Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai
Patent
1992-06-24
1994-04-26
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
C-o-group doai
A61K 31045
Patent
active
053067320
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a tumour necrosis factor (TNF) antagonist. TNF is a mediator in the immune system.
Vinigrol is a known compound. It was purified from a culture of the fungus Virgaria nigra by Fujisawa Pharmaceutical company Limited, who also described anti-hypertensive and platelet aggregation inhibitory properties of the compound. The preparation and some pharmacological actions of vinigrol are described by Ando et al, J. Antibiotics XLI, 25-30 (1988) and Ando et al, J. Antibiotics XLI, 31-35 (1988). The structure of vinigrol has been reported by Uchida et al, J. Org. Chem. 52, 529203 (1987) and is: ##STR1##
We have now found that vinigrol is a TNF antagonist. Vinigrol or one of its pharmaceutically acceptable salts may therefore be used to treat endotoxic shock, inflammation, infection or cachexia.
Accordingly, the present invention provides the use of vinigrol or a pharmaceutically acceptable salt thereof in the preparation of a medicament for use as a TNF antagonist. An agent for use as a TNF antagonist according to the invention therefore comprises vinigrol or a pharmaceutically acceptable salt thereof.
A patient is treated according to the present invention by a method comprising administering to the patient an effective amount of vinigrol or a pharmaceutically acceptable salt of vinigrol. In this way, vinigrol or the vinigrol salt can be used to control conditions attributable to TNF such as endotoxic shock, inflammation, infection and cachexia.
The vinigrol or vinigrol salt can be administered in a variety of dosage forms, for example orally such as in the form of tablets, capsules, sugar- or film-coated tablets, liquid solutions or suspensions or parenterally, for example intramuscularly, intravenously or subcutaneously. The vinigrol or vinigrol salt may therefore be given by injection or infusion.
The dosage depends on a variety of factors including the age, weight and condition of the patient and the route of administration. Typically, however, the dosage adopted for each route of administration to adult humans is 0.001 to 10 mg/kg body weight. Such a dosage may be given from 1 to 5 times daily.
Vinigrol or a vinigrol salt are formulated for use as a pharmaceutical composition also comprising a pharmaceutically acceptable carrier or diluent. The pharmaceutical compositions are typically prepared following conventional methods and are administered in a pharmaceutically suitable form.
For example, the solid oral forms may contain, together with the active compound, diluents such as lactose, dextrose, saccharose, cellulose, corn starch or potato starch; lubricants such as silica, talc, stearic acid, magnesium or calcium stearate and/or polyethylene glycols; binding agents such as starches, arabic gums, gelatin, methylcellulose, carboxymethylcellulose, or polyvinyl pyrrolidone; disaggregating agents such as a starch, alginic acid, alginates or sodium starch glycolate; effervescing mixtures; dye-stuffs; sweeteners; wetting agents such as lecithin, polysorbates, laurylsulphates. Such pharmaceutical preparations may be manufactured in known manner, for example by means of mixing, granulating, tabletting, sugar coating, or film-coating processes.
Liquid dispersions for oral administration may be syrups, emulsions and suspensions. The syrups may contain as carrier, for example, saccharose or saccharose with glycerine and/or mannitol and/or sorbitol. In particular a syrup for diabetic patients can contain as carriers only products, for example sorbitol, which do not metabolise to glucose or which only metabolise a very small amount to glucose. The suspensions and the emulsions may contain as carrier, for example a natural gum, agar, sodium alginate, pectin, methylcellulose, carboxymethylcellulose or polyvinyl alcohol.
Suspensions or solutions for intramuscular injections may contain, together with the active compound, a pharmaceutically acceptable carrier such as sterile water, olive oil, ethyl oleate, glycols such as propylene glycol, and, if desired, a suitable amount of lidocaine hydro
REFERENCES:
The Journal of Antibiotics, vol. XLI, No. 1, 1988, Takeshi Ando et al.: "Vinigrol, a novel antihypertensive and platelet aggregation inhibitory agent produced by a fungus, Virgaria Nigra", pp. 25-30.
Nature, vol. 330, Dec. 17, 1987, K. J. Tracey et al.: "Anti-cachectin/TNF monoclonal antibodies prevent septic shock during lethal bacteraemic", pp. 662-664.
Depledge Paul
Jackson Andrew P.
Norris David B.
Goldberg Jerome D.
Xenova Limited
LandOfFree
Tumor necrosis factor antagonist does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Tumor necrosis factor antagonist, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Tumor necrosis factor antagonist will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1712024