GMHC Treatment Issues 1991 Dec 15; 5(9): 2
Hypericin is a natural pigment found in stems and petals of
plants in the genus hypericum. The compound hypericin has been
of interest to scientists for many years, as a natural
antiviral and antidepressant, and was first described as a
plant extract in 1830. In August, 1991 a form of hypericin was
successfully synthesized and FDA-approved for testing in humans
as an AIDS therapy.
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. 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
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.
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
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.
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, and
other retroviruses such as equine infectious anemia virus
(EIAV). We look forward to evidence determining whether this
drug will be effective against HIV.
1. VIIth Int'l Conf on AIDS. Abstract #A. 1022, Florence.
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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