      Document 0039
 DOCN  DRG0039
 UNIQUE IDENTIFIER        DRG-0208
 NAME OF SUBSTANCE        524W91 [FDA 233A]
 REGISTRY NUMBER          143491-54-7
 STANDARD CHEMICAL NAME   5-Fluoro-2'-deoxy-3'-thiacytidine [FDA 233A]
 SYNONYMS                 ddFTC [AIDS Therapies 1995]
 SYNONYMS                 cis-2',3'-Dideoxy-5-fluoro-3'-thiactidine [J
                          Pharm Sci 1994 Jan;83(1)]
 SYNONYMS                 FTC [Antimicrob Agents Chemother 1992
                          Dec;36(12)]
 PROTOCOL ID NUMBERS      FDA 233A
 SECONDARY SOURCE ID      DRG
 DISEASES STUDIED/TREATED Primary HIV infection [FDA 233A]
 DISEASES STUDIED/TREATED Drug development discontinued per company
                          [Glaxo Wellcome 4/96]
 CLASSIFICATION CODE      Antiretroviral [FDA 233A]
 CONTRAINDICATIONS        Contraindicated in pregnant or nursing women
                          [FDA 233A]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Nucleoside analog
                          [Antimicrob Agents Chemother 1994 Dec;38(12)
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORM: C8H10FN3O3S [CHEMLINE]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Capsules. [FDA 233A]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [FDA 233A]
 MANUFACTURERS            Glaxo Wellcome
 REFERENCES               Frick LW, Lambe CU, St John L, Taylor LC,
                          Nelson DJ. Pharmacokinetics, oral
                          bioavailability, and metabolism in mice and
                          cynomolgus monkeys of
                          ((2'R,5'S-)-cis-5-fluoro-1-[2-(hydroxymethyl)-
                          -1,3- oxathiolan-5-yl] cytosine, an agent
                          active against human immunodeficiency virus
                          and human hepatitis B virus. Antimicrob
                          Agents Chemother. 1994 Dec;38(12):2722-9.
 REFERENCES               Lacey SF, Larder BA. Novel mutation (V75T) in
                          human immunodeficiency virus type 1 reverse
                          transcriptase confers resistance to
                          2',3'-didehydro-2',3'-dideoxythymidine in
                          cell culture. Antimicrob Agents Chemother.
                          1994 Jun;38(6):1428-32.
 REFERENCES               Mathez D, Schinazi RF, Liotta DC, Leibowitch
                          J. Infectious amplification of wild-type
                          human immunodeficiency virus from patients'
                          lymphocytes and modulation by reverse
                          transcriptase inhibitors in vitro. Antimicrob
                          Agents Chemother. 1993 Oct;37(10):2206-11.
 REFERENCES               Wilson JE, Martin JL, Borroto-Esoda K,
                          Hopkins S, Painter G, Liotta DC, Furman PA.
                          The 5'-triphosphates of the (-) and (+)
                          enantiomers of
                          cis-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiola-
                          ne-5-yl] cytosine equally inhibit human
                          immunodeficiency virus type 1 reverse
                          transcriptase. Antimicrob Agents Chemother.
                          1993 Aug;37(8):1720-2.
 REFERENCES               Schinazi RF, Lloyd RM Jr, Nguyen MH, Cannon
                          DL, McMillan A, Ilksoy N, Chu CK, Liotta DC,
                          Bazmi HZ, Mellors JW. Characterization of
                          human immunodeficiency viruses resistant to
                          oxathiolane-cytosine nucleosides. Antimicrob
                          Agents Chemother. 1993 Apr;37(4):875-81.
 ENTRY MONTH              9405
 LAST REVISION DATE       960612
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
