Crofelemer is an antidiarrheal agent used for the symptomatic relief of drug-induced non-infectious diarrhea in adult patients with HIV/AIDS receiving antiretroviral therapy. Crofelemer, previously known as the investigational drug SP-303, is a novel proanthocyanidin purified from the bark latex of the Amazonian Croton tree Croton lechleri.
- Mechanism
- Curator reviewed
Crofelemer is an inhibitor of the cystic fibrosis transmembrane regulator chloride channel (CFTR), as evidenced by its activity on cell cultures, single cell patch clamps, single CFTR channels, and elaboration of mouse intestinal fluid secretion. Crofelemer also inhibits calcium activated chloride channels (CaCC), which in combination with CFTR, are expressed on the luminal side of intestinal cells. Crofelemer inhibition of both of these channels prevents water loss from diarrhea by inhibiting chloride secretion.
- Primary indication
- For the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy.Curator reviewed · 1 structured indication
- First approval
- United States, 2012
- Code names
- NP-303 · SP-303 · TRN-002
- Brand names
Resolves to
What you can answer from here — as of June 19, 2026
Which drugs share a target with Crofelemer, and which of those have an active Phase 3 trial?
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