PMID- 21838659
OWN - NLM
STAT- MEDLINE
DCOM- 20120816
LR  - 20191112
IS  - 1875-6220 (Electronic)
IS  - 1570-1638 (Linking)
VI  - 9
IP  - 2
DP  - 2012 Jun 1
TI  - New parenteral anticoagulants: focus on factor Xa and thrombin inhibitors.
PG  - 129-36
AB  - For decades, unfractionated heparin (UFH) was the most widely used parenteral 
      anticoagulant in a variety of clinical scenarios requiring rapid and reversible 
      anticoagulation. The shortcomings of UFH include a high inter-individual 
      variability and the occurrence of heparin induced thrombocytopenia with the 
      potential for serious thromboembolic complications. These shortcomings prompted 
      the successful clinical development of low molecular weight heparins (LMWH) and 
      indirect factor Xa inhibitors such as fondaparinux. LMWH and fondaparinux 
      demonstrated superiority in many clinical scenarios including acute coronary 
      syndromes (ACS). However the long half-life and the lack of a specific antidote 
      still require the usage of UFH in clinical situations where a rapid reversibility 
      of the anticoagulation is required. Especially in ACS patients undergoing PCI, a 
      direct parenteral inhibition of thrombin with the direct thrombin inhibitor (DTI) 
      bivalirudin proved to be an alternative anticoagulant strategy. This has set the 
      stage for the clinical development of other parenteral DTIs. The reduction in 
      clinical ischemic events that were achieved with indirect factor Xa inhibitors in 
      patients with ACS facilitated the clinical development of the first parenteral 
      direct factor Xa inhibitor, otamixaban which is currently investigated in a phase 
      III clinical trial in patients with ACS undergoing PCI. This article discusses 
      novel parenteral factor Xa and thrombin inhibitors currently under clinical 
      investigation including aptamers, a new class of drugs that allows the parallel 
      development of the combination of active drug and reversal agent, which is 
      facilitated by the DNA or RNA structure of which aptamers are composed of.
FAU - Ahrens, Ingo
AU  - Ahrens I
AD  - University Hospital Freiburg, Internal Medicine III, Department of Cardiology and 
      Angiology, Hugstetter Str. 55, 79106 Freiburg, Germany. 
      ingo.ahrens@uniklinik-freiburg.de
FAU - Bode, Christoph
AU  - Bode C
LA  - eng
PT  - Journal Article
PT  - Review
PL  - United Arab Emirates
TA  - Curr Drug Discov Technol
JT  - Current drug discovery technologies
JID - 101157212
RN  - 0 (Anticoagulants)
RN  - 0 (Factor Xa Inhibitors)
SB  - IM
MH  - Anticoagulants/administration & dosage/pharmacology/*therapeutic use
MH  - Blood Coagulation Disorders/*prevention & control
MH  - *Factor Xa Inhibitors
MH  - Humans
MH  - Infusions, Parenteral
EDAT- 2011/08/16 06:00
MHDA- 2012/08/17 06:00
CRDT- 2011/08/16 06:00
PHST- 2011/04/25 00:00 [received]
PHST- 2011/06/26 00:00 [revised]
PHST- 2011/08/02 00:00 [accepted]
PHST- 2011/08/16 06:00 [entrez]
PHST- 2011/08/16 06:00 [pubmed]
PHST- 2012/08/17 06:00 [medline]
AID - BSP/CDDT/E-Pub/0008 [pii]
AID - 10.2174/1570163811209020129 [doi]
PST - ppublish
SO  - Curr Drug Discov Technol. 2012 Jun 1;9(2):129-36. doi: 
      10.2174/1570163811209020129.