      Document 0110
 DOCN  DRG0110
 UNIQUE IDENTIFIER        DRG-0137
 NAME OF SUBSTANCE        Letrazuril [USAN 1996]
 REGISTRY NUMBER          103337-74-2
 STANDARD CHEMICAL NAME   (+/-)-[2,6-Dichloro-4-
                          (4,5-dihydro-3,5-dioxo-as-triazin-2(3H)-yl)ph-
                          enyl] (p-fluorophenyl)acetonitrile [USAN
                          1996]
 PROTOCOL ID NUMBERS      NIAID ACTG 198
 SECONDARY SOURCE ID      DRG
 DISEASES STUDIED/TREATED Being investigated for the treatment of
                          cryptosporidiosis [AmFAR Tx Dir 1995;7(4)]
                          [AIDS 1993 Aug;8(8)]
 CLASSIFICATION CODE      Antiprotozoal [AmFAR Tx Dir 1993;6(4)]
 ADVERSE EFFECTS          Adverse effects include transient rash. [AIDS
                          1993 Aug;8(8)]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Fluorine-based congener of
                          diclazuril [AmFAR Tx Dir 1995;7(4)]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C17H9Cl2FN4O2 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 391.19 [USAN 1996]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 10, 25, and 50 mg capsules.
                          [NIAID ACTG 198]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [AmFAR Tx Dir
                          1995;7(4)] [AIDS 1993 Aug;8(8)]
 MANUFACTURERS            Janssen Research Foundation
 REFERENCES               Loeb M, Walach C, Phillips J, Fong I, Salit
                          I, Rachlis A, Walmsley S. Treatment with
                          letrazuril of refractory crytosporidial
                          diarrhea complicating AIDS. J Acquir Immune
                          Defic Syndr Hum Retrovirol. 1995 Sep
                          1;10(1):48-53.
 REFERENCES               Harris M, Deutsch G, MacLean JD, Tsoukas CM.
                          A phase I study of letrazuril in AIDS-related
                          cryptosporidiosis. AIDS. 1994
                          Aug;8(8):1109-13.
 REFERENCES               Hamour AA, Bonnington A, Hawthorne B, Wilkins
                          EG. Successful treatment of AIDS-related
                          cryptosporidial sclerosing cholangitis. AIDS.
                          1993 Nov;7(11):1449-51.
 REFERENCES               Murdoch DA, Bloss DE, Glover SC.  Successful
                          treatment of cryptosporidiosis in an AIDS
                          patient with letrazuril [letter]. AIDS. 1993
                          Sep;7(9):1279-80.
 REFERENCES               Victor GH, Conway B, Hawley-Foss NC, Manion
                          D, Sahai J. Letrazuril therapy for
                          cryptosporidiosis: clinical response and
                          pharmacokinetics [letter]. AIDS. 1993
                          Mar;7(3):438-40.
 REFERENCES               Rubbert A, Schwab J, Kalden JR, Nusslein H.
                          Myositis, fever, rash and thrombopenia after
                          letrazuril treatment of intestinal
                          cryptosporidiosis: a case report. Int Conf
                          AIDS. 1993 Jun 6-11;9(1):373 (abstract no.
                          PO-B10-1430).
 REFERENCES               Hamour AA, Khoo S, Bonnington A, Barnes A,
                          Fraser I, Bailey G, Wilkins EG, Denning DW,
                          Dunbar EM, Mandal BK. Successful management
                          of AIDS-related sclerosing cholangitis with
                          paromomycin and letrazuril. Int Conf AIDS.
                          1992 Jul 19-24;8(3):87 (abstract no. PuB
                          7229).
 REFERENCES               Guillem S, Gomez M, Romeu J, Raventos A,
                          Fernandez A, Condom MJ, Clotet B. Letrazuril
                          for the treatment of severe cryptosporidial
                          diarrhoea in AIDS. Int Conf AIDS. 1992 Jul
                          19-24;8(2):B129 (abstract no. PoB 3257).
 ENTRY MONTH              9202
 LAST REVISION DATE       960314
 

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