The pharmacokinetic-pharmacodynamic (PKPD) relationships of AZD3229, a novel and selective inhibitor of cKIT, in a range of mouse xenograft models of GIST.

CONCLUSIONS: We demonstrate that AZD3229 warrants clinical investigation as a new treatment for GIST patients based on its ability to inhibit both ATP-binding and A-loop mutations of KIT at clinically relevant exposures.
PMID: 32220888 [PubMed - as supplied by publisher]

Source: Clinical Cancer Research - March 26, 2020 Category: Cancer & Oncology Authors: Pilla Reddy V, Anjum R, Grondine M, Smith A, Bhavsar D, Barry E, Guichard SM, Shao W, Kettle JG, Brown C, Banks E, Jones RDO Tags: Clin Cancer Res Source Type: research