Preclinical Development and First-in-Human Study of KA2507, a Selective and Potent Inhibitor of Histone Deacetylase 6, for Patients with Refractory Solid Tumors.
Apostolia M TsimberidouPhilip A BeerCarrie A CartwrightCara L HaymakerHenry H VoSimin KianyAlexander R L CecilJames DowKemal HaqueFranck A SilvaLucy CoeHelen BerrymanElisabeth A BoneGraciela Nogueras GonzalezDavid ViningHilary McElwaine-JohnnIgnacio I WistubaPublished in: Clinical cancer research : an official journal of the American Association for Cancer Research (2021)
KA2507 is a potent and selective inhibitor of HDAC6 showing antitumor efficacy and immune modulatory effects in preclinical models. In a phase I study, KA2507 showed selective target engagement, no significant toxicities, and prolonged disease stabilization in a subset of patients. Further clinical studies of KA2507 are warranted, as a single agent or, preferably, combined with other immuno-oncology drugs.