NCT03083782

Drug Interaction Study of Apixaban With Cyclosporine and Tacrolimus

A Phase I, Open-Label, Crossover, Drug Interaction Study of Apixaban With Cyclosporine and Tacrolimus in Healthy Volunteers

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 12 (actual)
• Sponsor: Thomas Jefferson University · Academic / Other
• Sex: All
• Age: 18 Years – 55 Years
• Healthy volunteers: Accepted

Summary

This study aims to evaluate the pharmacokinetics (PK) of apixaban when co-administered with cyclosporine and tacrolimus in healthy volunteers. The study participants will receive apixaban alone, cyclosporine followed by apixaban and tacrolimus followed by apixaban.

Detailed description

Life- and graft-threatening complications in solid organ transplant patients have been greatly reduced due to the potent immunosuppressive agents like calcineurin inhibitors (CNI) that include cyclosporine and tacrolimus. Venous thromboembolism (clots in legs or lungs) in transplant recipients is often difficult to manage due to polypharmacy and potential for drug interactions. More than 90% of renal transplant (RT) recipients are maintained on a CNI-based immunosuppressive regimen. Cyclosporine is an inhibitor of many metabolic pathways including cytochrome P450 (CYP) 3A4, permeability glycoprotein (P-gp) and, breast cancer resistance protein (BCRP). Tacrolimus shares some of the distributive and metabolic pathways of cyclosporine. Apixaban is a combined substrate of CYP3A4, P-gp and, BCRP and thus has the potential for drug interactions with cyclosporine and tacrolimus. Apixaban levels that are too high or too low could be a problem for transplant patients. The purpose of this study is to determine what happens to apixaban blood levels when given in combination with cyclosporine or tacrolimus.

Conditions

• Venous Thromboembolism
• Pharmacokinetics
• Healthy

Interventions

Type	Name	Description
DRUG	Apixaban alone	A single dose of 10 mg apixaban administered orally at 0H on Day 1.
DRUG	Cyclosporine	Once daily dose of 100 mg cyclosporine administered orally on Days 1 to 3.
DRUG	Tacrolimus	Once daily dose of 5 mg tacrolimus administered orally on Days 1 to 3.
DRUG	Apixaban	A single dose of 10 mg apixaban administered orally on Day 3 immediately following cyclosporine
DRUG	Apixaban	A single dose of 10 mg apixaban administered orally on Day 3 immediately following tacrolimus

Timeline

• Start date: 2017-04-18
• Primary completion: 2017-06-05
• Completion: 2017-06-30
• First posted: 2017-03-20
• Last updated: 2017-10-11

Locations

1 site across 1 country: United States

Regulatory

• FDA-regulated drug study