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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). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Buparlisib | BKM-120|BKM120 | PI3K Inhibitor (Pan) 42 | 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 |
---|---|---|---|---|---|---|---|
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 |
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 |
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 E542K PTEN loss | 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 PTEN loss (PMID: 30093452). | 30093452 |
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 |
TSC1 Q516* | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring TSC1 Q516* (PMID: 32767682; NCT01551030). | 32767682 |
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 |
TSC1 Y185* | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring TSC1 Y185* (PMID: 32767682; NCT01551030). | 32767682 |
TSC1 S331Efs*10 TSC1 LOH | transitional cell carcinoma | predicted - sensitive | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in stable disease in a patient with metastatic urothelial carcinoma harboring TSC1 S331Efs*10 and TSC1 loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
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 |
PIK3CA mut PTEN loss | breast cancer | sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, Buparlisib (BKM120) inhibited Akt signaling and growth in a PDX model of breast cancer cells harboring a PIK3CA mutation and PTEN loss ( Cancer Res October 1, 2014 74; LB-327 ). | detail... |
PTEN LOH | transitional cell carcinoma | predicted - sensitive | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in stable disease in a patient with metastatic urothelial carcinoma harboring PTEN loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
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 |
TSC1 R500* TSC1 LOH | transitional cell carcinoma | predicted - sensitive | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in a partial response in a patient with metastatic urothelial carcinoma harboring TSC1 R500* and TSC1 loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
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 E542K TSC1 LOH | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring PIK3CA E542K and TSC1 loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
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 |
PIK3CA amp TSC1 LOH | transitional cell carcinoma | predicted - sensitive | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in a partial response in a patient with metastatic urothelial carcinoma harboring PIK3CA amplification and TSC1 loss of heterozygosity (PMID: 32767682; NCT01551030). | 32767682 |
TSC1 R424fs | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring TSC1 R424fs (PMID: 32767682; NCT01551030). | 32767682 |
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 |
PTEN negative | endometrial carcinoma | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) inhibited Akt signaling, induced DNA damage, and inhibited the growth of PTEN-deficient endometrial carcinoma cell lines in culture (PMID: 28945226). | 28945226 |
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 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 |
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 |
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 |
PTEN del | endometrial carcinoma | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) inhibited Akt signaling, induced DNA damage, and inhibited the growth of an endometrial carcinoma cell line with PTEN knocked out via CRISPR/Cas9 system in culture (PMID: 28945226). | 28945226 |
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 |
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 |
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 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 |
PIK3CA H1047R | transitional cell carcinoma | no benefit | Buparlisib | Case Reports/Case Series | Actionable | In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring PIK3CA H1047R (PMID: 32767682; NCT01551030). | 32767682 |
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 expressing PIK3CA H1047R in culture (PMID: 26013318). | 26013318 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT02220855 | Phase II | Buparlisib | A Study of BKM120 (Buparlisib) in Relapsed or Refractory Thymomas | Completed | USA | 0 |
NCT01820325 | Phase II | Buparlisib | Safety and Efficacy of Buparlisib (BKM120) in Patients With Untreated Squamous Non-small Cell Lung Cancer | Terminated | USA | ITA | ESP | DEU | CAN | 0 |
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 | USA | SWE | ITA | FRA | ESP | DEU | BEL | 1 |
NCT01816984 | Phase Ib/II | Cetuximab Buparlisib | PI3K Inhibitor BKM120 and Cetuximab in Treating Patients With Recurrent or Metastatic Head and Neck Cancer | Completed | USA | 0 |
NCT01719250 | Phase I | Buparlisib | Buparlisib in Treating Patients With Relapsed or Refractory Non-Hodgkin Lymphoma | Completed | USA | 0 |
NCT02340780 | Phase II | Buparlisib | Buparlisib in Patients With Relapsed and Refractory Chronic Lymphocytic Leukemia | Completed | CAN | 0 |
NCT01396499 | Phase I | Buparlisib | Study to Assess Safety, Tolerability and Preliminary Efficacy of BKM120, PI3K Kinase Inhibitor, With Advanced Leukemias | Completed | USA | 0 |
NCT01833169 | Phase II | Buparlisib | BKM120 for Patients With PI3K-activated Tumors | Completed | USA | 0 |
NCT01695473 | Phase II | Buparlisib | Neoadjuvant BKM120 in High-risk Prostate Cancer | Terminated | USA | 0 |
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 | USA | 0 |
NCT01571024 | Phase I | Fluorouracil + Leucovorin + Oxaliplatin + Pembrolizumab Buparlisib | BKM120 + mFOLFOX6 in Advanced Solid Tumors With Expansion Cohort Pancreatic Cancer | Completed | USA | 0 |