Pilot Study of the Pharmacokinetic Profile of Deferiprone Sustained-Release Formulation in Healthy Volunteers

NCT02189941 | Completed Phase 1 Results

• 1 other identifier: LA43-0114
• Study Type: interventional
• Target: 11
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study was to evaluate the pharmacokinetic and safety profile of the sustained-release formulation of deferiprone under both fasting and fed conditions, and evaluate the relative bioavailability of this sustained-release formulation when compared to immediate-release formulation of deferiprone under fasting conditions.

Conditions

Healthy

Keywords

Deferiprone; Deferiprone sustained-release tablets; Pharmacokinetics

Outcome Measures

Primary Outcomes (5)

• AUCt for Serum Deferiprone and Deferiprone 3-O-glucuronide

  AUCt (Area Under the Curve to the last measured time) was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite. Blood samples were obtained prior to dosing and at 0.25, 0.5, 0.75, 1, 1.3333, 1.6667, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16 and 24 hours post-dose.

  24-hour interval

• AUCinf for Serum Deferiprone and Deferiprone 3-O-glucuronide

  AUCinf (Area Under the Curve to infinity) was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite. Blood samples were obtained prior to dosing and at 0.25, 0.5, 0.75, 1, 1.3333, 1.6667, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16 and 24 hours post-dose.

  24-hour interval

• Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

  Cmax (maximum concentration in the serum) was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite. Blood samples were obtained prior to dosing and at 0.25, 0.5, 0.75, 1, 1.3333, 1.6667, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16 and 24 hours post-dose.

  24-hour interval

• Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide

  Tmax (the time to Cmax) was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite. Blood samples were obtained prior to dosing and at 0.25, 0.5, 0.75, 1, 1.3333, 1.6667, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16 and 24 hours post-dose.

  24-hour interval

• Thalf for Serum Deferiprone and Deferiprone 3-O-glucuronide

  Thalf (the apparent terminal elimination half-life of the drug) was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite. Blood samples were obtained prior to dosing and at 0.25, 0.5, 0.75, 1, 1.3333, 1.6667, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16 and 24 hours post-dose.

  24-hour interval

Secondary Outcomes (1)

• Safety and Tolerability of Deferiprone Sustained Release Tablets

  From time of dose until 24 hours post dose

Study Arms (3)

Deferiprone sustained-release (fed)

EXPERIMENTAL

A single 1000 mg dose of deferiprone sustained-release following a high fat high calorie breakfast.

Drug: Deferiprone sustained-release

Deferiprone sustained-release (fasting)

EXPERIMENTAL

A single 1000 mg dose of deferiprone sustained-release under fasting conditions.

Drug: Deferiprone sustained-release

Deferiprone immediate-release (fasting)

ACTIVE COMPARATOR

A single 1000 mg dose of Deferiprone immediate-release under fasting conditions.

Drug: Deferiprone immediate-release

Interventions

Deferiprone sustained-release DRUG

Deferiprone sustained-release tablets

Also known as: Deferiprone

Deferiprone sustained-release (fasting); Deferiprone sustained-release (fed)

Deferiprone immediate-release DRUG

Deferiprone immediate-release tablets

Also known as: Ferriprox

Deferiprone immediate-release (fasting)

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Meeting the age, body mass index (BMI) and weight requirements.
• Signing the Informed Consent Form.
• Acceptable alcohol and/or drug screen at check-in of each period.
• Acceptable health, blood pressure, pulse rate and temperature at check-in.
• Being a non-smoker.
• Female subjects of childbearing potential should be either sexually inactive (abstinent) for 60 days prior to the first dose of the study and throughout the study, and for 30 days after completion of the study, or be using an acceptable method of birth control.

You may not qualify if:

• A history of presence of significant asthma, chronic bronchitis, seizure, diabetes, migraine, hypertension, cardiovascular, pulmonary, neurological conditions, psychiatric conditions, hepatic, renal, hematopoietic or gastrointestinal diseases or ongoing infectious diseases, or any other significant abnormality as evidenced by a medical history and physical examination.
• Blood chemistry, hematology, international normalized ratio, partial thromboplastin time and urinalysis values outside clinically acceptable limits.
• A positive screen for Hepatitis B surface antigens, Hepatitis C antibodies or HIV.
• Significant abnormality found on ECG.
• Known sensitivity to deferiprone or any components of the Ferriprox tablets.
• Requiring other medication at the time of the study. Oral, injectable or topical contraceptives, and contraceptive implants are permitted as they are acceptable methods of contraception.
• Acetaminophen use within 2 weeks prior to dosing and for the duration of the study.
• History of drug or alcohol abuse within the last 6 months.
• Any known enzyme inducing or inhibiting drug taken within 30 days before the study.
• History of long QT syndrome, cardiac arrhythmias.
• Infection within two weeks prior to dosing.
• Participation in an investigational drug study within 30 days prior to first dosing in this study.
• Blood donation of 50 mL to 499 mL of whole blood within 30 days, or more than 499 mL of whole blood within 56 days prior to drug administration.
• Positive test for pregnancy at medical screening or prior to dosing in either period.
• Female subjects who are breast-feeding.

Sponsors & Collaborators

• ApoPharma: lead

Study Sites (1)

Apotex Inc. BioClinical Development

Toronto, Ontario, M9L 1P7, Canada

Location

MeSH Terms

Interventions

Deferiprone

Intervention Hierarchy (Ancestors)

Pyridones; Pyridines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Results Point of Contact

• Title: Fernando Tricta, MD
• Organization: ApoPharma Inc.

ftricta@apopharma.com

416-401-7332

Study Officials

• Gurinder Rai, MD

  Apotex Inc.

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: Yes

Study Design

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

Study Record Dates

• First Submitted: July 11, 2014
• First Posted: July 15, 2014
• Study Start: May 1, 2014
• Primary Completion: June 1, 2014
• Study Completion: June 1, 2014
• Last Updated: May 20, 2016
• Results First Posted: May 20, 2016

Record last verified: 2016-04

Locations

CA (1)