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Phase I Studies of Hypericin, the Active Compound in St. John's Wort, as an Antiretroviral Agent in HIV-Infected Adults: AIDS Clinical Trials Group Protocols 150 and 258

Roy M. Gulick, MD, MPH; Vincent McAuliffe, MD; Jeanne Holden-Wiltse, MPH; Clyde Crumpacker, MD; Leonard Liebes, PhD; Daniel S. Stein, MD; Patricia Meehan, PhD; Sheila Hussey, RN; Janet Forcht, RN; Fred T. Valentine, MD, for the AIDS Clinical Trials Group 150 and 258 Protocol Teams
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From New York University Medical Center, New York, New York; Harvard University School of Public Health and the AIDS Clinical Trial Unit, Beth Israel Hospital, Boston, Massachusetts; and National Institutes of Health, Rockville, Maryland.

Ann Intern Med. 1999;130(6):510-514. doi:10.7326/0003-4819-130-6-199903160-00015
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Background: Hypericin, the active compound in St. John's Wort, has antiretroviral activity in vitro. Many HIV-infected persons use St. John's wort.

Objective: To evaluate the safety and antiretroviral activity of hypericin in HIV-infected patients.

Design: Phase I study.

Setting: Four clinical research units.

Patients: 30 HIV-infected patients with CD4 counts less than 350 cells/mm3.

Intervention: Intravenous hypericin, 0.25 or 0.5 mg/kg of body weight twice weekly or 0.25 mg/kg three times weekly, or oral hypericin, 0.5 mg/kg daily.

Measurements: Safety was assessed at weekly visits. Antiretroviral activity was assessed by changes in HIV p24 antigen level, HIV titer, HIV RNA copies, and CD4 cell counts.

Results: Of the 30 patients who were enrolled, 16 discontinued treatment early because of toxic effects. Severe cutaneous phototoxicity was observed in 11 of 23 (48% [95% CI, 27% to 69%]) evaluable patients, and dose escalation could not be completed. Virologic markers and CD4 cell count did not significantly change.

Conclusions: Hypericin caused significant phototoxicity and had no antiretroviral activity in the limited number of patients studied.


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Disposition of the study patients.

*To establish the pharmacokinetics of oral hypericin, a single oral dose of hypericin (1.25 mg/kg) was tested in four patients in the cohort that received 0.25 mg/kg of intravenous hypericin twice weekly.

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