title: Buparlisib in breast cancer.
abstract: Buparlisib (formerly BKM 120), an oral 2,6-dimorpholino pyrimidine derivative is a potent pan-PI3K inhibitor causing inhibition of PI3K downstream signaling including downregulation of p-Akt and p-S6R and apoptosis of cancer cells. Buparlisib is rapidly absorbed, has more than 90% bioavailability, good blood-brain barrier penetration and half-life of 40 h. Phase I trials have shown good disease control rate with tolerable toxicity profile at the recommended doses of 100 mg. The most common adverse events noted with buparlisib are rash, hyperglycemia, derangement of liver functions and psychiatric events. Several clinical trials with buparlisib alone or in combination with chemotherapy and targeted therapies are underway. Buparlisib has not yet been approved for regular use. Further randomized trials are required before buparlisib is approved for treatment of breast cancer.
authors.affiliation: Department of Medical Oncology, Mazumdar Shaw Cancer Centre, Narayana Health, Bangalore, India.
authors.forename: Bhawna
authors.initials: B
authors.lastname: Sirohi
authors.forename: Sameer
authors.initials: S
authors.lastname: Rastogi
authors.forename: Shaheenah
authors.initials: S
authors.lastname: Dawood
mesh_terms: D000631:Aminopyridines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy*; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D004353:Drug Evaluation, Preclinical; D005260:Female; D006801:Humans; D009025:Morpholines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D058570:TOR Serine-Threonine Kinases / Q000378:metabolism; D016896:Treatment Outcome
chemical_list: D000631:Aminopyridines; D000970:Antineoplastic Agents; D009025:Morpholines; D019869:Phosphatidylinositol 3-Kinases; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors; D051057:Proto-Oncogene Proteins c-akt; D058570:TOR Serine-Threonine Kinases; C571178:NVP-BKM120
keywords: PI3K; breast cancer; buparlisib; mTOR