PEPI-TiDP23-C103: First-in-Human Study to Examine the Safety, Tolerability, and Plasma Pharmacokinetics of Increasing Single and Repeated Oral Doses of TMC558445 and of a Combined Single Day Dosing of Oral TMC558445 and Oral TMC310911 and Also Oral

• Status: Completed
• Trial end date: 2009-10-01
• Target enrollment: 0
• Participant gender: All

Summary

The purpose of the study is to determine the safety, tolerability and plasma pharmacokinetics (pk) (i.e., the levels of TMC558445 circulating in your blood over time) of increasing single oral doses of TMC558445 and of multiple increasing oral doses followed by a single dose of TMC310911 to assess the potential boosting effect on the latter compound. In this study, two investigational new drugs are involved, TMC558445 and TMC310911.

The study has been amended as follows:

TMC558445 will be administered either twice a day (b.i.d.) or once daily (q.d.). A single 300 mg or 600 mg dose of TMC310911 will be administered under fasted or fed conditions. The boosting effect on Darunavir will be investigated.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: Tibotec Pharmaceuticals, Ireland
• Treatments: Darunavir; TMC-310911

Criteria

Inclusion Criteria:

• Nonsmokers for at least 3 months prior to selection

• Weight as defined by a Body Mass Index (BMI, weight in kg divided by the square of height in meters) of 18.0 to 30.0 kg/m2, extremes included

• Informed Consent Form (ICF) signed voluntarily

• Able to comply with protocol requirements

• Healthy on the basis of a pretrial physical examination, medical history, the results of blood biochemistry and hematology tests, a urinalysis, vital signs, and a 12-lead electrocardiogram (ECG)

Exclusion Criteria:

• Past history of clinically significant heart arrhythmias (extrasystoli, tachycardia at rest)

• Having baseline prolongation of QTc interval > 450 ms, history of risk factors for Torsade de Pointes syndrome (hypokalemia, family history of long QT Syndrome)

• Female, except if postmenopausal for more than 2 years, or post-hysterectomy or post-surgical sterilization (without reversal operation)

• Currently active clinically relevant or significant underlying gastrointestinal, cardiovascular, nervous system, psychiatric, metabolic, renal, hepatic, respiratory, inflammatory, or infectious disease

• History of clinically relevant skin disease or allergy including drug allergy as well