Chemistry and Life

Medicinal chemistry. Pharmacology. Toxicology. Environmental sciences.

Tenapanor, the “salt-buster”

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Tenapanor (AZD1722, RDX5791) is a drug currently under development by Ardelyx and Astra-Zeneca.  It is designed to prevent the absorption of sodium from the salt in food.

It is an inhibitor of a protein called non-absorbed solute carrier family 9 sodium hydrogen exchanger member 3.  (That’s quite a mouthful, so it is referred to as an NHE3 inhibitor).  Your body needs a certain about of sodium to function properly, so it has a mechanism for extracting it from food in your digestive system.  Basically, tenapanor blocks the action of this mechanism, preventing it from transporting sodium across the gut lining into the blood.

Chemical structure of tenapanor

Chemical structure of tenapanor

Tenapanor is putatively aimed at patients with kidney disease and other health problems that make them very susceptible to adverse effects of high salt intake.  But no doubt, there are also visions of a lifestyle drug that can be taken by anyone.  Just like the way that weightloss drugs which are approved for use in severely obese patients are sought after by people looking for a quick way to loose a few pounds.  The temptation to find a drug to solve the problem rather than to change one’s bad habits is just too great for some.

Tenapanor is already being referred to in the media as a “salt-buster drug” (here, for example) giving it the same type of appeal as the latest “fat buster” being advertised.  The idea is that maybe someday you can eat all the potato chips you like without worrying about the salt affecting your high blood pressure.

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3 thoughts on “Tenapanor, the “salt-buster”

  1. high sodium intake with this inhibitor is bound to result in diarrhea – a simple osmolarity issue. Also, from medicinal chemistry standpoint, the molecule is ugly as hell – perhaps having a non-absorbable inhibitor in this case is the way to go.

    • One of the original groups that they were trying to market the drug to was ibs-c patients to prevent constipation.

  2. Yes, I think it’s likely that this compound won’t get out of the gut. I wonder how that might affect the length of its effectiveness. Would it need to be taken with each meal, for example?

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