Crofelemer
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| Trade names | Mytesi (Fulyzaq) |
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Oral (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | Little or no absorption from the gut |
| Identifiers | |
| Synonyms | SP-303 |
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| Formula | (C15O6,7H12)n |
| Molar mass | 860–9100 g/mol |
Crofelemer (USAN, trade name Mytesi) is a botanical drug for the treatment of diarrhoea associated with anti-HIV drugs such as nucleoside analog reverse transcriptase inhibitors and protease inhibitors. Other possible uses include diarrhoea in children, acute infectious diarrhoea, and diarrhoea in patients with irritable bowel syndrome. It is a purified oligomeric proanthocyanidin from "dragon's blood", the sap of the South American tree Croton lechleri.
Crofelemer treats the symptoms of disease, but it is not used to treat infectious diarrhoea (diarrhoea caused by infection of the digestive system by a bacterium, virus or parasite). It was initially developed by Napo Pharmaceuticals, which licensed it to Glenmark Pharmaceuticals in 140 emerging markets and to Salix Pharmaceuticals in the US, EU and some other markets. A Phase III clinical trial for diarrhoea in HIV patients was completed in 2012, and the drug was approved by the US Food and Drug Administration (FDA) on 31 December 2012.
The drug is taken by mouth and works by voltage-independently blocking two structurally unrelated chloride channels in the gut, namely the cystic fibrosis transmembrane conductance regulator (CFTR) with an in vitro maximum inhibition of about 60%, and the calcium-activated chloride channel anoctamin 1, with a maximum inhibition of over 90%. This is a hitherto undescribed mechanism of action. As a result of the channel inhibition, fewer chloride ions are excreted into the gut, which also decreases the excretion of sodium ions and water, improving stool consistency and reducing duration of the diarrhoea. The mechanism seems to be selective as other channels involved in intestinal fluid secretion, namely sodium and potassium channels, are not affected by crofelemer, nor is cAMP or calcium signalling.
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