The first anti-diarrheal drug for HIV/AIDS patients, Fulyzaq (crofelemer 125 mg delayed-release tablets), has been approved by the FDA (Food and Drug Administration). The Agency informed that it is the second botanical medication it has approved.

Fulyzaq (crofelemer) is taken to alleviate the symptoms of diarrhea in patients taking antiretroviral therapy for HIV/AIDS. Antiretroviral therapy refers to a combination of drugs for the treatment of HIV infection.

HIV/AIDS patients commonly suffer from diarrhea. In fact, diarrhea is a main reason for compliance problems – patients discontinuing their medication regimes (not following doctor’s instructions), or switching their antiretroviral therapies.

Fulyzaq is meant for patients whose diarrhea is caused by their medication regime, and not a virus, parasite or bacterium.

Fulyzaq is taken twice daily for the management of watery diarrhea caused by electrolyte and water secretion in the gut.

Fulyzaq, which is derived from the red sap of the Croton lechleri plant, native to northwestern South America, is the 2nd botanical prescription medication the FDA has ever approved. The Croton lechleri plant has been used by Amazon Indians for centuries to treat diarrhea, wounds, stomach upsets, and other conditions.

Botanical medications typically consist of a complex mixture derived from at least one plant, with different degrees of purification. Veregen (sinecatechins), for the treatment of external genital perianal warts, was approved in 2006 and was the first botanical prescription drug to enter the US market.

Julie Beitz, M.D., director of the Office of Drug Evaluation III in FDA’s Center for Drug Evaluation and Research, said:

“Currently, there are no FDA-approved therapies for HIV-associated diarrhea. Fulyzaq may be helpful to HIV/AIDS patients with this troublesome condition.”

The FDA establishes a botanical medication’s safety and efficacy through human trials (clinical trials). Also, botanical drug product makers have to make sure there is rigorous control of raw materials, good agricultural and collection practices, as well as optimal analytical testing of the complex mixture.

The FDA looked at data from a clinical trial involving 374 HIV-positive patients on stable antiretroviral therapy. They all had a history of persistent diarrhea – one which had lasted for at least one month. They had a watery bowel movement (average) at least 2.5 times per day. The study researchers excluded those whose diarrheas were caused by a gastrointestinal disease or infection. The double-blind, randomly controlled trial compared patients of Fulyzaq to those on a placebo. Both groups were given their tablets twice a day.

The researchers measured the patients’ clinical response to treatment – specifically, they counted how many had two or fewer watery bowel movements each week.

The results showed that:

  • 17.6% of those on Fylyzaq had 2 or fewer watery bowel movements each week
  • 8% of the placebo patients experienced a clinical response

In a number of patients, the researchers observed an ant-diarrheal clinical response that persisted for 20 weeks.

The FDA emphasizes that doctors should test patients carefully to make sure that their diarrhea is not caused by a gastrointestinal disease or an infection.

The most common side effects reported during the trial among the Fulyzaq patients included, cough, flatulence, higher levels of bilirubin (an enzyme), bronchitis and upper respiratory tract infection.

Salix Pharmaceuticals distributes Fulyzaq in the USA, under license from Napo Pharmaceuticals Inc.

Carolyn Logan, President and CEO of Salix, said:

“The FDA approval of Fulyzaq™ is a significant step forward in addressing the unmet medical need of people with HIV/AIDS on ART who experience non-infectious diarrhea, which often can lead to reduced treatment compliance. Since the introduction of antiretroviral therapy, people with HIV are living longer and thus medication compliance and tolerability as well as quality of life issues are increasingly important components of their overall health outlook. Diarrhea negatively affects quality of life and is a common reason for discontinuing or switching ART regimen. Salix’s expertise in gastrointestinal medicine should position the Company to deliver this much-needed treatment to HIV patients.”

Diarrhea is a common problem for HIV and/or AIDS patients. It typically has a negative impact on the individual’s quality of life and often leads to therapy discontinuation or the premature switching of ART (antiretroviral therapy).

According to Salix Pharmaceuticals, about 1.2 million Americans aged at least 13 years are HIV positive. Over half of all HIV-positive young Americans are not aware of their HIV status. The Centers for Disease Control and Prevention estimates that between 150,000 and 180,000 patients on ART suffer from diarrhea (not caused by infection or a gastrointestinal disease).

Not only can HIV/AIDS-associated diarrhea impact negatively on patients’ quality of life, it can also result in higher direct and indirect healthcare costs. Patients frequently lose too much weight, develop depression, and become more socially isolated.

Written Christian Nordqvist