In the literature: February 2022

[摘要] PIK3CA is one of the most frequently mutated oncogene incancer. Phosphoinositide 3-kinase (PI3K) is a heterodimercomprising two subunits: a catalytic subunit (p110) and aregulatory subunit (p85). Activating mutations in PIK3CA arefound in w30%-40% of patients with breast cancer (BC) andinduce hyperactivation of the catalytic subunit.1 This mutation has been associated with endocrine therapy resistance in luminal BC, and also with anti-HER2 therapy inHER2þ BC. In May 2019, alpelisib, an a-specific PI3K inhibitor, was approved for the treatment of patients withadvanced PIK3CA-mutant luminal BC.2 However, the efficacyhas been modest, in part due to a limited therapeutic index.

[学科分类] 社会科学、人文和艺术（综合）