      Document 0192
 DOCN  DRG0192
 UNIQUE IDENTIFIER        DRG-0055
 NAME OF SUBSTANCE        Inosine pranobex [USAN 1996]
 REGISTRY NUMBER          36703-88-5
 STANDARD CHEMICAL NAME   Inosine-2-hydroxypropyldimethyl-ammonium
                          4-acetamido-benzoate (1:3) [USAN 1996]
 SYNONYMS                 Delimmun [Merck Index 1989]
 SYNONYMS                 Immunoviral [Merck Index 1989]
 SYNONYMS                 Inosiplex [Drug Evaluations Annual 1992]
 SYNONYMS                 Isoprinosina [Merck Index 1989]
 SYNONYMS                 Isoprinosine [Drug Evaluations Annual 1992]
 SYNONYMS                 Isoprinosin [Merck Index 1989]
 SYNONYMS                 Methisoprinol [Drug Evaluations Annual 1992]
 SYNONYMS                 Pranosina [Merck Index 1989]
 SYNONYMS                 Pranosine [Merck Index 1989]
 SYNONYMS                 Viruxan [Merck Index 1989]
 SYNONYMS                 INPX [NIAID NS 403]
 SYNONYMS                 Immunovir [Merck Index 1989]
 SYNONYMS                 Aviral [Merck Index 1989]
 PROTOCOL ID NUMBERS      NIAID NS 403
 PROTOCOL ID NUMBERS      FDA 008A
 PROTOCOL ID NUMBERS      FDA 008B
 PROTOCOL ID NUMBERS      FDA 008C
 PROTOCOL ID NUMBERS      FDA 008D
 PROTOCOL ID NUMBERS      FDA 008E
 PROTOCOL ID NUMBERS      FDA 008F
 IND NUMBER               31,103
 SECONDARY SOURCE ID      U.S. Patent 3646,007 [Merck Index 1983]
 SECONDARY SOURCE ID      NP 113 [Merck Index 1989]
 SECONDARY SOURCE ID      NPT 10381 [Merck Index 1989]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Antiviral activity via
                          augmentation of immunologic responsiveness.
                          Inosine pranobex (INPX) is a synthetic
                          immunopotentiating agent which has been shown
                          capable of in vitro enhancement of
                          mitogen-induced lymphocyte proliferation,
                          macrophage activation, T-rosette formation of
                          lymphocyte, natural killer (NK) cell
                          activity, and production of lymphotoxin. In
                          vitro studies have also suggested that
                          isoprinosine may have the ability to enhance
                          interleukin-1 (IL-1) and interleukin-2 (IL-2)
                          production and IL-2 receptor formation. The
                          results of human clinical trials in HIV
                          positive patients with persistent generalized
                          lymphadenopathy (PGL or AIDS related complex
                          (ARC) have shown that INPX had a profound and
                          lasting effect on the immunologic and
                          clinical status of these patients. Treatment
                          with INPX at 3 g/day for 28 days resulted in
                          significant increases in NK cell activity,
                          total T-lymphocytes, and T-helper cells.
                          [Drug Evaluations Annual 1992] [AmFAR Tx Dir
                          May, 1989] [Cancer Detection and Prevention
                          Suppl 1 (1987)]
 DISEASES STUDIED/TREATED Primary HIV infection: Persistent generalized
                          lymphadenopathy (PGL) and ARC [NIAID NS 403]
 CLASSIFICATION CODE      Immunostimulant [Drug Evaluations Annual
                          1992]
 CLASSIFICATION CODE      Antiviral [Drug Evaluations Annual 1992]
 CLASSIFICATION CODE      Antiretroviral [NIAID NS 403]
 OTHER MAJOR USES         Used in Europe to treat a number of viral
                          diseases, including herpesvirus, rhinovirus,
                          influenza A infections, and viral hepatitis.
                          Treatment of subacute sclerosing
                          panencephalitis (SSPE), of immunodepressed
                          patients after burns, cancer chemotherapy,
                          surgery, and other clinically distinct
                          immunodeficiencies [Drug Evaluations Annual
                          1992] [Cancer Detection and Prevention Suppl
                          1 (1987)]
 ADVERSE EFFECTS          Adverse effects include mild and transient
                          elevation of serum and urinary uric acid due
                          to the metabolism of inosine pranobex, and
                          the conversion of the inosine moiety to uric
                          acid through normal purine metabolic pathway.
                          [Meyler's Side Effects of Drugs 1989;797]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Synthetic drug, chemically
                          combining 1 part inosine with 3 parts each of
                          p-acetaminobenzoic acid (PABA) and
                          dimethylamino-isopropanol.
                          Naturally-occurring substance found in the
                          metabolic pathway of purines and in small
                          amounts in
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: cells and tissue fluids
                          [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C52H78N10O17 [Merck Index
                          1989]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 1115.26 [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White crystalline
                          powder [AmFAR Tx Dir May 1989]
 CHEMICAL/PHYSICAL DATA   PERCENT ELEMENTAL COMPOSITION: C56.00%,
                          H7.05%, N12.56%, O24.39% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Neutral water soluble solid
                          [Merck Index 1989]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Capsules (500 mg). [NIAID NS
                          403]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral. [NIAID NS 403]
 MANUFACTURERS            Newport Pharmaceuticals
 REFERENCES               Thorsen S, Pedersen C, Sandstrom E, Petersen
                          CS, Norkrans G, Gerstoft J, Karlsson A,
                          Christensen KC, Hakansson C, Pehrson PO, et
                          al. [Controlled, clinical trial of
                          isoprinosine administration to HIV-infected
                          patients.] Ugeskr Laeger. 1994 May
                          30;156(22):3314-8.
 REFERENCES               Shavdia N, Sharvadze L, Tsertsvadze T,
                          Medulashvili G, Aladashvili M, Chubinishvili
                          O. The comparative efficacy of acyclovir,
                          isoprinosine and their combination in
                          patients with herpes simplex. Int Conf AIDS.
                          1993 Jun 6-11;9(1):354 (abstract no.
                          PO-B08-1313).
 REFERENCES               Thorsen S, Pedersen C, Sandstrom E, Petersen
                          CS, Norkrans G, Gerstoft J, Karlsson A,
                          Christensen KC, Hakansson C, Pehrson PO, et
                          al. One-year follow-up on the safety and
                          efficacy of isoprinosine for human
                          immunodeficiency virus infection. J Intern
                          Med. 1992 Jun;231(6):607-15.
 REFERENCES               Teglbjaerg LL, Kroon S, Sandstrom E, Moestrup
                          T, Hansson BG, Vestergaard BF. Effect of
                          isoprinosine on HIV antigenaemia. AIDS. 1992
                          Feb;6(2):199-201.
 REFERENCES               De Simone C, Famularo G, Tzantzoglou S,
                          Moretti S, Jirillo E. Inosine pranobex in the
                          treatment of HIV infection: a review. Int J
                          Immunopharmacol. 1991;13 Suppl 1:19-27.
 REFERENCES               Thorsen S. Prospective study of isoprinosine
                          in HIV-infected patients: final results from
                          1 year of observation. Int Conf AIDS. 1991
                          Jun 16-21;7(2):222 (abstract no. W.B.2162).
 REFERENCES               Pedersen C, Sandstrom E, Petersen CS,
                          Norkrans G, Gerstoft J, Karlsson A,
                          Christensen KC, Hakansson C, Pehrson PO,
                          Nielsen JO, et al. The efficacy of inosine
                          pranobex in preventing the acquired
                          immunodeficiency syndrome in patients with
                          human immunodeficiency virus infection. N
                          Engl J Med. 1990 Jun 21;322(25):1757-63.
 REFERENCES               Schulof RS, Parenti DM, Simon GL, Paxton H,
                          Meyer WA 3d, Schlesselman SB, Courtless J,
                          LeLacheur S, Sztein MB. Clinical, virologic,
                          and immunologic effects of combination
                          therapy with ribavirin and isoprinosine in
                          HIV-infected homosexual men. J Acquir Immune
                          Defic Syndr. 1990;3(5):485-92.
 REFERENCES               Loveless MO, Robins DS. The effect of
                          isoprinosine R (inosine pranobex) (IP) in
                          HIV-seropositive patients with low risk for
                          developing AIDS. Int Conf AIDS. 1989 Jun
                          4-9;5:399 (abstact no. W.B.P.288).
 REFERENCES               Schulof R, Simon G, Parenti D, Sztein M,
                          Meyer W, Paxton H. Phase I/II trial of
                          ribavirin + isoprinosine in asymptomatic HIV
                          viremic gay men. Int Conf AIDS. 1989 Jun
                          4-9;5:212 (abstract no. Th.B.O.2).
 ENTRY MONTH              8910
 LAST REVISION DATE       960311
 

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