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Pharmacological properties of betrixaban
#MMPMID29977164
Huisman MV
; Klok FA
Eur Heart J Suppl
2018[May]; 20
(Suppl E
): E12-E15
PMID29977164
show ga
Venous thromboembolism (VTE) in acute medically ill patients is a leading cause
of in-hospital morbidity and mortality. A majority of these VTE events occur
post-discharge, and patients remain at increased VTE risk for up to 3?months
post-discharge. Recent clinical trials of extended-duration thromboprophylaxis
with enoxaparin, rivaroxaban, and apixaban in acute medically ill patients did
not demonstrate a net clinical benefit compared with in-hospital
thromboprophylaxis, and were shown to be associated with higher risks of major
bleeding. Betrixaban is a new direct oral anticoagulant (DOAC) with a different
pharmacokinetic profile than other DOACs. Betrixaban has the longest half-life
among the DOAC class, with a terminal half-life of 35-45?h and an effective
half-life of 19-27?h. Betrixaban has a low peak-to-trough ratio compared with
other anticoagulants and a predictable duration of drug exposure, leading to
overall consistent anticoagulant effect over 24?h. Betrixaban is mainly cleared
via the hepatobiliary system and therefore not contraindicated in patients with
severe renal insufficiency. Betrixaban was recently approved for the indication
of extended thromboprophylaxis in the United States based on the APEX trial of
betrixaban 80?mg once daily for 35-42?days compared with low molecular weight
heparin enoxaparin for 10?±?4?days in hospitalized acute medically ill patients.
This study demonstrated that extended-duration betrixaban reduced VTE compared
with standard-duration enoxaparin in acute medically ill patients, without
increased risk of major bleeding. This patient population at risk of VTE may
benefit from extended prophylaxis, ensuring continuum of care from in-hospital to
post-discharge.