molecules of the month

Context. ACT-660602 (Idorsia Pharmaceuticals) is an oral chemokine receptor CXCR3 antagonist being developed for autoimmune diseases. Chemokines and their receptors make up the signaling system that is responsible for immune cell migration. This is important for the innate immune system’s ability for fighting infection, but dysregulation of these pathways can lead to autoimmune disorders, especially when T cells migrate into inflamed tissue and cause tissue and organ damage. Since the identification of CXCR3 in 1996 and findings that it’s overexpression led to cell migration, CXCR3 has been implicated in a number of diseases, driving the search for potent antagonists. However, only three drugs have been approved for chemokine receptors so far: CXCR4 antagonist plerixafor, CCR5 antagonist maraviroc, and anti-CCR4 mAb…