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QuickView for ximelagatran (compound)


PubChem
Name: ximelagatran
PubChem Compound ID: 9574101
Molecular formula: C24H35N5O5
Molecular weight: 473.565 g/mol
Synonyms:
D01981; Exanta; H-376/95; 192939-46-1; Ximelagatran; H 376-95; Ethyl (((1R)-1-cyclohexyl-2-((2S)-2-((4-(hydroxycarbamimidoyl)benzyl)carbamoyl)azetidin-1-yl-2-oxoethyl)amino)acetate; Glycine, N-((1)1-cyclohexyl-2-((2)-((((4-(amino(hydroxyimino)methyl)phenyl)methyl)amino)carbonyl)-1-azetidinyl)2-oxoethyl)-, ethyl ester; H 376/95; H 37695.
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DrugBank
Identification
Name: ximelagatran
Name (isomeric): DB04898
Drug Type: small molecule
Synonyms:
H 376/95
Brand: Exarta, Exanta
Category: Anticoagulants, Antithrombotic Agents
CAS number: 192939-46-1
Pharmacology
Indication: For the treatment of acute deep vein thrombosis.
Mechanism of Action: Ximelagatran was the first member of the drug class of direct thrombin inhibitors that can be taken orally. It acts solely by inhibiting the actions of thrombin. Ximelagatran is a prodrug, being converted in vivo to the active agent melagatran.
Absorption: Rapidly absorbed by the small intestine with an oral bioavailability of 20%.
Biotransformation: Hepatic. Ximelagatran is a prodrug, being converted in vivo to the active agent melagatran. This conversion takes place in the liver and many other tissues through dealkylation and dehydroxylation (replacing the ethyl and hydroxyl groups with hydrogen).
Half Life: 3-5 hours
Toxicity: Hepatotoxicity (liver damage) was reported during trials.
Affected organisms: Humans and other mammals

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