      Document 0182
 DOCN  DRG0182
 UNIQUE IDENTIFIER        DRG-0065
 NAME OF SUBSTANCE        Thymopentin [USAN 1996]
 REGISTRY NUMBER          69558-55-0
 STANDARD CHEMICAL NAME   L-Tyrosine,N-[N-[N-(N(2)-L-arginyl-L-lysyl)
                          -L-alpha-aspartyl]-L-valyl]- [USAN 1996]
 SYNONYMS                 Timunox [Merck Index 1989]
 SYNONYMS                 Thymopoietin 32-36 [USAN 1996]
 SYNONYMS                 TP-5 [Merck Index 1989]
 SYNONYMS                 Immunox [Merck Index 1989]
 SYNONYMS                 Sintomodulina [Merck Index 1989]
 PROTOCOL ID NUMBERS      FDA 015A
 PROTOCOL ID NUMBERS      FDA 015B
 PROTOCOL ID NUMBERS      FDA 015C
 PROTOCOL ID NUMBERS      FDA 015D
 PROTOCOL ID NUMBERS      FDA 015E
 PROTOCOL ID NUMBERS      FDA 015H
 PROTOCOL ID NUMBERS      FDA 015I
 SECONDARY SOURCE ID      US Patent 4U77.949 [USAN 1990]
 SECONDARY SOURCE ID      ORF 15244 [USAN 1996]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: In vitro, TP-5 regulates the
                          function of peripheral T cells, acting via a
                          cyclic GMP-linked cell surface receptor and
                          enhances T-cell functions by increasing
                          lymphokine production. The mechanism of
                          action in HIV disease is unclear. It has been
                          reported that thymopentin had no effect on
                          HIV replication in vitro. Thymopentin is a
                          thymic hormone analog corresponding to
                          residues 32-36 of thymopoietin, which
                          exhibits the full biological activity of the
                          natural hormone. These activities include
                          selective induction of T-cell maturation from
                          prothymocytes and inhibition of B-cell
                          differentiation. The hormone is a factor
                          causing impaired neuromuscular transmission
                          in myasthenia gravis. [AmFAR TX Dir
                          1995;7(4)] [Merck Index 1989]
 DISEASES STUDIED/TREATED Stimulation of immune function in HIV
                          infection [AmFAR Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Immunomodulator [USAN 1996]
 OTHER MAJOR USES         Treatment of rheumatoid arthritis [Ann NY
                          Acad Sci. 1992 May 4;651]
                          [Arzneimittelforschung 1994;44(10)]
 ADVERSE EFFECTS          Adverse effects include respiratory
                          congestion. [AmFAR Tx Dir 1995;7(4)]
                          [Meyler's Side Effects of Drugs, 1989]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Thymopentin (TP-5) is a
                          biologically active synthetic pentapeptide
                          that corresponds to the active site of the
                          thymic hormone, thymopoietin [AmFAR Tx Dir
                          1995;7(4)]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C30H49N9O9 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 679.77 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C53.01%, H7.27%,
                          N18.54%, O21.18% [Merck Index 1989]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intramuscular injection.
                          [FDA 015A-E]
 MANUFACTURERS            Immunobiology Research
 MANUFACTURERS            Ortho Pharmaceutical
 REFERENCES               Goldstein G, Conant MA, Beall G, Grossman HA,
                          Galpin JE, Blick G, Calabrese LH, Hirsch RL,
                          Fisher A, Stampone P, et al. Safety and
                          efficacy of thymopentin in zidovudine
                          (AZT)-treated astmptomatic HIV-infected
                          subjects with 200-500 CD4 cells/mm3: a
                          double-blind placebo-controlled trial. J
                          Acquir Immune Defic Syndr Hum Retrovirol.
                          1995 Mar 1;8(3):279-88.
 REFERENCES               Goldstein G, Conant MA, Beall G, Grossman H,
                          Galpin J, Hirsch RL. Thymopentin with
                          zidovudine (AZT) reduces disease progression
                          in asymptomatic HIV infected patients. Int
                          Conf AIDS. 1993 Jun 6-11;9(1):492 (abstract
                          no. PO-B28-2144).
 REFERENCES               Iannitelli PS, Palacios MF, Diez RA, Sen L,
                          Estevez ME. [Late effect of thymopentin in
                          HIV infection (letter)]. Medicina (B Aires).
                          1993;53(3):280-1.
 REFERENCES               Conant MA, Calabrese LH, Thompson SE, Poiesz
                          BJ, Rasheed S, Hirsch RL, Meyerson LA, Kremer
                          AB, Wang CC, Goldstein G. Maintenance of CD4+
                          cells by thymopentin in asymptomatic
                          HIV-infected subjects: results of a
                          double-blind, placebo-controlled study. AIDS.
                          1992 Nov;6(11):1335-9.
 REFERENCES               Barbarini G, Poma G, Zanaboni D, Capelli D,
                          Comolli G, Campisi D, Chiesa A. Therapy of
                          HIV infection with thymostimulin and
                          zidovudine. Int Conf AIDS. 1991 Jun
                          16-21;7(2):214 (abstract no. W.B.2130).
 REFERENCES               Cognazzo A, Seliak D, Fruttero A. Effect of
                          thymopentin on peripheral blood T-lymphocytes
                          subsets and on the clinical course of the
                          disease in patients affected by multiple
                          sclerosis. Riv Neurol. 1991
                          May-Jun;61(3):110-5.
 REFERENCES               Conant M, Goldstein G, Hirsch RL, Meyerson
                          LA, Kremer AB. Twenty-four week double blind
                          evaluation of thymopentin treatment on
                          disease progression in HIV infected patients.
                          Int Conf AIDS. 1990 Jun 20-23;6(3):207
                          (abstract no. S.B.485).
 REFERENCES               Thompson SE, Calabrese L, Hirsch RL,
                          Longworth D, Rehm S, Kremer AB, Meyerson LA,
                          Goldstein G. Effects of thymopentin on
                          disease progression and surrogate markers in
                          HIV infection - a 1 year study. Int Conf
                          AIDS. 1990 Jun 20-23;6(3):207 (abstract no.
                          S.B.484)
 REFERENCES               Silvestris F, Gernone A, Frassanito MA,
                          Dammacco F. Immunologic effects of long-term
                          thymopentin treatment in patients with
                          HIV-induced lymphadenopathy syndrome. J Lab
                          Clin Med. 1989 Feb;113(2):139-44.
 ENTRY MONTH              8911
 LAST REVISION DATE       960310
 

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