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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) 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). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 |
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 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 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 |
MST1R pos PIK3CA wild-type | estrogen-receptor positive breast cancer | predicted - sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, BKM120 inhibited tumor growth in patient-derived xenograft (PDX) models of estrogen-receptor positive breast cancer with wild-type PIK3CA and expressing the short isoform of MST1R (RON) (PMID: 26289070). | 26289070 |
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 |
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 |
ERBB3 V104M | colon cancer | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) treatment inhibited proliferation of a colon cancer cell line harboring ERBB3 (HER3) V104M in culture (PMID: 38751013). | 38751013 |
ERBB3 V104M | urinary bladder cancer | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) treatment inhibited proliferation of a bladder cancer cell line harboring ERBB3 (HER3) V104M in culture (PMID: 38751013). | 38751013 |
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 |
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 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 |
ERBB3 V104M | lung cancer | sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, Buparlisib (BKM120) treatment inhibited proliferation of a lung cancer cell line harboring ERBB3 (HER3) V104M in culture (PMID: 38751013). | 38751013 |
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 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... |
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 | 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 |
MST1R pos PIK3CA E545K | breast cancer | predicted - sensitive | Buparlisib | Preclinical - Cell culture | Actionable | In a preclinical study, BKM120 decreased viability of a breast cancer cell line expressing the constitutively active short isoform of MST1R (RON) and PIK3CA E545K in culture (PMID: 26289070). | 26289070 |
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 |
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 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 |
ERBB3 over exp PIK3CA H1047R | breast cancer | resistant | Buparlisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, a breast cancer cell line xenograft model harboring ERBB3 (HER3) over expression and PIK3CA H1047R in brain metastases demonstrated resistance to treatment with Buparlisib (BKM120) (PMID: 28539475). | 28539475 |
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 |
MST1R pos PIK3CA H1047R | estrogen-receptor positive breast cancer | predicted - sensitive | Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, BKM120 inhibited tumor growth in patient-derived xenograft (PDX) models of estrogen-receptor positive breast cancer harboring PIK3CA H1047R and expressing the short isoform of MST1R (RON) (PMID: 26289070). | 26289070 |
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 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 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 |
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 |
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 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 |
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 |
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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
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 |
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 |
NCT01695473 | Phase II | Buparlisib | Neoadjuvant BKM120 in High-risk Prostate Cancer | Terminated | USA | 0 |
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 |
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 |
NCT01571024 | Phase I | Fluorouracil + Leucovorin + Oxaliplatin + Pembrolizumab Buparlisib | BKM120 + mFOLFOX6 in Advanced Solid Tumors With Expansion Cohort Pancreatic Cancer | Completed | USA | 0 |
NCT01833169 | Phase II | Buparlisib | BKM120 for Patients With PI3K-activated Tumors | Completed | USA | 0 |
NCT01719250 | Phase I | Buparlisib | Buparlisib in Treating Patients With Relapsed or Refractory Non-Hodgkin Lymphoma | Completed | USA | 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 | ITA | FRA | ESP | DEU | BEL | 2 |