A Phase I Dose Escalation Study of Synthetic Hypericin in HIV-Infected Patients With Less Than 300 CD4 Lymphocytes

Hypericin is unlike other drugs presently being used to treat AIDS patients. Hypericin shows anti-HIV activity in test tube experiments.

Each group of eight patients receives a given dose of hypericin by intravenous infusion. Doses are given three times per week for 8 weeks. When all eight patients at a dose level have been entered and four of the eight patients have completed 3 weeks of therapy without evidence of dose-limiting toxicity, additional patients may begin to receive drug at the next dose level. Concurrently, six patients wll participate in an oral-dosing bioavailability study. NOTE: The initial study was stopped secondary to an MTD being reached.

Inclusion criteria

Concurrent Medication:

Allowed:

• Prophylaxis for Pneumocystis carinii pneumonia (required for patients with CD4+ < 200).
• Symptomatic treatment with analgesics, antihistamines, antiemetics, antidiarrheal agents, or other supportive therapy.
• Short courses (< 10 days) with ketoconazole or fluconazole for oral candidiasis or acyclovir for herpes lesions.
• Topical medications such as clotrimazole troches or nystatin suspensions.

Concurrent Treatment:

Allowed:

• Blood transfusions.

Patients must have HIV infection with CD+4 lymphocyte count of < 300 cells/mm3.

Exclusion criteria

Co-existing Condition:

Patients with the following conditions or symptoms are excluded.

• Kaposi's sarcoma requiring systemic therapy.

Concurrent Medication:

Excluded:

• Continued use of opiates or drugs known to induce photosensitivity.

Patients with the following are excluded:

• Active or chronic opportunistic infection at time of study entry that required curative or suppressive therapy.
• Significant liver disease, orthostatic hypotension, cardiac disease, seizure disorder, lymphoma, hypotension.

Prior Medication:

Excluded:

• Zidovudine (AZT), dideoxyinosine (ddI), dideoxycytidine (ddC), interferon, other antiretroviral agents or immunomodulating drugs within 1 month prior to study entry. Ribavirin within 3 months of study entry.
• Ganciclovir (DHPG), antimycobacterial drugs, MAO inhibitors, hypertension-inducing, nephrotoxic, or hepatotoxic drugs within 14 days of entry.
• Cytotoxic chemotherapy within 1 month prior to study entry.

Active substance abuse.