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

Ann Intern Med. 1999 Mar 16;130(6):510-4. doi: 10.7326/0003-4819-130-6-199903160-00015.


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.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Multicenter Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Oral
  • Adult
  • Anthracenes
  • Anti-HIV Agents / adverse effects
  • Anti-HIV Agents / therapeutic use*
  • CD4 Lymphocyte Count
  • Dermatitis, Phototoxic / etiology
  • Female
  • Follow-Up Studies
  • HIV Core Protein p24 / blood
  • HIV Infections / drug therapy*
  • HIV Infections / immunology
  • HIV Infections / virology
  • Humans
  • Injections, Intravenous
  • Male
  • Perylene / adverse effects
  • Perylene / analogs & derivatives*
  • Perylene / therapeutic use
  • RNA, Viral / blood
  • Statistics, Nonparametric
  • Viral Load


  • Anthracenes
  • Anti-HIV Agents
  • HIV Core Protein p24
  • RNA, Viral
  • Perylene
  • hypericin