Antitumor Activity of RXDX-105 in Multiple Cancer Types with RET Rearrangements or Mutations.

ABSTRACT: Purpose: While multikinase inhibitors with RET activity are active in RET-rearranged thyroid and lung cancers, objective response rates are relatively low and toxicity can be substantial. The development of novel RET inhibitors with improved potency and/or reduced toxicity is thus an unmet need. RXDX-105 is a small molecule kinase inhibitor that potently inhibits RET. The purpose of the preclinical and clinical studies was to evaluate the potential of RXDX-105 as an effective therapy for cancers driven by RET alterations.Experimental design: The RET-inhibitory activity of RXDX-105 was assessed by biochemical and cellular assays, followed by in vivo tumor growth inhibition studies in cell line- and patient-derived xenograft models. Antitumor activity in pa

SUBMITTER: Li GG 

PROVIDER: S-EPMC5477238 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature