Pharmacokinetics of Granule and Tablet Formulations of Deferitazole (Disodium Salt) and a Capsule Formulation of Deferitazole (Magnesium Hydroxide Salt)

Overview

The purpose of this study is to compare the pharmacokinetic profiles of deferitazole after administration of granule and tablet formulations of a deferitazole disodium salt to a capsule formulation of deferitazole magnesium hydroxide salt (reference formulation) in healthy adult subjects.

Full Title of Study: “A Phase 1, Open-label, Randomized, 3-Period, Relative Bioavailability Study Comparing the Pharmacokinetics of Granule and Tablet Formulations of Deferitazole (Disodium Salt) and a Capsule Formulation of Deferitazole (Magnesium Hydroxide Salt), Each Administered as a Single Oral Dose”

Study Type

  • Study Type: Interventional
  • Study Design
    • Allocation: Randomized
    • Intervention Model: Crossover Assignment
    • Primary Purpose: Other
    • Masking: None (Open Label)
  • Study Primary Completion Date: March 19, 2014

Interventions

  • Drug: Deferitazole (disodium salt, granule)
    • Single oral dose of 1500 mg administered on Day 1
  • Drug: Deferitazole (disodium salt, tablet)
    • Single oral dose of 1500 mg administered on Day 1
  • Drug: Deferitazole (magnesium hydroxide salt)
    • Single oral dose of 2400 mg administered on Day 1

Arms, Groups and Cohorts

  • Experimental: Deferitazole (disodium salt, granule)
  • Experimental: Deferitazole (disodium salt, tablet)
  • Experimental: Deferitazole (magnesium hydroxide salt)

Clinical Trial Outcome Measures

Primary Measures

  • Area Under the Plasma Concentration-time Curve (AUC) of Deferitazole
    • Time Frame: Up to 120 hours post-dose
    • AUC of disodium salt granule, disodium salt tablet, and magnesium hydroxide salt
  • Maximum Plasma Concentration (Cmax) of Deferitazole
    • Time Frame: Up to 120 hours post-dose
    • Cmax of disodium salt granule, disodium salt tablet, and magnesium hydroxide salt

Secondary Measures

  • Taste of Deferitazole
    • Time Frame: Immediately after dose and 5 minutes post-dose
  • Bioequivalence of Deferitazole Disodium Salt Granule Formulation With Tablet Formulation
    • Time Frame: Up to 120 hours post-dose
    • Compare the pharmacokinetic profile of granule formulation with pharmacokinetic profile of tablet formulation

Participating in This Clinical Trial

Inclusion Criteria

1. Age 18-65 years inclusive at the time of consent. 2. Must be considered "healthy". 3. Serum ferritin, hemoglobin and erythrocyte indices (packed cell volume, mean corpuscular volume and mean corpuscular hemoglobin concentration) within normal range. 4. Willingness to comply with any applicable contraceptive requirements of the protocol and is:

  • Male, or – Female of non-childbearing potential (defined as a female who is post-menopausal ) – Non-pregnant, non-lactating female – Females must be at least 90 days post partum or nulliparous. 5. Body weight equal to or greater than 60kg. 6. Ability to swallow a dose of the investigational product. Exclusion Criteria:

1. Subject has a clinically significant history or a disorder detected during the medical interview/physical examination. 2. Acute illness. 3. Oral condition:

  • Has history of oral surgery (including extractions) within 4 weeks, operative dental work within 7 days, or a presence of any clinically significant oral pathology (as determined by the investigator) including lesions, sores or inflammation which would interfere with assessments. – Has fixed retainers, orthodontic appliances, or either maxillary and/or mandibular dentures or other appliances which may interfere with swilling or tasting the formulations. – Has current or recurrent disease that could affect the mouth and interfere with the taste assessment. – Has severe gingivitis, periodontitis or rampant caries. – Has the presence of oral or peri-oral ulceration including herpetic lesions – Has elective dentistry scheduled during the study duration. 4. Subject has a history of thyroid disorder that has not been stabilized on thyroid medication or treatment. 5. History of alcohol or other substance abuse within the year. 6. A positive screen for alcohol or drugs of abuse. 7. Confirmed systolic blood pressure >139mmHg or <89mmHg, and diastolic blood pressure >89mmHg or<49mmHg. 8. Routine consumption of more than 2 units of caffeine per day or subjects who experience caffeine withdrawal headaches. 9. Male subjects who consume more than 3 units of alcohol per day. Female subjects who consume more than 2 units of alcohol per day. 10. A positive human immunodeficiency virus antibody screen, hepatitis B surface antigen, or hepatitis C virus antibody. 11. Current use of any other medication (including over-the-counter, herbal, or homeopathic preparations) 12. Current use of iron supplements and/or multivitamins. 13. Use of tobacco in any form (e.g., smoking or chewing) or other nicotine-containing products. 14. Donation of blood or blood products (e.g., plasma or platelets) within 60 days.

Gender Eligibility: All

Minimum Age: 18 Years

Maximum Age: 65 Years

Are Healthy Volunteers Accepted: Accepts Healthy Volunteers

Investigator Details

  • Lead Sponsor
    • Shire
  • Provider of Information About this Clinical Study
    • Sponsor
  • Overall Official(s)
    • Study Director, Study Director, Takeda

Clinical trials entries are delivered from the US National Institutes of Health and are not reviewed separately by this site. Please see the identifier information above for retrieving further details from the government database.

At TrialBulletin.com, we keep tabs on over 200,000 clinical trials in the US and abroad, using medical data supplied directly by the US National Institutes of Health. Please see the About and Contact page for details.