Therapy Detail

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Therapy Name Buparlisib
Synonyms
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) 37 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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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA E545K lung squamous cell carcinoma sensitive Buparlisib Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). 26013318
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
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 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
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
PIK3CA E39K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E39K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
PIK3CA N345I breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA N345I demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
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
PIK3CA E542K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E542K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
PIK3CA amp lung squamous cell carcinoma no benefit Buparlisib Preclinical - Pdx Actionable In a preclinical study, lung squamous cell carcinoma a patient-derived xenograft (PDX) model harboring PIK3CA amplification, without additional PIK3CA mutations, did not respond to Buparlisib (BKM120) treatment (PMID: 30093452). 30093452
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
ERBB2 amp PIK3CA E545K breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model co-harboring ERBB2 (HER2) amplification and PIK3CA E545K demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
PIK3CA act mut lung squamous cell carcinoma predicted - sensitive Buparlisib Preclinical - Pdx Actionable In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable responses in 4/5 lung squamous cell carcinoma patient-derived xenograft (PDX) models harboring PIK3CA E545K or E542K mutations, 3 that also had PIK3CA amplification and 1 with PTEN loss (PMID: 30093452). 30093452
PIK3CA E542K PIK3CA amp lung squamous cell carcinoma sensitive Buparlisib Preclinical - Pdx Actionable In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable response in a lung squamous cell carcinoma patient-derived xenograft (PDX) model harboring PIK3CA E542K and PIK3CA amplification (PMID: 30093452). 30093452
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
PIK3CA E453K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E453K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
PIK3CA E545K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E545K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
PIK3CA H1047R breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model harboring PIK3CA H1047R demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
PIK3CA H1047R lung squamous cell carcinoma sensitive Buparlisib Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). 26013318
PIK3CA E545K PIK3CA amp lung squamous cell carcinoma predicted - sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, Buparlisib (BKM120) treatment resulted in inhibition of AKT and S6 phosphorylation and durable responses in 2 of 3 lung squamous cell carcinoma patient-derived xenograft (PDX) models harboring PIK3CA E545K and PIK3CA amplification (PMID: 30093452). 30093452
PIK3CA G1049R breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA G1049R demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
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
PIK3CA over exp lung squamous cell carcinoma sensitive Buparlisib Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). 26013318
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

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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 Unknown status
NCT01571024 Phase I Fluorouracil + Leucovorin + Oxaliplatin + Pembrolizumab Buparlisib BKM120 + mFOLFOX6 in Advanced Solid Tumors With Expansion Cohort Pancreatic Cancer Completed
NCT01820325 Phase II Buparlisib Safety and Efficacy of Buparlisib (BKM120) in Patients With Untreated Squamous Non-small Cell Lung Cancer Terminated
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
NCT01833169 Phase II Buparlisib BKM120 for Patients With PI3K-activated Tumors Completed
NCT02340780 Phase II Buparlisib Buparlisib in Patients With Relapsed and Refractory Chronic Lymphocytic Leukemia Completed
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
NCT02220855 Phase II Buparlisib A Study of BKM120 (Buparlisib) in Relapsed or Refractory Thymomas Active, not recruiting
NCT01719250 Phase I Buparlisib Buparlisib in Treating Patients With Relapsed or Refractory Non-Hodgkin Lymphoma Completed
NCT01396499 Phase I Buparlisib Study to Assess Safety, Tolerability and Preliminary Efficacy of BKM120, PI3K Kinase Inhibitor, With Advanced Leukemias Completed
NCT01695473 Phase II Buparlisib Neoadjuvant BKM120 in High-risk Prostate Cancer Completed


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