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.

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.

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