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The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [3] [14] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [15]
Rivaroxaban, sold under the brand name Xarelto among others, is an anticoagulant medication (blood thinner) used to treat and prevent blood clots. [8] Specifically it is used to treat deep vein thrombosis and pulmonary emboli and prevent blood clots in atrial fibrillation and following hip or knee surgery. [ 8 ]
Although, while anticoagulation is the preferred treatment for DVT, [125] thrombolysis is a treatment option for those with the severe DVT form of phlegmasia cerula dorens (bottom left image) and in some younger patients with DVT affecting the iliac and common femoral veins. [12] Of note, a variety of contraindications to thrombolysis exist. [125]
Rivaroxaban. During the SAR development of rivaroxaban, researchers realized that adding a 5-chlorothiophene-2-carboxamide group to the oxazolidonine core could increase the potency by 200 fold, which had previously been too weak for medical use. In addition to this discovery, a clear preference for the (S)-configuration was confirmed.
The abbreviation DVT/PE refers to a VTE where a deep vein thrombosis (DVT) has moved to the lungs (PE or pulmonary embolism). [4] Since the veins return blood to the heart, if a piece of a blood clot formed in a vein breaks off it can be transported to the right side of the heart, and from there into the lungs.
Andexanet alfa is used to stop life-threatening or uncontrollable bleeding in people who are taking rivaroxaban or apixaban. [8] Studies in healthy volunteers show that the molecule binds factor Xa inhibitors and counters their anti-Xa-activity. [11] The first published clinical trial was a prospective, open label, single group study. [12]
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