GtoPdb Ligand ID: 7453

Synonyms: Fulyzaq® | SP-303
crofelemer is an approved drug (FDA (2012))
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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Bioactivity Comments
Studies in mouse models report that crofelemer has an inhibitory effect on intestinal cAMP-mediated (active) Cl- and fluid secretion [1]. Patch-clamp analysis of cells stably expressing hCFTR or hANO1, and cAMP and calcium signaling measurements in human colorectal cancer cells (T84 cells) confirm the activity of crofelemer at the proposed human Cl- channels.
Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
CaCC Hs Inhibitor Inhibition 5.2 pIC50 - 2
pIC50 5.2 (IC50 6.5x10-6 M) [2]
CFTR Hs Inhibitor Inhibition 5.2 pIC50 - 2
pIC50 5.2 (IC50 7x10-6 M) [2]