Crofelemer is a chemical compound primarily used as a treatment for diarrhea, particularly in patients with HIV/AIDS who are receiving antiretroviral therapy. It is derived from the sap of the Croton lechleri tree, a plant native to the Amazon rainforest. Crofelemer functions as an antidiarrheal agent by inhibiting chloride channels in the intestinal epithelium, thereby reducing fluid secretion into the intestinal lumen and normalizing bowel movements. Its mechanism of action involves the selective inhibition of the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CaCCs), which play a role in electrolyte and fluid transport. Crofelemer is generally well-tolerated, with a favorable safety profile, and is administered orally. Its unique botanical origin and specific action on intestinal chloride channels distinguish it from other antidiarrheal medications. As a result, it represents a novel therapeutic approach for managing diarrhea in specific patient populations.

Crofelemer was approved by the US FDA in December 2012 for the
treatment of diarrhea in HIV/AIDS patients on antiretroviral therapy. Crofelemer is indicated for a subset of the population (30–40% of HIV/AIDS cases) whose diarrhea is determined
to be noninfective in origin. Crofelemer is an oligomeric proanthocyanidin
natural product that is isolated fromthe red latex of Croton lechleri and has been historically used by traditional practitioners of medicine in South America to treat diarrhea. Previously known as SP-303, crofelemer has been shown to
inhibit chloride secretion across epithelial cell monolayers, which causes concomitantmovement of water and sodium.

Crofelemer

148465-45-6: Crofelemer is a chemical compound primarily used as a treatment for diarrhea, particularly in patients with HIV/AIDS who are receiving antiretroviral therapy. It is derived from the sap of the Croton lechleri tree, a plant native to the Amazon rainforest. Crofelemer functions as an antidiarrheal agent by inhibiting chloride channels in the intestinal epithelium, thereby reducing fluid secretion into the intestinal lumen and normalizing bowel movements. Its mechanism of action involves the selective inhibition of the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CaCCs), which play a role in electrolyte and fluid transport. Crofelemer is generally well-tolerated, with a favorable safety profile, and is administered orally. Its unique botanical origin and specific action on intestinal chloride channels distinguish it from other antidiarrheal medications. As a result, it represents a novel therapeutic approach for managing diarrhea in specific patient populations.

<p>Crofelemer (Provir) is an orally active antidiarrheal agent. It targets the cystic fibrosis transmembrane conductance regulator (CFTR) and calcium-activated chloride channels (CACC), which are responsible for chloride and fluid secretion in the gastrointestinal tract. Crofelemer is applicable for research in diarrhea-related conditions.</p>

CAS 148465-45-6

Crofelemer

Crofelemer

Ref: TM-T205474