Evaluation of the antiherpetic activity of 2'-fluoro-5-iodo-ara-C in rabbit eyes and cell cultures.

ABSTRACT

2-Fluoro-5-iodo-ara-C (FIAC), a new and potent drug, was tested for antiviral activity against several strains of herpes simplex virus (HSV), types 1 and 2. Effective dose-50% (ED-50) determinations for FIAC ranged from 0.023 to 0.51 muM for HSV-2. FIAC-treated cells did not exhibit any toxicity until the drug concentration was increased 2000-fold above the ED-50 level. Ocular herpetic keratitis in New Zealand white rabbits was treated with 1.0%, 0.1%, 0.01% FIAC beginning 3 days after inoculation wit HSV-1 (McKrae strain). Topical chemotherapy was administered five times per day for 7 consecutive days. After 4 days of treatment, corneal epithelial involvement, conjunctivitis, iritis, and clouding were not detectable in eyes receiving 1.0% FIAC. Toxic reactions were not observed in rabbit eyes treated with FIAC drug. HSV was not prevented from spreading into the central nervous system when topical FIAC therapy was initiated on day 3 after inoculation.