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

An Open-Label, Randomized, Single-Dose, 2-Treatment, 2-Sequence, Crossover, Exploratory Pharmacokinetic and Bioavailability Study of 2 Capsule Formulations of TR-701 (Torezolid Phosphate) in Normal Healthy Adults

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: TR-701 free acid phosphate; Drug: TR-701 di-sodium phosphate salt

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 Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • Austin, Texas, United States, 78752
      • Covance Clinical Research Unit

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 60 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: free acid; TR-701 free acid phosphate powder in capsule formulation (equivalent to 150 mg TR-700)	Drug: TR-701 free acid phosphate; One 182 mg capsule of TR-701 free acid phosphate (equivalent to 150 mg TR-700)
Experimental: di-sodium phosphate salt; One 200 mg capsule of TR-701 di-sodium phosphate salt (equivalent to 150 mg TR-700)	Drug: TR-701 di-sodium phosphate salt; One 200 mg capsule of TR-701 di-sodium phosphate salt (equivalent to 150 mg TR-700)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
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

Outcome Measure	Time Frame
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

Collaborators and Investigators

• Sponsor: Trius Therapeutics LLC
• Investigators: Principal Investigator: David C Carter, MD, Covance CRU

Publications and helpful links

General Publications

• Flanagan SD, Bien PA, Munoz KA, Minassian SL, Prokocimer PG. Pharmacokinetics of tedizolid following oral administration: single and multiple dose, effect of food, and comparison of two solid forms of the prodrug. Pharmacotherapy. 2014 Mar;34(3):240-50. doi: 10.1002/phar.1337. Epub 2013 Aug 7.

Study record dates

Study Major Dates

• Study Start: February 1, 2009
• Primary Completion (Actual): March 1, 2009
• Study Completion (Actual): March 1, 2009

Study Registration Dates

• First Submitted: April 3, 2009
• First Submitted That Met QC Criteria: April 6, 2009
• First Posted (Estimate): April 7, 2009

Study Record Updates

• Last Update Posted (Estimate): May 3, 2016
• Last Update Submitted That Met QC Criteria: May 2, 2016
• Last Verified: May 1, 2016

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Anti-Infective Agents; Anti-Bacterial Agents; Tedizolid phosphate
• Other Study ID Numbers: 1986-025; TR701-108 (Other Identifier: TriusRX Unique ID)