Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development

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Fältnamn	Indikatorer	Metadata
000		03003naa a2200397 4500
001		oai:gup.ub.gu.se/107026
003		SwePub
008		240528s2009 \| \|\|\|\|\|\|\|\|\|\|\|000 \|\|eng\|
024	7	a https://gup.ub.gu.se/publication/1070262 URI
040		a (SwePub)gu
041		a eng
042		9 SwePub
072	7	a ref2 swepub-contenttype
072	7	a art2 swepub-publicationtype
100	1	a Eriksson, Bengt I.,d 1946u Gothenburg University,Göteborgs universitet,Institutionen för kliniska vetenskaper,Institute of Clinical Sciences4 aut0 (Swepub:gu)xerben
245	1 0	a Comparative pharmacodynamics and pharmacokinetics of oral direct thrombin and factor xa inhibitors in development
264	1	c 2009
520		a For the past five decades, there has been little progress in the development of oral anticoagulants, with the choices being limited to the vitamin K antagonists (VKAs). The situation is changing with the development of orally active small molecules that directly target thrombin or activated factor X (FXa). The two agents in the most advanced stages of development are dabigatran etexilate and rivaroxaban, which inhibit thrombin and FXa, respectively. Both are approved in the EU and Canada for venous thromboprophylaxis in patients undergoing elective hip- or knee-replacement surgery. Other agents in the early stages of development include several FXa inhibitors (apixaban, DU 176b, LY 517717, YM 150, betrixaban, eribaxaban [PD 0348292] and TAK 442) and one thrombin inhibitor (AZD 0837). With a predictable anticoagulant response and low potential for drug-drug interactions, these new agents can be given in fixed doses without coagulation monitoring. This renders them more convenient than VKAs. While the anticoagulant effect of the new thrombin and FXa inhibitors is similar, differences in the pharmacokinetic and pharmacodynamic parameters may influence their use in clinical practice. Here, we compare the pharmacokinetic and pharmacodynamic features of these new oral agents.
650	7	a MEDICIN OCH HÄLSOVETENSKAPx Klinisk medicinx Kirurgi0 (SwePub)302122 hsv//swe
650	7	a MEDICAL AND HEALTH SCIENCESx Clinical Medicinex Surgery0 (SwePub)302122 hsv//eng
653		a Animals
653		a Antithrombin III/pharmacokinetics/pharmacology
653		a Benzimidazoles/pharmacokinetics/pharmacology
653		a Drug Discovery
653		a Humans
653		a Morpholines/pharmacokinetics/pharmacology
653		a Pyrazoles/pharmacokinetics/pharmacology
653		a Pyridines/pharmacokinetics/pharmacology
653		a Pyridones/pharmacokinetics/pharmacology
653		a Thiophenes/pharmacokinetics/pharmacology
653		a Thrombin/*antagonists & inhibitors
700	1	a Quinlan, D. J.4 aut
700	1	a Weitz, J. I.4 aut
710	2	a Göteborgs universitetb Institutionen för kliniska vetenskaper4 org
773	0	t Clin Pharmacokinetg 48:1, s. 1-22q 48:1<1-22x 0312-5963
856	4 8	u https://gup.ub.gu.se/publication/107026

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Av författaren/redakt...: Eriksson, Bengt ...; Quinlan, D. J.; Weitz, J. I.

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MEDICIN OCH HÄLSOVETENSKAP: MEDICIN OCH HÄLS ...; och Klinisk medicin; och Kirurgi

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Av lärosätet: Göteborgs universitet

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