Xarelto (rivaroxaban)

The following drug information is obtained from various newswires, published medical journal articles, and medical conference presentations.

Approval Status:

Approved October 2018

Specific Treatments:

major cardiovascular (CV) events in people with chronic coronary or peripheral artery disease

Therapeutic Areas

General Information

Xarelto (rivaroxaban) is a factor Xa inhibitor.

Xarelto is specifically indicated for use in combination with aspirin, to reduce the risk of major cardiovascular events (cardiovascular (CV) death, myocardial infarction (MI) and stroke) in patients with chronic coronary artery disease (CAD) or peripheral artery disease (PAD).

Xarelto is supplied as a tablet for oral administration. The recommended dose is this population is 2.5 mg orally twice daily, with or without food, in combination with aspirin (75-100 mg) once daily.

Clinical Results

FDA Approval

The FDA approval of Xarelto for risk reduction of major cardiovascular (CV) events in people with chronic coronary or peripheral artery disease was based on COMPASS, a Phase 3 clinical study of 27,395 patients with chronic CAD or PAD from 33 countries. The trial examined the use of Xarelto, alone or in combination with aspirin, for the long-term prevention of major adverse CV events, including heart attack, stroke and CV death. Results showed a significant 24% reduction of the risk of major CV events in patients with chronic CAD and/or PAD with the Xarelto 2.5-mg vascular dose twice daily plus aspirin 100 mg once daily, compared to aspirin alone. Specifically data showed a 42% reduction in stroke, 22% reduction in CV death and 14% reduction in heart attack. The risk of major bleeding was significantly higher in patients taking the Xarelto/aspirin regimen compared to aspirin alone, with no significant increase in fatal or intracranial bleeds.

Side Effects

The most common adverse effect associated with the use of Xarelto is bleeding.

The Xarelto drug label comes with the following Black Box Warning:

(A) Premature discontinuation of Xarelto increases the risk of thrombotic events Premature discontinuation of any oral anticoagulant, including Xarelto, increases the risk of thrombotic events. To reduce this risk, consider coverage with another anticoagulant if Xarelto is discontinued for a reason other than pathological bleeding or completion of a course of therapy. (B) Spinal/epidural hematoma Epidural or spinal hematomas have occurred in patients treated with Xarelto who are receiving neuraxial anesthesia or undergoing spinal puncture. These hematomas may result in long-term or permanent paralysis.  Monitor patients frequently for signs and symptoms of neurological impairment and if observed, treat urgently. Consider the benefits and risks before neuraxial intervention in patients who are or who need to be anticoagulated.

Mechanism of Action

Xarelto is a selective inhibitor of factor Xa (FXa). It does not require a cofactor (such as Anti-thrombin III) for activity. Rivaroxaban inhibits free FXa and prothrombinase activity. Rivaroxaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, rivaroxaban decreases thrombin generation.

Additional Information

For additional information regarding Xarelto and it's ability to reduce the risk of major cardiovascular (CV) events in people with chronic coronary or peripheral artery disease, please visit https://www.xarelto-us.com