Pharmacokinetics of Intravenous Difelikefalin in Chinese Adult Subjects on Haemodialysis

NCT05885763 | Completed Phase 1 Results

• 2 other identifiers: KOR-CHINA-101JXHL2101166
• Study Type: interventional
• Target: 30
• Locations: 1 country
• Sites: 4

Brief Summary

This is a Phase 1, single-arm, open-label study to evaluate the safety, PK, and tolerability of a repeated (3 times weekly) dose of difelikefalin administered as IV bolus injections to adult Chinese HD subjects. Treatment period is one week and there is a safety follow-up period of 1 week.

Conditions

End Stage Renal Disease on Hemodialysis

Keywords

Difelikefalin; Pharmacokinetics

Outcome Measures

Primary Outcomes (14)

• Evaluation of the PK Profile of Difelikefalin - Cmax - Dose 1

  Cmax = Maximum (peak) observed plasma concentration

  1 week

• Evaluation of the PK Profile of Difelikefalin - Tmax - Dose 1

  Tmax = Time to reach maximum observed plasma concentration

  1 week

• Evaluation of the PK Profile of Difelikefalin - AUC0-t - Dose 1

  AUC0-t = Area under the concentration-versus-time curve (AUC) from time zero to time "t"

  1 week

• AUCinf - Dose 1

  AUCinf = AUC from time zero to infinity

  1 week

• AUCextrap(%) - Dose 1

  AUCextrap(%) = percentage of AUCinf based on extrapolation

  1 week

• t½ - Dose 1

  t½ = elimination half-life

  1 week

• Clearance - Dose 1

  Clearance = the volume of blood or plasma that can be freed of a specified constituent in a specified time by its excretion into the urine through the kidneys

  1 week

• Vz - Dose 1

  Vz = volume of distribution

  1 week

• Evaluation of the PK Profile of Difelikefalin - Cmax - Dose 3

  Cmax = Maximum (peak) observed plasma concentration

  1 week

• Evaluation of the PK Profile of Difelikefalin - Tmax - Dose 3

  Tmax = Time to reach maximum observed plasma concentration

  1 week

• Evaluation of the PK Profile of Difelikefalin - AUC0-t - Dose 3

  AUC0-t = Area under the concentration-versus-time curve (AUC) from time zero to time "t"

  1 week

• AUCinf - Dose 3

  AUCinf = AUC from time zero to infinity

  1 week

• AUCextrap(%) - Dose 3

  AUCextrap(%) = percentage of AUCinf based on extrapolation

  1 week

• t½ - Dose 3

  t½ = elimination half-life

  1 week

Study Arms (1)

1-week, single arm, open label treatment phase

EXPERIMENTAL

Drug: Difelikefalin Injection

Interventions

Difelikefalin Injection DRUG

Participants receive Difelikefalin three times a week (0,5 micrograms/kg dry body weight). Difelikefalin is administered by intravenous bolus injection into the venous line of the dialysis circuit at the end of each dialysis.

1-week, single arm, open label treatment phase

Eligibility Criteria

• Age: 18 Years - 85 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• End-stage renal disease (ESRD) subjects who have been on HD for at least 3 months before enrolment in the study and are currently on HD 3 times per week.
• Subjects with a prescription dry body weight between 40 and 100 kg, inclusive.
• If female, is not pregnant, or nursing
• If female:
• Is surgically sterile; or
• Has been amenorrhoeic for at least 1 year and is over the age of 55 years; or
• Has a negative serum pregnancy test within 7 days before first dose of investigational product, and agrees to use adequate contraceptive precautions (e.g., hormonal contraceptives, barrier with spermicide, intrauterine device, vasectomised partner, or abstinence) from the time of informed consent until 7 days after the last dose of investigational product.
• If male, agrees not to donate sperm from the first dose of investigational product administration (Day 1) until 7 days after last dosing, and agrees to use a condom with spermicide or abstain from heterosexual intercourse during the study until 7 days after the last dose of investigational product.

You may not qualify if:

• Planned or anticipated to receive a kidney transplant during the study.
• Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) greater than 2.5 × the reference upper limit of normal (ULN), or bilirubin (total) greater than 4 × the ULN at screening.
• Subjects with severe hepatic impairment (Child-Pugh Class C).
• Known history of allergic reaction to opiates such as hives. Note: Side effects related to the use of opioids such as constipation or nausea would not exclude the subjects from the study.
• Subject has known hypersensitivity to the study intervention or any component of the investigational product formulation.

Sponsors & Collaborators

• Vifor Fresenius Medical Care Renal Pharma: lead
• Tigermed Consulting Co., Ltd: collaborator

Study Sites (4)

Investigator Site 1

Beijing, China

Location

Investigator Site 2

Beijing, China

Location

Investigator Site 3

Beijing, China

Location

Investigator Site 4

Shijiazhuang, China

Location

MeSH Terms

Interventions

difelikefalin

Results Point of Contact

• Title: Milica Enoiu
• Organization: CSL Vifor

milica.enoiu@viforpharma.com

+41 58 851 82 64

Study Officials

• Milica Enoiu, PhD

  Vifor Pharma Group

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: A Single-arm, Open-label Study

Study Record Dates

• First Submitted: May 17, 2023
• First Posted: June 2, 2023
• Study Start: June 26, 2023
• Primary Completion: October 9, 2023
• Study Completion: October 9, 2023
• Last Updated: February 14, 2025
• Results First Posted: February 14, 2025

Record last verified: 2025-02

Data Sharing

• IPD Sharing: Will not share

Locations

CN (4)