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Tenapanor

IBSRELA

What it isNHE3 inhibitor reducing intestinal sodium and phosphate absorption; IBS with constipation and hyperphosphatemia in dialysis.

Why this oneIt reduces phosphate absorption rather than binding it, so it is not a binder and the pill burden is small.

What limits itDiarrhea is dose-limiting and is the mechanism. Contraindicated under age 6.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Hyperphosphatemia in CKD on dialysis (add-on/intolerant to binders)Adults30 mg BID30 mg BID30 mg BID

Renal Undefined

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Essentially non-absorbed; maternal use not expected to result in fetal exposure; available data show no drug-associated risk

Lactation Not detected in human milk; maternal use not expected to expose infant

⚠ BOXED WARNING

Cost, est. cash$300–$2,500/month

Generic entry2034 est.

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk0 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityDiarrhea, dehydration and electrolyte disturbance, especially with excessive or prolonged use.

Mechanism of action: Tenapanor ballicule

Tenapanor ballicule: receptor binding, kinetics and half-life diagram

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