A Clinical Trial to Evaluate the Effect of Grapefruit Juice on the PK/PD of Edoxaban

NCT07113054 | Active Not Recruiting Phase 1

• 1 other identifier: EG-DDI
• Study Type: interventional
• Target: 14
• Locations: 1 country
• Sites: 1

Brief Summary

The aim of the study is to evaluate the effect of grapefruit juice on the pharmacokinetics and pharmacodynamics of edoxaban in healthy adults

Conditions

Healthy

Keywords

Grapefruit Juice; Edoxaban

Outcome Measures

Primary Outcomes (5)

• Cmax

  maximum concentration

  24 hours post-dose

• AUCinf

  Area under the concentration-time curve from time of administration extrapolated to infinity

  24 hours post-dose

• PT

  prothrombin time

  24 hours post-dose

• aPTT

  activated partial thromboplastin time

  24 hours post-dose

• TGA

  Thrombin generation assay

  24 hours post-dose

Study Arms (1)

Edoxaban and Grapefruit Juice

EXPERIMENTAL

* Period 1: Single dose of edoxaban 60 mg administered alone * Period 2: Single dose of edoxaban 60 mg coadministered with grapefruit juice 3 times daily for 3 days

Drug: Edoxaban 60 MG [Lixiana]; Other: Edoxaban 60 MG [Lixiana] + Grapefruit Juice

Interventions

Edoxaban 60 MG [Lixiana] DRUG

Single administration of edoxaban

Edoxaban and Grapefruit Juice

Edoxaban 60 MG [Lixiana] + Grapefruit Juice OTHER

Coadministration of edoxaban and grapefruit juice

Edoxaban and Grapefruit Juice

Eligibility Criteria

• Age: 19 Years - 50 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Adults aged 19 to 50 years of age (inclusive) at the time of screening
• Subjects with BMI of 18 to 32 kg/m2 (inclusive)
• Subjects who agree to use medically acceptable methods of contraception and not to donate sperm or oocyte
• Subjects who voluntarily decided to participate in the study and provided written consent to comply with the protocol

You may not qualify if:

• Subjects with current or history of clinically significant cardiovascular, respiratory, hepatic, renal, hematological, gastrointestinal, endocrine, immunological, dermatological, or neuropsychiatric disease
• Subjects with current or history of clinically significant hypersensitivity reactions or hypersensitivity reactions to the components or constituents of the investigational product
• Subjects who have clinically significant hemorrhage or increased risk of hemorrhage due to the following conditions A. Recent history of gastrointesinal ulcers B. Malignant tumor with a high risk of bleeding C. Recent brain or spinal cord injury D. Recent brain, spinal cord, or opthalmic surgery E. Recent history of intracranial or intracerebral hemorrhage F. Esophageal varices, arterial malformations, vascular aneurysms, or spinal cord or cerebral vascular abnormalities G. Coagulation disorders, thrombocytopenia, or platelet dysfunction H. Recent biopsy or major trauma I. Bacterial endocarditis J. Esophagitis, Gastritis, or Gastroesophageal reflux
• Subjects with a history of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption
• Subjects whose eGFR calculated by the CKD-EPI formula is 80mL/min or less at Screening
• Subjects whose AST or ALT levels are more than 2 times the upper limit of normal range, or total bilirubin levels are more than 1.5 times the upper limit of normal range at screening
• Subjects whose coagulation test (aPTT, PT) exceeds the normal range at screening
• Subjects who have taken the following medication or medication known to have significant drug interactions with the investigational product within the 2 weeks prior to the first administration day A. Strong P-gp inhibitor or inducer B. Acetylsalicylic acid, antiplatelet agent, anticoagulant, fibrinolytic agent, non-steroidal anti-inflammatory drug (NSAID), selective serotonin reuptake inhibitor (SSRI), or selective serotonin-norepinephrine reuptake inhibitor (SNRI)
• Subjects who donated whole blood within 60 days or blood components within 30 days, or received blood transfusion within 30 days prior to the first administration day
• Subjects who participated and have been exposed to an investigational product in other clinical study within 180 days prior to the first administration day
• Subjects who consistently consumed alcohol (alcohol 21 units/week \[1 unit = 10 g of pure alcohol\]) within 2 weeks of the first administration day
• Subjects who consumed grapefruit or grapefruit juice within 2 weeks of the first administration day
• Pregnant or breastfeeding women
• Subjects judged unsuitable to participate in the clinical study by investigators due to other reasons, including the results of laboratory tests

Sponsors & Collaborators

• Hyewon Chung: lead

Study Sites (1)

Korea University Guro Hospital

Seoul, Seoul, 08308, South Korea

Location

Related Publications (5)

• Mendell J, Zahir H, Matsushima N, Noveck R, Lee F, Chen S, Zhang G, Shi M. Drug-drug interaction studies of cardiovascular drugs involving P-glycoprotein, an efflux transporter, on the pharmacokinetics of edoxaban, an oral factor Xa inhibitor. Am J Cardiovasc Drugs. 2013 Oct;13(5):331-42. doi: 10.1007/s40256-013-0029-0.

  PMID: 23784266 BACKGROUND

• Ogata K, Mendell-Harary J, Tachibana M, Masumoto H, Oguma T, Kojima M, Kunitada S. Clinical safety, tolerability, pharmacokinetics, and pharmacodynamics of the novel factor Xa inhibitor edoxaban in healthy volunteers. J Clin Pharmacol. 2010 Jul;50(7):743-53. doi: 10.1177/0091270009351883. Epub 2010 Jan 15.

  PMID: 20081065 BACKGROUND

• Liu L, Li X, Liu Y, Xu B, Li Y, Yuan F, Zhang P, Tu S, Hu W. Bioequivalence and Pharmacokinetic Study of 2 Edoxaban Tablets in Healthy Chinese Subjects. Clin Pharmacol Drug Dev. 2022 Dec;11(12):1440-1446. doi: 10.1002/cpdd.1156. Epub 2022 Aug 11.

  PMID: 35950601 BACKGROUND

• Wang EJ, Casciano CN, Clement RP, Johnson WW. Inhibition of P-glycoprotein transport function by grapefruit juice psoralen. Pharm Res. 2001 Apr;18(4):432-8. doi: 10.1023/a:1011089924099.

  PMID: 11451028 BACKGROUND

• Mikkaichi T, Yoshigae Y, Masumoto H, Imaoka T, Rozehnal V, Fischer T, Okudaira N, Izumi T. Edoxaban transport via P-glycoprotein is a key factor for the drug's disposition. Drug Metab Dispos. 2014 Apr;42(4):520-8. doi: 10.1124/dmd.113.054866. Epub 2014 Jan 23.

  PMID: 24459178 BACKGROUND

MeSH Terms

Interventions

edoxaban

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: HEALTH SERVICES RESEARCH
• Intervention Model: SINGLE GROUP
• Sponsor Type: OTHER
• Responsible Party: SPONSOR INVESTIGATOR
• PI Title: Assistant Professor

Study Record Dates

• First Submitted: August 1, 2025
• First Posted: August 8, 2025
• Study Start: September 2, 2025
• Primary Completion: September 24, 2025
• Study Completion: October 1, 2025
• Last Updated: September 16, 2025

Record last verified: 2025-09

Locations

KR (1)