SAN FRANCISCO, CA—In HIV-seropositive patients on antiretroviral therapy (ART) with non-infectious diarrhea, crofelemer 125mg twice daily was well tolerated with a low incidence of adverse events and no clinical deterioration of immune status, study investigators reported at IDWeek 2013.

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Non-infectious diarrhea is major health concern in some HIV-seropositive patients on ART. A first-in-class drug, crofelemer, is a minimally absorbed, botanically derived gastrointestinal drug that is indicated for symptomatic relief of non-infectious diarrhea in patients with HIV receiving ART.

Trevor Hawkins, MD, from Southwest Care Center, Santa Fe, NM, and colleagues assessed the long-term safety and tolerability of twice-daily crofelemer 125mg in a 48-week, multicenter, open-label trial.

Crofelemer 125mg twice daily for up to 48 weeks was administered in HIV-seropositive adults receiving ART, with CD4+ counts ≥100cells/mm3 and self-reported diarrhea necessitating antidiarrheal medication (ADM) use for ≥4 weeks.

Researchers conducted assessments that included periodic monitoring of adverse events and clinical laboratory tests. Immune status (HIV viral load, CD4+ count) was evaluated at baseline and Month 12, the end of treatment. Concomitant antidiarrheal medications were permitted.

The safety population consisted of (n=250; 206 new patients and 44 patients from a previous trial [ADVENT]) 84.4% male and 53.6% white, with a mean (SD) age of 46.8 (8.3) years. At baseline, 74.4% of patients used concomitant antidiarrheal medications and 100% reported current ART use. The most frequently used ART at baseline included ritonavir, tenofovir/emtricitabine, and raltegravir. Participants were exposed to crofelemer for a median of 335 (range 7–366) days, with 78.8% of patients treated for ≥9 months.

The most commonly reported adverse events were infection (eg, upper respiratory tract [16.8%], intestinal parasitic [12.4%], giardiasis [8.0%]) or gastrointestinal-related (eg, nausea [5.6%], constipation [5.6%]). The majority of adverse events (90.5% of patients) were mild or moderate in severity.  Ten out of 14 patients who reported experiencing constipation also used antidiarrheal medications during the study.

Only 3.6% of patients reported diarrhea as an adverse event and no deaths were reported during this study. Although 20 patients (8.0%) experienced serious adverse events, including infection in 10 patients, none were considered drug-related. Change from baseline in CD4+ count (>500 to ≤500 cells/mm3; 9.4% of patients) and viral load (<400 to ≥400 copies/mL; 14.3%) were minimal, they reported.

“Data from this study showed crofelemer had no apparent adverse effect on HIV status, which is suggestive of adherence to ART regimens and continued ART efficacy,” stated Dr. Hawkins.