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crofelemer
- Development stage
- Approved
- Lead developer
- Napo Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Crofelemer is a botanical antidiarrheal agent derived from the latex of the South American tree Croton lechleri. It is indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS who are receiving antiretroviral therapy. Crofelemer acts locally in the gastrointestinal tract and is minimally absorbed systemically. Its mechanism of action involves inhibition of two chloride channels on intestinal epithelial cells—the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium activated chloride channel (CaCC). By inhibiting these channels, crofelemer reduces chloride and water secretion into the gut, improving stool consistency without affecting motility or causing constipation[3][5][6]. The drug is available as an oral delayed-release tablet.
- Brand names
- MytesiFulyzaqCanalevia
- Other names
- crofelemer
02
Targets
CFTR (Cystic fibrosis transmembrane conductance regulator)CaCC (Calcium-activated chloride channel protein regulator 1)
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