Comparison of Deferiprone Extended Release Tablets and Ferriprox Immediate Release Tablets in Healthy Volunteers

NCT02465489 | Completed Phase 1 Results

• 1 other identifier: LA51-0115
• Study Type: interventional
• Target: 20
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to look at the pharmacokinetics of a new formulation of deferiprone (deferiprone extended release tablets) under fed and fasting conditions.

Conditions

Healthy

Keywords

deferiprone; deferiprone extended release formulation; pharmacokinetics

Outcome Measures

Primary Outcomes (3)

• Cmax for Serum Deferiprone

  Maximum measured serum concentration. Blood samples will be collected pre-dose and over a 24-hour interval post-dose

  Samples were collected pre-dose and at 0.25, 0.5, 0.75, 1.0, 1.33, 1.66, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 8.0, 12.0, 16.0, and 24.0 hours post-dose.

• Tmax for Serum Deferiprone

  Time of maximum observed serum concentration. Blood samples will be collected pre-dose and over a 24-hour interval post-dose

  Samples were collected pre-dose and at 0.25, 0.5, 0.75, 1.0, 1.33, 1.66, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 8.0, 12.0, 16.0, and 24.0 hours post-dose.

• AUC0-∞for Serum Deferiprone

  Area under the serum concentration time curve extrapolated to infinity. Blood samples will be collected pre-dose and over a 24-hour interval post-dose.

  Samples were collected pre-dose and at 0.25, 0.5, 0.75, 1.0, 1.33, 1.66, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 8.0, 12.0, 16.0, and 24.0 hours post-dose.

Secondary Outcomes (1)

• Number of Subjects With Adverse Events (AEs)

  Throughout the trial, from the time of the first dose until the last study visit (Day 36 or early termination)

Study Arms (5)

ER, fasting conditions

EXPERIMENTAL

A single 1000 mg dose of deferiprone extended release tablet formulation administered under fasting conditions

Drug: Deferiprone extended release

ER, fed conditions

EXPERIMENTAL

A single 1000 mg dose of deferiprone extended release tablet formulation administered under fed conditions

Drug: Deferiprone extended release

ER half-tablets, fed conditions

EXPERIMENTAL

A single 1000 mg dose of deferiprone extended release tablet formulation (one 1000 mg tablet divided in two) administered under fed conditions

Drug: Deferiprone extended release

IR, fasting conditions

ACTIVE COMPARATOR

A single 1000 mg dose of deferiprone immediate release tablet formulation administered under fasting conditions

Drug: Deferiprone immediate release

IR, fed conditions

ACTIVE COMPARATOR

A single 1000 mg dose of deferiprone immediate release tablet formulation administered under fed conditions

Drug: Deferiprone immediate release

Interventions

Deferiprone extended release DRUG

Deferiprone 1000 mg extended release tablet formulation

Also known as: Deferiprone extended release tablet formulation

ER half-tablets, fed conditions; ER, fasting conditions; ER, fed conditions

Deferiprone immediate release DRUG

Ferriprox (deferiprone) 500 mg immediate release tablet formulation

Also known as: Ferriprox immediate release tablet formulation

IR, fasting conditions; IR, fed conditions

Eligibility Criteria

• Age: 18 Years - 49 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male or female aged ≥18 to \<50 years
• A female volunteer of childbearing potential must agree to use an accepted contraceptive regimen from at least 28 days prior to the first administration of the study drug until at least 30 days after the last dose of the study drug
• A sexually active male must agree that he and/or his female partner will use a medically acceptable method of contraception throughout the study and for at least 30 days following drug administration
• Body mass index (BMI) greater than or equal to 18.5 kg/m\^2 and below 30.0 kg/m\^2
• Body weight of at least 60 kg
• Non- or ex smoker
• Clinical laboratory values within the laboratory's stated normal range; if not within this range, an abnormal value must be without any clinical significance
• Have no clinically significant diseases captured in the medical history, or evidence of clinically significant findings on physical examination and/or clinical laboratory evaluations (hematology, general biochemistry, coagulation, ECG, and urinalysis)

You may not qualify if:

• Pregnant or breastfeeding
• Absolute neutrophil count (ANC) \< 1.8 x 109/L at screening (no repeat can be performed)
• History of significant hypersensitivity to deferiprone or any related products (including excipients of the formulations) as well as severe hypersensitivity reactions (such as angioedema) to any drugs
• History or presence of gastrointestinal, liver or kidney disease, or any other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs or known to potentiate or predispose to undesired effects
• Presence of significant cardiovascular, pulmonary, hematologic, neurological, psychiatric, endocrine, immunologic or dermatologic disease
• Suicidal tendency, history of seizures, history of head trauma with coma or craniotomy/trepanation, state of confusion, or clinically relevant psychiatric diseases
• Presence of out-of-range cardiac interval (PR \< 110 msec, PR \> 220 msec, QRS \< 60 msec, QRS \>119 msec and QTcF \> 450 msec for males and \> 460 msec for females) on the screening ECG or other clinically significant ECG abnormalities
• Maintenance therapy with any drug or significant history of drug dependency or alcohol abuse (\> 3 units of alcohol per day, intake of excessive alcohol, acute or chronic)
• Any clinically significant illness in the previous 28 days before Day 1 of this study
• Use of any enzyme-modifying drugs, including strong inhibitors of cytochrome P450 (CYP) enzymes (such as cimetidine, fluoxetine, quinidine, erythromycin, ciprofloxacin, fluconazole, ketoconazole, diltiazem and HIV antivirals) and strong inducers of CYP enzymes (such as barbiturates, carbamazepine, glucocorticoids, phenytoin, rifampin and St John's Wort), in the previous 28 days before Day 1 of this study
• Any history of tuberculosis and/or prophylaxis for tuberculosis
• Serum ferritin value below the normal limit of the reference laboratory at screening
• Positive urine screening of alcohol and/or drugs of abuse
• Positive results on HIV Ag/Ab Combo, Hepatitis B surface Antigen (HBsAG (B) (hepatitis B)) or anti-Hepatitis C Virus (HCV (C)) tests
• Positive result on a serum pregnancy test

Sponsors & Collaborators

• ApoPharma: lead

Study Sites (1)

Algorithme Pharma Inc.

Mount Royal, Quebec, H3P 3P1, Canada

Location

MeSH Terms

Interventions

Deferiprone

Intervention Hierarchy (Ancestors)

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

Results Point of Contact

• Title: Caroline Fradette, PhD
• Organization: ApoPharma Inc.

cfradett@apopharma.com

416-401-7543

Study Officials

• Eric Sicard, MD

  Algorithme Pharma Inc

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

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

Study Record Dates

• First Submitted: June 4, 2015
• First Posted: June 8, 2015
• Study Start: June 1, 2015
• Primary Completion: August 1, 2015
• Study Completion: August 1, 2015
• Last Updated: February 26, 2016
• Results First Posted: January 26, 2016

Record last verified: 2015-06

Locations

CA (1)