1 response endpoints (PMID: 26098748). 26098748
BRCA1 loss FGFR2-DNM3 triple-receptor negative breast cancer decreased response Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, BRCA1-deficient triple-receptor negative breast cancer xenograft models treated with BKM120 demonstrated only delayed tumor progression when compared to treatment with BGJ398, which resulted in tumor regression (PMID: 29203461). 29203461
FGFR2-TNS1 triple-receptor negative breast cancer no benefit Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, triple-receptor negative breast cancer xenograft models harboring FGFR2-TNS1 demonstrated stable disease upon treatment with Buparlisib (BKM120), but also exhibited general toxicity (PMID: 29203461). 29203461
ERBB2 T798M breast cancer sensitive Buparlisib Preclinical Actionable In a preclinical study, human breast cancer cells expressing the ERBB2 (HER2) T798M mutation demonstrated sensitivity to BKM120 (PMID: 23948973). 23948973
PTEN loss lung squamous cell carcinoma no benefit Buparlisib Preclinical - Pdx & cell culture Actionable In a preclinical study, lung squamous cell carcinoma patient-derived xenograft (PDX) models harboring PTEN loss did not respond to Buparlisib (BKM120) treatment (PMID: 30093452). 30093452
Unknown unknown Advanced Solid Tumor not applicable Buparlisib Phase I Actionable In a Phase I trial, Buparlisib (BKM120) demonstrated safety and preliminary efficacy in patients with advanced solid tumors (PMID: 22162589). 22162589
Clinical Trial Phase Therapies Title Recruitment Status
NCT01816984 Phase Ib/II Cetuximab Buparlisib PI3K Inhibitor BKM120 and Cetuximab in Treating Patients With Recurrent or Metastatic Head and Neck Cancer Active, not recruiting
NCT01396499 Phase I Buparlisib Study to Assess Safety, Tolerability and Preliminary Efficacy of BKM120, PI3K Kinase Inhibitor, With Advanced Leukemias Completed
NCT01911325 Phase Ib/II Buparlisib Docetaxel Phase II Study of Buparlisib + Docetaxel in Advanced or Metastatic Squamous Non-small Cell Lung Cancer (NSCLC) Patients Terminated
NCT01820325 Phase II Buparlisib Safety and Efficacy of Buparlisib (BKM120) in Patients With Untreated Squamous Non-small Cell Lung Cancer Terminated
NCT01719250 Phase I Buparlisib Buparlisib in Treating Patients With Relapsed or Refractory Non-Hodgkin Lymphoma Completed
NCT02340780 Phase II Buparlisib Buparlisib in Patients With Relapsed and Refractory Chronic Lymphocytic Leukemia Active, not recruiting
NCT02301364 Phase II Buparlisib Buparlisib (BKM120) In Patients With Recurrent/Refractory Primary Central Nervous System Lymphoma (PCNSL) and Recurrent/Refractory Secondary Central Nervous System Lymphoma (SCNSL) Completed
NCT01571024 Phase I Fluorouracil + Leucovorin + Oxaliplatin + Pembrolizumab Buparlisib BKM120 + mFOLFOX6 in Advanced Solid Tumors With Expansion Cohort Pancreatic Cancer Completed
NCT02220855 Phase II Buparlisib A Study of BKM120 (Buparlisib) in Relapsed or Refractory Thymomas Active, not recruiting
NCT01833169 Phase II Buparlisib BKM120 for Patients With PI3K-activated Tumors Completed
NCT01695473 Phase II Buparlisib Neoadjuvant BKM120 in High-risk Prostate Cancer Completed