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

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
 
ClinicalTrials.gov Identifier: NCT02189941
Recruitment Status : Completed
First Posted : July 15, 2014
Results First Posted : May 20, 2016
Last Update Posted : May 20, 2016
Sponsor:
Information provided by (Responsible Party):
ApoPharma

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.

Condition or disease Intervention/treatment Phase
Healthy Drug: Deferiprone sustained-release Drug: Deferiprone immediate-release Phase 1

Detailed Description:

This was an open-label, single-dose, randomized, three-way crossover study under fed and fasting conditions designed to determine the pharmacokinetics, safety, and tolerability of deferiprone sustained-release tablets in healthy volunteers. Subjects were randomized to receive the following 3 treatments in different orders, with a washout period of 7 days between treatments:

  • 2000 mg of deferiprone sustained-release tablets under fed conditions
  • 2000 mg of deferiprone sustained-release tablets under fasted conditions
  • 2000 mg of Ferriprox immediate-release tablets under fasted conditions

In each period, blood samples for pharmacokinetics (PK) assessment were collected prior to dosing and at specified time points up to 24 hours post-dose. Safety assessments were conducted throughout the study.

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Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 11 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: Pilot Study of the Pharmacokinetic Profile of a Single Dose of Deferiprone Sustained-Release Formulation in Healthy Volunteers
Study Start Date : May 2014
Actual Primary Completion Date : June 2014
Actual Study Completion Date : June 2014

Resource links provided by the National Library of Medicine

Drug Information available for: Deferiprone

Arm Intervention/treatment
Experimental: Deferiprone sustained-release (fed)
A single 1000 mg dose of deferiprone sustained-release following a high fat high calorie breakfast.
Drug: Deferiprone sustained-release
Deferiprone sustained-release tablets
Other Name: Deferiprone

Experimental: Deferiprone sustained-release (fasting)
A single 1000 mg dose of deferiprone sustained-release under fasting conditions.
Drug: Deferiprone sustained-release
Deferiprone sustained-release tablets
Other Name: Deferiprone

Active Comparator: Deferiprone immediate-release (fasting)
A single 1000 mg dose of Deferiprone immediate-release under fasting conditions.
Drug: Deferiprone immediate-release
Deferiprone immediate-release tablets
Other Name: Ferriprox




Primary Outcome Measures :
  1. AUCt for Serum Deferiprone and Deferiprone 3-O-glucuronide [ Time Frame: 24-hour interval ]
    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.

  2. AUCinf for Serum Deferiprone and Deferiprone 3-O-glucuronide [ Time Frame: 24-hour interval ]
    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.

  3. Cmax for Serum Deferiprone and Deferiprone 3-O-glucuronide [ Time Frame: 24-hour interval ]
    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.

  4. Tmax for Serum Deferiprone and Deferiprone 3-O-glucuronide [ Time Frame: 24-hour interval ]
    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.

  5. Thalf for Serum Deferiprone and Deferiprone 3-O-glucuronide [ Time Frame: 24-hour interval ]
    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.


Secondary Outcome Measures :
  1. Safety and Tolerability of Deferiprone Sustained Release Tablets [ Time Frame: From time of dose until 24 hours post dose ]
    The number of participants who experienced adverse events between the time of dosing up to 24 hours post-dose, including any changes of clinical significance in vital signs, 12-lead ECG, and clinical laboratory tests



Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes
Criteria

Main Inclusion Criteria:

  • 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.

Exclusion Criteria:

  • 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.
  • Absolute neutrophil count (ANC) <= 1.0 x 10E9 cells/L prior to dosing for each period.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT02189941


Locations
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Canada, Ontario
Apotex Inc. BioClinical Development
Toronto, Ontario, Canada, M9L 1P7
Sponsors and Collaborators
ApoPharma
Investigators
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Principal Investigator: Gurinder Rai, MD Apotex Inc.
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Responsible Party: ApoPharma
ClinicalTrials.gov Identifier: NCT02189941    
Other Study ID Numbers: LA43-0114
First Posted: July 15, 2014    Key Record Dates
Results First Posted: May 20, 2016
Last Update Posted: May 20, 2016
Last Verified: April 2016
Keywords provided by ApoPharma:
Deferiprone
Deferiprone sustained-release tablets
Pharmacokinetics
Additional relevant MeSH terms:
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Deferiprone
Iron Chelating Agents
Chelating Agents
Sequestering Agents
Molecular Mechanisms of Pharmacological Action