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. It is marketed under the brand name Fulyzaq and indicated for the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy. Fulyzaq treats the symptoms of disease, but it is not used to treat infectious diarrhea (diarrhea caused by infection of the digestive system by a bacteria, 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.
Originator
Approval Year
PubMed
Sample Use Guides
The recommended dose of FULYZAQ (crofelemer) is one 125 mg delayed-release tablettaken orally two 7 times a day, with or without food.
Route of Administration:
Oral
In Cyclic Nucleotide Assays T84 cells were grown in 24-well plates, treated for 45 min with crofelemer 50 uM crofelemer and then for 10 min with 0 or 20 μM forskolin, lysed by sonication, and centrifuged to remove cell debris, and the supernatant was assayed for cAMP according to manufacturer's instructions (Parameter cAMP immunoassay kit; R&D Systems, Minneapolis, MN).
ACTIVE MOIETY
