      Document 0237
 DOCN  DRG0237
 UNIQUE IDENTIFIER        DRG-0010
 NAME OF SUBSTANCE        AS 101 [AmFAR Tx Dir May 1989]
 REGISTRY NUMBER          106566-58-9
 STANDARD CHEMICAL NAME   Tellurate (1-), trichloro (1,2-ethanediolato
                          (2-)-O,O')- ammonium, (SP-5-22)- [CHEMLINE]
 SYNONYMS                 Trichloro(dioxoethylene-O,O'-)tellurate
                          [CHEMLINE]
 SYNONYMS                 AS 101 [Int J Immunopharm 1992; Vol 14, No 4]
 SYNONYMS                 AS101 [Int J Immunopharm 1992; Vol 14, No 4]
 SYNONYMS                 Ammonium
                          trichloro(dioxyethylene-O-O'-)tellurate [Int
                          J Immunopharm 1992; Vol 14, No 4]
 SYNONYMS                 Ammonium trichlorotellurate [NIAID ACTG 046]
 PROTOCOL ID NUMBERS      NIAID ACTG 046
 PROTOCOL ID NUMBERS      NIAID 89 CC-75
 PROTOCOL ID NUMBERS      FDA 045A
 PROTOCOL ID NUMBERS      FDA 045B
 PROTOCOL ID NUMBERS      FDA 045C
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Enhances production of colony
                          stimulating factor and interleukin-2 (IL-2)
                          in murine splenocytes and human peripheral
                          blood mononuclear cells and stimulates
                          mitogenesis and increases the percentages of
                          cells with receptors for IL-2. Increases
                          gamma interferon and natural killer cell
                          activity, and tumor necrosis factor
                          production; suppresses growth of
                          methylcholanthrene-induced sarcoma (animal
                          studies); may restore immune function in mice
                          immunosuppressed by irradiation. [AmFAR Tx
                          Dir May 1989] [Nat Immun 1993 Jan-Feb;12(1)]
                          [Intl J Immunopharm 1992; 14(4)]
 DISEASES STUDIED/TREATED Treatment of patients with low CD4 cells and
                          HIV infection [NIAID ACTG 046]
 CLASSIFICATION CODE      Immunomodulator [Int J Immunopharm 1992; Vol
                          14 No 4]
 ADVERSE EFFECTS          May cause transient microscopic hematuria and
                          asymptomatic transient temperature increases,
                          fever, rash, proteinuria, and hypotension.
                          Persistent garlic odor in AIDS/ARC patients.
                          Less frequently seen side effects are nausea,
                          vomiting, and diarrhea. 7 subjects receiving
                          13 mg/m2 IV t.i.w. have experienced a greying
                          of their skin color. [AmFAR Tx Dir May 1989]
                          [NIAID ACTG 046]
 CONTRAINDICATIONS        Should not be used by pregnant women or
                          nursing mothers. [ACTG 046]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Chemically synthesized
                          organotellurium salt [Nat Immun 1993
                          Jan-Feb;12(1)]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C2H4C13O2Te.H4N [CHEMLINE]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 312 [NIAID ACTG 046]
 CHEMICAL/PHYSICAL DATA   STABILITY: When placed in solution, it is
                          hydrated and converted to tellurous acid,
                          tellurium salts, and a small amount of
                          ethylene glycol (about 20 percent of AS-101)
                          [NIAID ACTG 046]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Crystalline white
                          powder [NIAID ACTG 046]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Sterile solution (50 mcg/ml in
                          100 ml vial). [NIAID ACTG 046]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intravenous infusion.
                          [NIAID ACTG 046]
 SUBSTANCE DELIVERY DATA  STORAGE: Refrigerate under dry conditions; is
                          converted to tellurous acid, tellurium salts,
                          and a small amount of ethylene glycol when
                          hydrated. [NIAID ACTG 046]
 MANUFACTURERS            Wyeth-Ayerst Research
 REFERENCES               Amarante JM, Levi GC, Pedro RJ, Galvao PA,
                          Scheinberg M, Levy DS. A double blind
                          controlled study with AS-101 in patients
                          infected with HIV. Int Conf AIDS. 1992 Jul
                          19-24;8(2):B160 (abstract no. PoB 3439).
 REFERENCES               Lewi DS, Acceturi CA, Diaz RS, Lofty C, Sader
                          H. AS 101: tolerability, safety and clinical
                          efficacy in HIV positive patients with
                          advanced disease. Int Conf AIDS. 1992 Jul
                          19-24;8(3):100 (abstract no. PuB 7310).
 REFERENCES               Vonsover A, Loya S, Sredni B, Albeck M,
                          Gotlieb-Stematsky T, Araf O, Hizi A.
                          Inhibition of the reverse transcriptase
                          activity and replication of human
                          immunodeficiency virus type 1 by AS 101 in
                          vitro. AIDS Res Hum Retroviruses. 1992
                          May;8(5):613-23.
 REFERENCES               Falloon J, Ogata-Arakaki D, Baseler M, Davey
                          R, Polis M, Kovacs J, Zurlo J, Zunich K, Lane
                          HC, Masur H. Therapy of HIV infection with
                          AS-101 and zidovudine. Int Conf AIDS. 1990
                          Jun 20-23;6(3):209 (abstract no. S.B.492).
 REFERENCES               Shani A, Tichler T, Catane R, Gurwith M,
                          Rosenszajn LA, Gezin A, Levi E, Schlesinger
                          M, Kalechman Y, Michlin H, et al. Immunologic
                          effects of AS101 in the treatment of cancer
                          patients. Nat Immune Cell Growth Regul.
                          1990;9(3):182-90.
 REFERENCES               Vonsover A, Kalechman Y, Oron M, Shalit F,
                          Albeck M, Sredni B. The immunomodulating and
                          antiviral effects of AS101, an
                          organotellurium compound. Int Conf AIDS. 1989
                          Jun 4-9;5:590 (abstract no. T.C.P.142).
 REFERENCES               Laporte JP, Lebas J, Gonzales G, Meyohas M,
                          Srenndi B, Najman A. AS-101, a new
                          immunomodulating compound in the treatment of
                          AIDS. Int Conf AIDS. 1989 Jun 4-9;5:399
                          (abstract no. W.B.P.283).
 REFERENCES               Laporate JP, Frottier J, Dormont D, Imbert
                          JC, Albeck M, Najman A. As 101 in association
                          with azt in AIDS patients: a phase I pilot
                          study. Int Conf AIDS. 1989 Jun 4-9;5:405
                          (abstract no. W.B.P.320).
 REFERENCES               Nyska A, Waner T, Pirak M, Albeck M, Sredni
                          B. Toxicity study in rats of a tellurium
                          based immunomodulating drug, AS-101: a
                          potential drug for AIDS and cancer patients.
                          Arch Toxicol. 1989;63(5):386-93.
 ENTRY MONTH              8906
 LAST REVISION DATE       960501
 

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