Comparison of Deferiprone Delayed Release Tablets and Deferiprone Oral Solution in Healthy Volunteers

ApoPharma

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Deferiprone oral solution; Drug: Deferiprone delayed release tablet formulation

Study type: Interventional

Funder types: Industry

Identifiers

NCT02442310

LA46-0114

Details and patient eligibility

About

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

Full description

This is a single-center, open-label, randomized, 4-period crossover study of the pharmacokinetics of a new formulation of deferiprone, delayed release tablets in twenty healthy volunteers. In each study period, blood samples for pharmacokinetics assessment will be collected pre-dose and over 24 hours post-dose. Safety will be assessed throughout the study.

Enrollment: 20 patients

Sex: All

Ages: 18 to 49 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

1. Male or female aged ≥18 to <50 years
2. 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
3. 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
4. Body mass index (BMI) greater than or equal to 18.5 kg/m^2 and below 30.0 kg/m^2
5. Non- or ex smoker
6. Clinical laboratory values within the laboratory's stated normal range; if not within this range, an abnormal value must be without any clinical significance
7. 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)

Exclusion criteria

1. Pregnant or breastfeeding
2. Absolute neutrophil count (ANC) < 1.8 x 109/L at screening (no repeat can be performed)
3. 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
4. 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
5. Presence of significant cardiovascular, pulmonary, hematologic, neurological, psychiatric, endocrine, immunologic or dermatologic disease
6. 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
7. 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)
8. Any clinically significant illness in the previous 28 days before Day 1 of this study
9. Serum ferritin value below the normal limit of the reference laboratory at screening
10. Positive urine screening of alcohol and/or drugs of abuse
11. Positive results to HIV Ag/Ab Combo, Hepatitis B surface Antigen (HBsAG (B) (hepatitis B)) or anti-Hepatitis C Virus (HCV (C)) tests

Trial design

20 participants in 4 patient groups

Delayed release, fed conditions

Experimental group

Description:

A single 1200 mg dose of deferiprone delayed release tablet formulation administered following a high-fat breakfast

Treatment:

Drug: Deferiprone delayed release tablet formulation

Delayed release, fasting conditions

Experimental group

Description:

A single 1200 mg dose of deferiprone delayed release tablet formulation, administered following a 10-hour fast

Treatment:

Drug: Deferiprone delayed release tablet formulation

Delayed release half-tablets

Experimental group

Description:

A single 1200 mg dose of deferiprone delayed release tablet formulation, following a high-fat breakfast

Treatment:

Drug: Deferiprone delayed release tablet formulation

Oral solution, fasting conditions

Active Comparator group

Description:

A single 1200 mg dose of deferiprone oral solution, administered following a 10-hour fast

Treatment:

Drug: Deferiprone oral solution