Exploratory Pharmacokinetic and Bioavailability Study of 2 Capsule Formulations of Torezolid Phosphate

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: TR-701 di-sodium phosphate salt; Drug: TR-701 free acid phosphate

• Registration Number: NCT00876655
• Lead Sponsor: Trius Therapeutics LLC, a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA)

Brief Summary

The purpose of this study is to evaluate the safety, tolerability, and pharmacokinetics (PK) of 2 different TR-701 oral formulations (free acid phosphate powder in capsule and di-sodium phosphate salt formulated capsule) after single doses in normal healthy adult subjects and to assess the relative bioavailability of TR-701 free acid phosphate powder in capsule formulation compared to di-sodium phosphate salt formulated capsule.

Detailed Description

Subjects will receive the following treatments in a crossover design:

Treatment A (Reference): One 200 mg capsule of TR-701 di-sodium phosphate salt (equivalent to 150 mg TR-700) administered orally after at least an 8-hour fast with 240 mL room temperature water;

Treatment B (Test): One 182 mg capsule of TR-701 free acid phosphate (equivalent to 150 mg TR-700) administered orally after at least an 8-hour fast with 240 mL room temperature water;

Descriptive statistics will be calculated for PK parameters including Cmax, Tmax, AUC0-t, and AUC0-inf.

Study Timeline

• Study Start: 2009-02
• Primary Completion: 2009-03
• Study Completion: 2009-03
• Study First Submitted: 2009-04-03
• Study First Submitted QC: 2009-04-06
• Study First Posted: 2009-04-07
• Status Verified: 2016-05
• Last Update Submitted: 2016-05-02
• Last Update Posted: 2016-05-03

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 12

Inclusion Criteria

• In good health, determined by no clinically significant findings from medical history, physical examination, 12-lead ECG, and vital signs;
• Females will be non-pregnant, non-lactating, and either postmenopausal for at least 1 year, surgically sterile for at least 90 days, or agree to use an acceptable form of contraception
• BMI of 18.5 to 32.0 kg/m2, inclusive

Exclusion Criteria

• Significant history or clinical manifestation of any significant metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder
• History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance
• Pregnancy, lactation, or breastfeeding

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
di-sodium phosphate salt	TR-701 di-sodium phosphate salt	One 200 mg capsule of TR-701 di-sodium phosphate salt (equivalent to 150 mg TR-700)
free acid	TR-701 free acid phosphate	TR-701 free acid phosphate powder in capsule formulation (equivalent to 150 mg TR-700)

Primary Outcome Measures

Name	Time	Method
To evaluate the pharmacokinetics and relative bioavailability of TR-701 free acid phosphate powder in capsule formulation compared to di-sodium phosphate salt formulated capsule after single doses in normal healthy adult subjects	4 days

Secondary Outcome Measures

Name	Time	Method
To determine the safety and tolerability of 2 different TR-701 oral formulations (free acid phosphate powder in capsule and di-sodium phosphate salt formulated capsule) after single doses in normal healthy adult	4 days

Trial Locations

Locations (1)

Covance Clinical Research Unit; 🇺🇸 Austin, Texas, United States