Edoxaban tosylate monohydrate

Table of contents

• What is edoxaban?
• How does edoxaban work?
• Which conditions is edoxaban used or studied for?
• How is edoxaban given?
• What do the clinical trials show?
• What side effects are known?

What is edoxaban?

Edoxaban tosylate monohydrate, known simply as edoxaban, is a chemically synthesised anticoagulant medicine, meaning it helps prevent blood clots from forming.^[6] It belongs to a class of medicines called direct oral anticoagulants (DOACs) and is classified under the ATC code B01AF03. Edoxaban is authorised as a medicine in the European Union under the brand name Lixiana.^[4] It is available only with a prescription.^[6]

How does edoxaban work?

Edoxaban is a factor Xa inhibitor. It blocks factor Xa, an enzyme involved in the production of thrombin, a substance essential for blood clotting. By blocking factor Xa, edoxaban reduces the levels of thrombin in the blood, which helps treat existing clots and reduces the risk of new ones forming in arteries and veins.^[4] This mechanism helps prevent conditions such as deep vein thrombosis (DVT), pulmonary embolism, and stroke.^[6][4]

Which conditions is edoxaban used or studied for?

Edoxaban is authorised for use in adults for several conditions, and additional trials are exploring its use in other situations.

• Atrial fibrillation — an irregular heart rhythm that increases the risk of stroke; edoxaban is authorised to prevent stroke and systemic embolism in people with this condition.^[4]
• Deep vein thrombosis (DVT) — a blood clot in a deep vein, usually in the leg; edoxaban is authorised to treat DVT and prevent it from recurring.^[6][4]
• Pulmonary embolism — a blood clot in the lungs; edoxaban is authorised to treat this condition and prevent it from recurring.^[6][4]
• Chronic subdural hematoma with atrial fibrillation — a collection of blood on the brain surface in people with an irregular heart rhythm; a Phase 4 trial is studying when to restart edoxaban after surgery for this condition.^[3]
• Frail older patients with atrial fibrillation or venous thromboembolism — a low-intervention study is testing a single measurement and adjustment strategy for edoxaban and other DOACs in this population.^[1]
• Incidental subsegmental pulmonary embolism in cancer patients — a Phase 3 trial is comparing edoxaban and other anticoagulants against no treatment in cancer patients with this type of clot.^[2]

How is edoxaban given?

Edoxaban comes as a film-coated tablet that is swallowed with water.^[6] It is taken orally, once a day, with or without food.^[6] The usual dose is 60 mg once a day, but the dose may be adjusted based on kidney function, low body weight, or use of certain other medicines known as P-gp inhibitors.^[4] In the clinical trials listed, edoxaban is given orally at a dose of 60 mg in two studies.^[3][1][2]

What do the clinical trials show?

Three authorised clinical trials are investigating edoxaban in different patient populations. All three are interventional studies, but they differ in phase, size, and focus.

The RELACS trial is a Phase 4 study enrolling 332 participants with chronic subdural hematoma and atrial fibrillation. It compares early versus later resumption of oral anticoagulation, including edoxaban, after surgery for the hematoma. The primary outcome is a composite of thromboembolic events such as ischemic stroke and systemic embolism, hemorrhagic events including intracranial hemorrhage and major extracranial bleeding, and vascular death.^[3]

A low-intervention study is evaluating a single measurement and adjustment strategy based on DOAC levels in 2,000 frail older patients with atrial fibrillation or venous thromboembolism. The primary endpoint is the composite outcome of thromboembolic events or bleedings, with bleeding defined as major bleeding or clinically relevant non-major bleeding according to the International Society on Thrombosis and Haemostasis (ISTH). Thromboembolic events include ischemic stroke, transient ischemic attack, and peripheral thromboembolism.^[1]

The PEACE trial is a Phase 3 study enrolling 234 cancer patients with incidental subsegmental pulmonary embolism. It compares withholding anticoagulant treatment versus initiating anticoagulant treatment, including edoxaban. The primary outcome is a win ratio of a composite hierarchical endpoint including all-cause mortality, clinical pulmonary embolism verified by imaging, major bleeding, and clinically relevant non-major bleeding, both defined by ISTH criteria.^[2]

What side effects are known?

The most common side effect of edoxaban is bleeding, because the medicine reduces the blood's ability to clot.^[6] Signs of bleeding to watch for include bruising or bleeding under the skin, blood in the urine, coughing up blood, and vomiting blood or material that looks like ground coffee.^[5] The patient alert card for Lixiana states that edoxaban may increase the risk of bleeding, and that in case of clinically significant bleeding, treatment should be stopped immediately.^[5] Not everyone who takes edoxaban will experience side effects.^[6]