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Melagatran

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. more...

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Method 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. It is taken orally twice daily, and rapidly absorbed by the small intestine. 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).

Uses

Ximelagatran was expected to replace warfarin and sometimes aspirin and heparin in many therapeutic settings, including deep venous thrombosis, prevention of secondary venous thromboembolism and atrial fibrillation. The efficacy of ximelagatran for these indications had been well-documented (Eriksson et al 2003, Frances et al 2004, Schulman et al 2004).

An advantage, according to early reports by its manufacturer, was that it could be taken orally without any monitoring of its anticoagulant properties. This would have set it apart from warfarin and heparin, which require monitoring of the international normalized ratio (INR) and the partial thromboplastin time (PTT), respectively. A disadvantage recognised early was the absence of an antidote in case acute bleeding develops, while warfarin can be antagonised by vitamin K and heparin by protamine sulfate.

Side-effects

Ximelagatran was generally well tolerated in the trial populations, but a small proportion (5-6%) developed elevated liver enzyme levels, which prompted the FDA to reject an initial application for approval in 2004. The further development was discontinued in 2006 after it turned out hepatic damage could develop in the period subsequent to withdrawal of the drug. According to AstraZeneca, a chemically different but pharmacologically similar substance, AZD0837, is undergoing testing for similar indications.

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Safety Syringes Inc. and AstraZeneca Announce Launch in Europe of Injectable Form of Exanta with the UltraSafe Passive Delivery System
From Business Wire, 6/24/04

CARLSBAD, Calif. & MOLNDAL, Sweden -- Safety Syringes Inc. and AstraZeneca this week announced the first launch in Germany of oral and injectable Exanta(TM) in its first indication prevention of venous thromboembolic events (VTE) in elective hip or knee replacement surgery (orthopaedic surgery). The European treatment regimen for Exanta involves an early postoperative start of treatment, with initial injectable dosing administered 4-8 hours after the completion of surgery, followed by oral Exanta 24mg twice daily for up to 11 days. This approach supports the increasing use of relatively early postoperative initiation of VTE preventative treatment in clinical practice across Europe.

The injectable form of Exanta (Melagatran AstraZeneca(TM)) is using the UltraSafe(R) Passive(TM) Delivery System to enhance protection of health care personnel against blood transmitted diseases. "Exanta is a new anticoagulant and the first oral treatment in a new class of direct thrombin inhibitors (DTIs), and we are pleased to launch the injectable form of Exanta in an innovative drug delivery system," commented Thomas Rask, Global Brand Manager. "We found the UltraSafe Passive Delivery System to be clearly preferred to standard prefilled syringes because of its safety profile in protecting from needle injuries."

"AstraZeneca is to be commended for their commitment to clinician safety, they have a terrific new treatment regimen and they have been a terrific partner," stated Christer Andreasson, Safety Syringes Inc.'s CEO. "The UltraSafe Passive Delivery System meets or exceeds all needle safety standards to date. It has also proven to be widely preferred by clinicians as a delivery system for injectable medications."

Designed to ensure the ultimate in user preference, compliance and protection, the UltraSafe Passive Delivery System is intended for unit dose, prefilled glass syringe presentations. The easy-to-use, intuitive and innovative system provides an optimal drug delivery system with the preferred passive activation method.

--Founded in 1991, Safety Syringes Inc. is a global market leader for drug delivery systems for pre-filled glass syringes. The UltraSafe Delivery System has been marketed since 1999. U.S. and international patents protect all products developed and marketed by Safety Syringes Inc.

--AstraZeneca is a major international healthcare business engaged in the research, development, manufacture and marketing of prescription pharmaceuticals and the supply of healthcare services. It is one of the world's leading pharmaceutical companies with healthcare sales of over $18.8 billion and leading positions in sales of gastrointestinal, oncology, cardiovascular, neuroscience and respiratory products. AstraZeneca is listed in the Dow Jones Sustainability Index (Global and European) as well as the FTSE4Good Index.

-- Exanta(TM) is a trademark of the AstraZeneca group of companies

--UltraSafe(R) Passive(TM) is a registered trademark of Safety Syringes Inc.

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