Edoxaban

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Edoxaban
Edoxaban skeletal.svg
Systematic (IUPAC) name
N'-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[(5-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl]oxamide
Clinical data
Trade names Lixiana
Legal status
?
Identifiers
CAS number 912273-65-5 YesY
ATC code None
PubChem CID 25022378
UNII NDU3J18APO N
KEGG D09710 N
Chemical data
Formula C24H30ClN7O4S 
Mol. mass 548.056 g/mol
 N (what is this?)  (verify)

Edoxaban (INN, codenamed DU-176b, trade name Lixiana) is an anticoagulant drug which acts as a direct factor Xa inhibitor. It is being developed by Daiichi Sankyo. It was approved in July 2011 in Japan for prevention of venous thromboembolisms (VTE) following lower-limb orthopedic surgery.[1]

Preclinical research[edit]

In animal studies, edoxaban is potent, selective for factor Xa and has good oral bioavailability.[2]

Clinical trials[edit]

Several Phase II clinical trials have been conducted, for example for thromboprophylaxis after total hip replacement[3] (phase III early results compare well to enoxaparin[4]), and for stroke prevention in patients with atrial fibrillation[5] (phase III has completed enrollment[4]).

A large phase III trial showed that edoxaban was non inferior to warfarin in preventing recurrent venous thromboembolic events with fewer episodes of major bleeding.[6] This paper follows similar recent major trials showing similar results for the other new factor Xa inhibitors, rivaroxaban and apixaban.[5]

References[edit]

  1. ^ "First market approval in Japan for LIXIANA (Edoxaban)". Press Release. Daiichi Sankyo Europe GmbH. 2011-04-22. 
  2. ^ Furugohri T, Isobe K, Honda Y, Kamisato-Matsumoto C, Sugiyama N, Nagahara T, Morishima Y, Shibano T (September 2008). "DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles". J. Thromb. Haemost. 6 (9): 1542–9. doi:10.1111/j.1538-7836.2008.03064.x. PMID 18624979. 
  3. ^ Raskob, G.; Cohen, A. T.; Eriksson, B. I.; Puskas, D.; Shi, M.; Bocanegra, T.; Weitz, J. I. (2010). "Oral direct factor Xa inhibition with edoxaban for thromboprophylaxis after elective total hip replacement". Thrombosis and Haemostasis 104 (3): 642–649. doi:10.1160/TH10-02-0142. PMID 20589317.  edit
  4. ^ a b "Phase III Trial Finds Edoxaban Outclasses Enoxaparin in Preventing Venous Thromboembolic Events". 8 Dec 2010. 
  5. ^ a b Weitz JI, Connolly SJ, Patel I, Salazar D, Rohatagi S, Mendell J, Kastrissios H, Jin J, Kunitada S (September 2010). "Randomised, parallel-group, multicentre, multinational phase 2 study comparing edoxaban, an oral factor Xa inhibitor, with warfarin for stroke prevention in patients with atrial fibrillation". Thromb. Haemost. 104 (3): 633–41. doi:10.1160/TH10-01-0066. 
  6. ^ "Edoxaban versus Warfarin for the Treatment of Symptomatic Venous Thromboembolism". N. Engl. J. Med. 369 (15): 1406–15. August 2013. doi:10.1056/NEJMoa1306638. PMID 23991658.