LCI136

LCI136 is a novel, multitargeted small molecule inhibitor developed by the Molecular Targeted Therapeutics Laboratory at the Levine Cancer Institute (Atrium Health). It is designed to simultaneously inhibit multiple signaling nodes, including Phosphoinositide 3-kinase (PI3K), Bromodomain-containing protein 4 (BRD4), and Cyclin-dependent kinases (CDK4, CDK6, and CDK9). The compound is intended to induce synthetic lethality in cancers with specific genetic vulnerabilities, such as PTEN/PI3K co-mutated endometrial carcinoma, by preventing compensatory kinome adaptation and overcoming resistance associated with single-agent therapies. Preclinical data presented at ASCO 2023 demonstrated that LCI136 possesses nanomolar potency against endometrial carcinoma cell lines, inducing cytostatic and cytotoxic responses.