molecules of the month


purinergic receptor (ion channel) antagonist

up to 300 mg PO QD, phase IIb, chronic cough

from opt. of prior P2X3 antagonist

Bioorganic and Medicinal Chemistry Letters


Chemical structure of molecule S-600918
1 min read

The Shionogi P2X3 ligand-gated ion channel antagonist, sivopixant (S-600918), is an oral Ph. II candidate for refractory chronic cough, which recently completed a its Ph. IIb study, overcoming the projected high dose requirement of a prior preclinical candidate. The molecule has a very polar core structure with both a dioxotriazine and carboxylic acid, yet is highly bioavailable. From a chemistry perspective, it is an interesting example where adding another aromatic heterocycle at a late stage of optimization led to a significant lowering of human dose projection, whereas typically at a late stage adding large new groups tends to be avoided.

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