BETHESDA, MD 02 January 2013—FDA on December 31 announced the approval of crofelemer delayed-release oral tablets for the treatment of symptoms of noninfectious diarrhea in adults receiving antiretroviral therapy for HIV infection.
The drug will be marketed as Fulyzaq by Salix Pharmaceuticals. The company expects the product to be available early this year.
for crofelemer states that the drug is derived from latex produced by the Croton lechleri plant.
The plant, a South American native, is also known as dragon's blood.
According to FDA, crofelemer is the first oral botanical prescription drug approved by the agency and the first antidiarrheal remedy approved specifically for use in HIV-infected patients.
The labeling for crofelemer states that the drug blocks chloride ion secretion by intestinal epithelial cells, thereby normalizing the flow of chloride ions and water in the gastrointestinal tract.
Crofelemer was approved on the basis of data from placebo-controlled clinical trials indicating that the drug reduced the frequency of watery bowel movements in HIV-infected patients treated with antiretroviral medications.
The recommended dosage of crofelemer is one 125-mg tablet taken twice daily with or without food. The enteric-coated tablets should be swallowed whole and not crushed or chewed.
Patients should be assessed to rule out an infectious or gastrointestinal-disease-related cause for their diarrhea before initiating crofelemer therapy.
Crofelemer is minimally absorbed in the gastrointestinal tract and is unlikely to cause systemic inhibition of the cytochrome P-450 (CYP) isoenzymes 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, or 3A4. In vitro data suggest that the drug may inhibit CYP 3A and drug transporters MRP2 and OATP1A2 at concentrations expected in the gastrointestinal tract.
According to the labeling, a study conducted in healthy volunteers found that the drug did not alter recipients' exposure to zidovudine or nelfinavir. A 20% reduction in exposure to lamivudine was reported but was not deemed to be clinically important.
The most frequently reported adverse events associated with crofelemer during clinical trials were upper-respiratory-tract infection, bronchitis, cough, flatulence, and increased bilirubin levels.
Crofelemer 125-mg tablets will be available in bottles of 60 each and should be stored at controlled room temperature.