Initiation of the First-In-Human Clinical Trial of Novel FGFR Inhibitor HMPL-453 in Australia

Shanghai: Tuesday, February 14, 2017: Hutchison MediPharma Limited (“HMP”) today announces that it has initiated the first-in-human (“FIH”) Phase I clinical trial of HMPL-453 in Australia.  HMPL-453 is a novel, highly selective and potent small molecule inhibitor targeting fibroblast growth factor receptor (“FGFR”).  The first drug dose was administered on February 14, 2017.

FGFRs are a sub-family of receptor tyrosine kinases.  Activation of FGFR signaling pathways is central to several biological processes, including angiogenesis, tissue growth and repair.  Given its complexity and critical role in a number of important physiological processes, aberrant FGFR signaling has been found to be a driving force in tumor growth, promotion of angiogenesis, as well as, conferring resistance to anti-tumor therapies.  To date, there are no approved therapies specifically targeting the FGFR signaling pathway.

The FIH dose-escalation trial aims to evaluate the safety, tolerability, pharmacokinetics and preliminary anti-tumor activity of HMPL-453 in patients with advanced or metastatic solid malignancies, who have failed or are unable to tolerate standard therapies or for whom no standard therapies exist.  This open-label study consists of two preliminary phases, a dose-escalation (stage 1) and a dose-expansion stage (stage 2).

In pre-clinical studies, HMPL-453 demonstrated superior potency and better kinase selectivity as compared to other drugs in the same class, as well as a favorable safety profile.  Additional details about this study may be found at clinicaltrials.gov, using identifier NCT02966171.