      Document 0030
 DOCN  DRG0030
 UNIQUE IDENTIFIER        DRG-0217
 NAME OF SUBSTANCE        Tecogalan sodium [USAN 1996]
 REGISTRY NUMBER          134633-29-7
 STANDARD CHEMICAL NAME   D-gluco-D-galactan sulfate [FDA 088A]
 SYNONYMS                 DS 4152 [CHEMLINE]
 SYNONYMS                 DS-4152 [USAN 1996]
 SYNONYMS                 SP-PG [AmFAR Tx Dir Jan 1995;7(4)]
 PROTOCOL ID NUMBERS      FDA 088A
 PROTOCOL ID NUMBERS      FDA 088B
 PROTOCOL ID NUMBERS      FDA 088C
 PROTOCOL ID NUMBERS      FDA 088D
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Inhibitory effect of
                          tecogalan sodium on endothelial cell
                          migration and proliferation is thought to be
                          mediated by the inhibition of the binding of
                          fibroblast growth factor to endothelial
                          cells. Tecogalan sodium has shown potent and
                          selective inhibition of HIV-1 replication in
                          vitro. SP-PG (tecogalan sodium) controlled
                          the in vitro growth of AIDS-associated
                          Kaposi's sarcoma (KS)-derived spindle-shaped
                          cells at noncytotoxic concentrations. SP-PG
                          also inhibited the vascular hyperpermeability
                          response and the angiogenesis associated with
                          the induction of KS-like lesions. The
                          antitumor effect of tecogalan is thought to
                          be mediated by the inhibitor of the binding
                          of fibroblast growth factors to cell
                          receptors. Pharmacokinetic studies (in phase
                          I trial) show that the peak plasma
                          concentration correlates with the peak
                          activated partial thromboplastin time and
                          that little of the drug is excreted in the
                          urine. [Proc Annu Meet Am Soc Clin Oncol 13
                          1994] [Science 1992 Mar 13;255(5050)] [Proc
                          Annu Meet Am Assoc Cancer Res 1995;36]
 DISEASES STUDIED/TREATED Inhibitor of Kaposi's sarcoma [AmFAR Tx Dir
                          Jan 1995;7(4)]
 CLASSIFICATION CODE      Angiogenesis inhibitor [AmFAR Tx Dir
                          1995;7(4)]
 OTHER MAJOR USES         Treatment of solid tumors [Proc Annu Meet Am
                          Soc Clin Oncol 13 1994]
 ADVERSE EFFECTS          Adverse effects include prolongation of
                          activated partial thromboplastin time (with
                          peak times being 1.0-4.0 x the upper limit of
                          normal), fever, and chills. [Proc Annu Meet
                          Amm Soc Clin Oncol 13 1994]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Fermentation product of
                          Arthrobacter sp. AT-25, and composed of
                          sulfated polysaccharide and small amounts of
                          peptidoglycan and phosphorous [CHEMLINE]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: ca. 29,000 [USAN 1996]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Intravenous. [FDA 088A]
 MANUFACTURERS            Daiichi Pharmaceutical Corporation
 REFERENCES               Sakamoto T, Ishibashi T, Kimura H, Yoshikawa
                          H, Spee C, Harris MS, Hinton DR, Ryan SJ.
                          Effect of tecogalan sodium on angiogenesis in
                          vitro by choroidal endothelial cells. Invest
                          Ophthalmol Vis Sci 1995 May;36(6):1076-83.
 REFERENCES               Bicknell R. Vascular targeting and the
                          inhibition of angiogenesis. Ann Oncol 1994;5
                          Suppl 4:45-50.
 REFERENCES               Chleboun JO, Sellers P, Muir G, Chew P,
                          Martins RN. The effect of tecogalan sodium on
                          the development of the collateral circulation
                          after acute arterial occlusion. Biochem
                          Biophys Res Commun 1994 Jul
                          29;202(2):1149-55.
 REFERENCES               Krown SE. AIDS-related Kaposi's sarcoma:
                          clinical aspects (Meeting abstract). Proc
                          Annu Meet Am Assoc Cancer Res;35:659-60 1994.
 REFERENCES               Eckhardt SG, Burris HA, Eckardt JR, Weiss G,
                          Rinaldi D, Barrington R, Smith L, Fields S,
                          Kuhn J, Smith S, et al. Phase I assessment of
                          the novel angiogenesis inhibitor DS4152
                          (Tecogalan Sodium) (Meeting abstract). Proc
                          Annu Meet Am Soc Clin Oncol. 1994;13:A23.
 REFERENCES               Baba M, Shigeta S, Ikeuchi T, Korenaga H,
                          Osada Y. Anti-angiogenesis agent DS-4152 is a
                          potent and selective inhibitor of HIV-1
                          replication in vitro. AIDS. 1994
                          Jan;8(1):43-8.
 REFERENCES               Nakayama Y, Iwahana M, Sakamoto N, Tanaka NG,
                          Osada Y. Inhibitory effects of a
                          bacteria-derived sulfated polysaccharide
                          against basic fibroblast growth
                          factor-induced endothelial cell growth and
                          chemotaxis. J Cell Physiol 1993
                          Jan;154(1):1-6.
 REFERENCES               Tanaka NG, Sakamoto N, Inoue K, Korenaga H,
                          Kadoya S, Ogawa H, Osada Y. Antitumor effects
                          of an antiangiogenic polysaccharide from an
                          Arthrobacter species with or without a
                          steroid. Cancer Res;VOL 49,ISS
                          23,1989,P6727-30.
 ENTRY MONTH              9409
 LAST REVISION DATE       960424
 

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