Amcasertib

Description: Amcasertib (formerly known as BBI503) is an orally-administered small molecule compound, that is designed to target CSC (Cancer Stem Cell) pathways in multiple tumour types. It is the first-in-class cancer stemness kinase inhibitor, and is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity. In a phase I study, BI503 as a monotherapy was tolerated at the recommended phase 2 dose of 300 mg once daily. At the recommended phase 2 dose, common adverse events were grade 1 to 2 diarrhea, nausea, abdominal cramping, anorexia and fatigue, and grade 3 adverse events were fatigue (n= 4), and diarrhea, nausea, and weight loss (n=1 each).

References: Boston Biomedical Data at ASCO 2015