Gay Men's Health Crisis Treatment Issues, Vol. 5, No. 9, December 1991
Anna Blume

DATA LEADING TO HUMAN TESTING

In test tube studies, hypericin hardens the outer surface of HIV, inhibiting the virus from infecting cells. Hypericin also inhibits the replication of cells already infected with HIV and is able to enter both lymphocytes and macrophages.[1] These functions, if indeed they occur in the human body, could slow the progression of HIV disease. Based on the potential of this drug, testing in humans has long been recommended and will soon begin.

One recent dose-ranging, observational, phase I/II study from Australia found that hypericin at a dose of 2.0 mg/day appears to be safe in the majority of subjects observed so far. Participants in this study were gay and bisexual men visiting an AIDS clinic in Australia. They were followed, while taking hypericin, for 12 weeks. No specific T4 cell count criteria were required for entry. Side effects included diarrhea, indigestion, infrequent rash, and fatigue or depression. Monitoring of blood and liver tests is recommended.[2]

No marked anti-HIV activity was discovered in this early trial data. It should be noted, though, that this was a relatively relaxed, uncontrolled trial, using the street-version, rather than the synthetic, of hypericin.

BACKGROUND ON DRUG DEVELOPMENT

Hypericin was given "ACTG status" over a year ago. This means that a specific protocol and a series of sites were chosen to carry out government-funded clinical trials of the drug in order to study the compound's effect in people living with HIV/AIDS. It took the small pharmaceutical company VIMRX over 17 months to formulate a drug which met FDA standards of quality for testing in human beings.

In May, 1991, members of ACT UP/NY waged a concentrated campaign aimed at VIMRX, NIAID and the FDA to accelerate development. On August 20, 1991, the compound was approved for testing in human beings, and a few days later the IRB (Internal Review Board) at New York University (NYU) approved the final protocol. These were the last major obstacles to setting up a trial. The hypericin trial has now begun and is recruiting 32 participants with T4 counts under 300. To enroll, or obtain more information, call Kate Krikorian, R. N. or Janet Vaccariello, R. N. at (212) 263-6565.

The trial will try to determine possible toxicities and appropriate dose ranges of synthetic hypericin in people. Shortly after the commencement of this trial, similar trials are scheduled to begin in Boston and Minneapolis. The principal investigator for the protocol is Dr. Fred Valentine of NYU.

The first segment of the trial will last for eight weeks. To enter the trial, patients must stop taking AZT, ddI or ddC for four weeks and must stop taking therapies against CMV and other OI's. Hypericin will be administered intravenously (IV) two times a week, and a hospital stay is required for the first infusion.

If safety and signs of efficacy are evident, the trial will continue for a total of 24 weeks. If safety and efficacy markers continue to be reached, NIAID and the sponsoring pharmaceutical company VIMRX, will immediately design phase II trials to test rigorously the possible use of hypericin as an anti-HIV drug. By February of 1992, it is hoped that sufficient evidence of safety and efficacy will allow hypericin to proceed into phase II trials.

CURRENT AVAILABILITY

In the phase I trial, researchers will use a synthetic hypericin that is not available on the market at this time, and that is said to be a more pure form of the drug. Hypericin is available in health food stores in a form called St. John's Wort, either as a pill or tincture (liquid extract), and it is also available in multiple pill forms from the different buyers clubs throughout the country.

To date there have been no evaluations about which available form of the drug is most effective. It is possible that the market formulations of hypericin may have enough active drug to be effective against HIV, but such an assertion has yet to be confirmed. Anecdotal reports suggest that people with HIV/AIDS do benefit from the hypericin on the market in the following ways: increase in energy; decrease in depression; and, for some, an increase in T4 cell counts.

Hypericin has been used as a natural anti-depressant and antiviral for centuries. In the test tube the drug has been shown to be effective against CMV and Sindbis virus[3], and other retroviruses such as equine infectious anemia virus (EIAV).[4] We look forward to evidence determining whether this drug will be effective against HIV.

References

1. VIIth Int'l Conf on AIDS. Abstract #A. 1022, Florence. June 1991.

2. VIIth Int'I Conf on AIDS. Abstract #W. B. 2071, Florence, June 1991.

3. Hudson JB et al. Antiviral properties of hypericin. Antiviral Research 15(2):101-12, 1991.

4. Kraus GA et al. Antiretroviral activity of synthetic hypericin and related analogs. Biochemical & Biophysical Research Communications 172(1):149-53, 1990.

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