EVALUATION OF THE ANTIHERPETIC ACTIVITY OF 2'-FLUORO-5-IODO-ARA-C IN RABBIT EYES AND CELL-CULTURES

  • 1 January 1981
    • journal article
    • research article
    • Vol. 21  (6) , 826-832
Abstract
2''-Fluoro-5-iodo-cytosine arabinoside (FIAC), a new 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 0.023-0.51 .mu.M for HSV-1 and 0.019-1.5 .mu.M 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 and 0.01 FIAC beginning 3 days after inoculation with HSV-1 (McKrae strain). Topical chemotherapy was administered 5 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. HSV was not prevented from spreading into the central nervous system when topical FIAC therapy was initiated on day 3 after inoculation.