Ximelagatran | Genelabs.com

Ximelagatran (Exanta® or Exarta®, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would not attempt to market ximelagatran after reports of hepatotoxicity (liver damage) during trials, and to discontinue its distribution in countries where the drug had been approved.
Brands	Exanta Exarta
Categories	Anticoagulants Antithrombotic Agents
Synonyms	H 376/95

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.

toxicity

Hepatotoxicity (liver damage) was reported during trials.

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).

absorption

Rapidly absorbed by the small intestine with an oral bioavailability of 20%.

half life

3-5 hours

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