crofelemer   Click here for help

GtoPdb Ligand ID: 7453

Synonyms: Fulyzaq® | SP-303
Approved drug
crofelemer is an approved drug (FDA (2012))
Compound class: Natural product or derivative
Comment: Crofelemer is an oligomeric proanthocyanidin extracted from Croton lechleri, a South American flowering tree of the Euphorbiaceae (or spurges). We do not show a chemical structure for this complex molecule, but [2] shows a putative chemical structure.
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View more information in the IUPHAR Pharmacology Education Project: crofelemer

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Summary of Clinical Use Click here for help
Crofelemer is approved as an anti-diarrheal medication for use in HIV/AIDS patients, and is not to be used for treating diarrhea caused by viral or bacterial infection.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Crofelemer inhibits intestinal chloride ion transport by inhibiting two unrelated chloride channels expressed in luminal membrane enterocytes, namely the cystic fibrosis transmembrane conductance regulator (CFTR) and CaCC (ANO1, a calcium-activated chloride channel) [2]. Inhibition of intestinal chloride excretion is accompanied by decreased passive excretion of sodium ions and water. This reduces the water entering the intestinal lumen, improves stool consistency and reduces diarrheal symptoms.
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For extended ADME data see the following:

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