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

Phase 1

Withdrawn

• Conditions: Healthy
• Interventions: Drug: Deferitazole (disodium salt, granule); Drug: Deferitazole (magnesium hydroxide salt); Drug: Deferitazole (disodium salt, tablet)

• Registration Number: NCT02065401
• Lead Sponsor: Shire

Brief Summary

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.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2014-02-10
• Study First Submitted QC: 2014-02-14
• Study First Posted: 2014-02-19
• Study Start: 2014-02-28
• Primary Completion: 2014-03-19
• Study Completion: 2014-03-19
• Status Verified: 2021-05
• Last Update Submitted: 2021-06-01
• Last Update Posted: 2021-06-02

Recruitment & Eligibility

• Status: WITHDRAWN
• Sex: All
• Target Recruitment: Not specified

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.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Deferitazole (disodium salt, granule)	Deferitazole (disodium salt, granule)	-
Deferitazole (magnesium hydroxide salt)	Deferitazole (magnesium hydroxide salt)	-
Deferitazole (disodium salt, tablet)	Deferitazole (disodium salt, tablet)	-

Primary Outcome Measures

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

Secondary Outcome Measures

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

Trial Locations

Locations (1)

Clinical Pharmacology of Miami; 🇺🇸 Miami, Florida, United States