molecules of the month


oral reversible CXCR3 antagonist

Ph. I in healthy subjects

opt. of known CXCR3 antagonists

J. Med. Chem., March 8, 2023

Idorsia Pharmaceuticals Ltd, Allschwil, CH

ACT-777991, oral reversible CXCR3 antagonist, Ph. I in healthy subjects, opt. of known CXCR3 antagonists, J. Med. Chem., March 8, 2023, IDORSIA PHARMACEUTICALS LTD, CH
11 mins read

ACT-777991: next-generation CXCR3 antagonist in Phase I trials for Type 1 diabetes. ACT-777991, an oral and insurmountable CXCR3 antagonist discovered by Idorsia (formerly Actelion), is under investigation for the treatment of Type 1 Diabetes (T1D). Despite the complex history of CXCR3 antagonists, ACT-777991 has shown promise with demonstrated in vivo efficacy in T1D mouse models. This compound is the first of its kind to progress to clinical trials since Amgen's AMG 487, which was discontinued due to CYP time-dependent inhibition (TDI) by sequential metabolites. As of May 2022, Phase I results for ACT-777991 are pending, and the asset is listed in Idorsia’s pipeline. The advancement of this candidate in T1D, outside of traditional inflammation indications, reflects the industry’s continued interest…

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