The Medical Letter on Drugs and Therapeutics
Crofelemer (Fulyzaq) for Antiretroviral-Induced Diarrhea
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The FDA has approved crofelemer (kroe fel’ e mer; Fulyzaq – Salix), a chloride channel inhibitor derived from the red sap of the South American plant Croton lechleri, for symptomatic relief of noninfectious diarrhea in patients with HIV taking antiretroviral drugs. It is the first drug approved for relief of antiretroviral-induced diarrhea and the first oral botanical drug approved by the FDA.

MECHANISM OF ACTION — Diarrhea is a common adverse effect of antiretroviral therapy. Crofelemer inhibits the secretion of chloride ions into the intestinal lumen by inhibiting both cystic fibrosis transmembrane conductance regulator and calcium-activated chloride channels. As a result, less water is drawn into the intestinal lumen via osmosis. Systemic absorption of crofelemer is minimal.1,2

A CLINICAL STUDY — Approval of crofelemer was based on ... more      

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