molecules of the month


oral gut-restricted Na+/H+ exchanger inhibitor

FDA-approved IBS treatment

from literature starting point and opt

ACS Med. Chem. Lett.

Ardelyx Inc., Fremont, CA/Waltham, MA

tenapanor chemical structure, oral gut-restricted Na+/H+ exchanger inhibitor - Ardelyx Inc., Fremont, CA/Waltham, MA
5 mins read

Context. Tenapanor (Ardelyx) is an oral, first-in-class Na+/H+ exchanger isoform 3 (NHE3) inhibitor approved by the FDA for irritable bowel syndrome with constipation (IBS-C) in adults. NHE3 is expressed predominantly in the gut and kidney and its role as a key mediator of sodium and water homeostasis makes the protein an ideal target for multiple disease states such as hypertension, heart/kidney failure, diabetes mellitus, irritable bowel syndrome (IBS), constipation, and even hyperphosphatemia. However, this also presents a drug discovery challenge since systemic exposure could mean an undesired inhibition of renal NHE3. Therefore, critical to the development of tenapanor for IBS-C by Ardelyx scientists was the identification of an agent with potent Na+/H+ antiport activity in the gut that exhibited poor…

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