      Document 0120
 DOCN  DRG0120
 UNIQUE IDENTIFIER        DRG-0127
 NAME OF SUBSTANCE        Trichosanthin [Facts and Comparisons 1995]
 REGISTRY NUMBER          60318-52-7
 SYNONYMS                 Compound Q [Facts and Comparisons 1995]
 PROTOCOL ID NUMBERS      FDA 106A
 SECONDARY SOURCE ID      GLQ-223 [Facts and Comparisons 1995]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Trichosanthin is a ribosomal
                          inhibitory protein which, in vitro, inhibits
                          HIV replication in lymphocytes and
                          macrophages, and specifically kills HIV
                          infected macrophages. GLQ-223 induces a
                          humoral immune response in patients with AIDS
                          and ARC. Frequency and time to development of
                          an IgG response appear to be dose related.
                          IgG antibodies to GLQ-223 do not appear to
                          cause adverse clinical events, may result in
                          decreased severity and frequency of side
                          effects, and do not seem to abrogate effects
                          of GLQ-223 on immunologic parameters. After
                          IV administration GLQ-223 undergoes rapid
                          distribution followed by a slower elimination
                          phase with a half-life of approximately 3
                          hours. [Int Conf AIDS 1992 Jul
                          19-24;8(3):(abstract no. PuB 7314)] [Int Conf
                          AIDS 1991 Jun 16-21;7(2):(abstract no
                          W.B.2171] [Antimicrob Agents Chemother 1994
                          Feb;38(2)]
 DISEASES STUDIED/TREATED HIV infection [Facts and Comparisons 1996]
 CLASSIFICATION CODE      Antiretroviral [Facts and Comparisons 1996]
 CLASSIFICATION CODE      Immunosuppressant [Nucleic Acids Res 1991 Nov
                          25;19(22)]
 CLASSIFICATION CODE      Antineoplastic [Nucleic Acids Res 1991 Nov
                          25;19(22)]
 CLASSIFICATION CODE      Abortifacient [Merck Index 1989]
 OTHER MAJOR USES         Treatment of trophoblastic tumors;
                          abortifacient  [Nucleic Acids Res 1991 Nov
                          25;19(22)] [Merck Index 1989]
 SUBSTANCE INTERACTIONS   In patients failing zidovudine response, with
                          decreasing CD4 cell levels, the addition of
                          trichosanthin has been shown to reverse this
                          trend. [Int Conf AIDS 1991 Jun
                          16-21;7(2):(abstract no. W.B.2171)]
 ADVERSE EFFECTS          Adverse effects include flu-like syndrome
                          characterized by fever, headache, myalgias,
                          and pharyngitis; allergic reactions
                          characterized primarily by rash, pruritis,
                          and rare hypertension. Transient confusion is
                          seen rarely, and transient elevations in
                          creatinine kinase have been noticed. [Int
                          Conf AIDS 1992 Jul 9-24;8(3):(abstract no.
                          PuB 7290)] [Antimicrob Agents Chemother 1994
                          Feb;38(2)]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Plant single chain
                          ribosome-inactivating protein [CRC Handbook
                          of Antibiotic Compounds Vol XIV, Pt 1] [Int
                          Conf AIDS 1991 Jun 16-21;7(2) (abstract no.
                          W.A.1064] [The Extra Pharmacopoeia 1993]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Purified from fresh root
                          tubers of the plant Trichosanthas kirilowii
                          [Int Conf AIDS 1991 Jun 16-21;7(2): (abstract
                          no. W.A. 1064)] [CRC Handbook of Antibiotic
                          Compounds Vol XIV, Pt 1] [The Extra
                          Pharmacopeia 30th edition 1993]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: GLQ-223 (Compound Q) is a
                          highly purified form of trichosanthin [Int
                          Conf AIDS 1991 Jun 16-21;7(2) (abstract no.
                          W.A.1064)] [CRC Handbook of Antibiotic
                          Compounds Vol XIV, Pt 1] [The Extra
                          Pharmacopoeia 1993]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION:  White crystals [CRC
                          Handbook of Antibiotic compounds Vol XIV, Pt
                          1, 1987]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT:  24000 [CRC Handbook of
                          Antibiotic Compounds Vol XIV, Pt 1, 1987]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY:  Poorly soluble in acetone and
                          hexane [CRC Handbook of Antibiotic Compounds
                          Vol XIV, Pt 1, 1987]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intravenous infusion,
                          intramuscular. [Int Conf AIDS 1992 Jul 19-24
                          8(3):(abstract no. PoB 7314)] [Antimicrob
                          Agents Chemother 1994 Feb;38(2)]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Injection. [Antimicrob Agents
                          Chemother 1994 Feb;38(2)]
 MANUFACTURERS            Genelabs, Incorporated
 REFERENCES               Kahn J, Gorelick K. Results of a randomized
                          study of GLQ223 in AIDS and ARC. Int Conf
                          AIDS. 1994 Aug 7-12;10(1):8 (abstact no.
                          006B).
 REFERENCES               Byers VS, Levin AS, Malvino A, Waites L,
                          Robins RA, Baldwin RW. A phase II study of
                          effect of addition of trichosanthin to
                          zidovudine in patients with HIV disease and
                          failing antiretroviral agents. AIDS Res Hum
                          Retroviruses. 1994 Apr;10(4):413-20.
 REFERENCES               Kahn JO, Gorelick KJ, Gatti G, Arri CJ,
                          Lifson JD, Gambertoglio JG, Bostrom A,
                          Williams R. Safety, activity, and
                          pharmacokinetics of GLQ223 in patients with
                          AIDS and AIDS-related complex. Antimicrob
                          Agents Chemother. 1994 Feb;38(2):260-7.
 REFERENCES               Batts D, Cox SR, Dietz AJ, Hanover C, Peel
                          BG, Staton BA. A phase I comparative study of
                          the safety, tolerance and pharmacokinetics
                          (PK) of 14 1/2 days of oral U-87,201E in men
                          versus women. Int Conf AIDS. 1992 Jul
                          19-24;8(2):B88 (abstact no. PoB 3009).
 REFERENCES               Kunz AY, Kahn JO, Gorelick KJ, Chew T, Lang
                          W, Williams R. Safety of GLQ223 in patients
                          with AIDS and ARC. Int Conf AIDS. 1992 Jul
                          19-24;8(3):97 (abstract no. PuB 7290).
 REFERENCES               Lifson J, Kahn JO, Chew T, Gorelick KJ, Lang
                          W, Williams R. Anti-GLQ223 antibodies in
                          treated patients with AIDS and ARC. Int Conf
                          AIDS. 1992 Jul 19-24;8(3):101 (abstract no.
                          PuB 7314).
 REFERENCES               Gorelick KJ, Kahn JO, Lang W, Chew T,
                          Williams R. Phase IB study of GLQ223 in AIDS:
                          surrogate markers. Int Conf AIDS. 1992 Jul
                          19-24;8(2):B160 (abstract no. PoB 3442).
 REFERENCES               Mayer RA, Sergios PA, Coonan K, O'Brien L.
                          Trichosanthin treatment of HIV-induced immune
                          dysregulation. Eur J Clin Invest. 1992
                          Feb;22(2):113-22.
 REFERENCES               Byers V, Levin AS, Waites L, Malvino A,
                          Robins RA, Baldwin RW. A phase II study of
                          the effect of trichosanthin treatment in
                          combination with zidovudine in HIV disease.
                          Int Conf AIDS. 1991 Jun 16-21;7(2):224
                          (abstract no. W.B.2171).
 REFERENCES               Ciesielka J, Jacobs M, Chew T, Williams R. A
                          phase I study to evaluate the tolerance and
                          safety of GLQ223 in HIV positive individuals.
                          Int Conf AIDS. 1991 Jun 16-21;7(2):202
                          (abstract no. W.B.2080).
 ENTRY MONTH              9111
 LAST REVISION DATE       960311
 

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