8 minute read
Sep. 21, 2023

An Azetidine-Containing, First-in-Class CCR4 Candidate with a 72 h Human Half-life

FLX475

oral CCR4 antagonist Ph. II for immunooncology, 100 mg QD from optimization of prior CCR4 ligands J. Clin. Oncol., June 1, 2023 RAPT Therapeutics, South San Francisco, CA

Editor:  

RAPT Therapeutics, formerly known as FLX Bio, was spun out of Flexus Biosciences after its billion-dollar acquisition by BMS for Flexus’s immuno-oncology IDO1 program. While the IDO1 molecule unfortunately did not show efficacy in Ph. III trials in combination with BMS’s PD-1 inhibitor nivolumab, RAPT Therapeutics appears to be having better luck with its potentially first-in-class CCR4 inhibitors FLX475 (for immune-oncology) and RPT193 (for atopic dermatitis). Oral FLX475 (100 mg QD, human T1/2 = 72 h) appears to shrink EBV+ tumors both as a monotherapy and in combination with a PD-1 inhibitor in clinical studies...

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