Innovation-TiFP4-C101: A Study to Evaluate the Pharmacokinetics of TMC114 and TMC41629 After a Single Oral Dose of 2 Controlled-release Coformulations as Compared to an Immediate-release Coformulation of TMC114/TMC41629 - Full Text View

Purpose

The purpose of this study is to compare the bioavailability (the degree to which a drug becomes available in the body after administration) of 3 different pharmaceutical preparations of a combination of two drugs, TMC114 and TMC41629. There will be 1 single oral intake (intake by mouth) of each of the 3 preparations. The study will also investigate the safety of use and the potential side effects of TMC114 and TMC41629, and determine the circulating levels of both compounds in your blood over time (pharmacokinetics), after a single intake.

Condition	Intervention	Phase
HIV-I	Drug: TMC114; TMC41629	Phase 1


Study Type:	Interventional
Study Design:	Allocation: Randomized Endpoint Classification: Pharmacokinetics Study Intervention Model: Crossover Assignment Masking: Open Label Primary Purpose: Treatment
Official Title:	Phase I, Open-label, 3-way Crossover Trial in Healthy Male Volunteers to Evaluate the Pharmacokinetics of TMC114 and TMC41629 After a Single Oral Dose of 2 Controlled-release Coformulations as Compared to an Immediate-release Coformulation of TMC114/TMC41629

Resource links provided by NLM:

Drug Information available for: Darunavir Darunavir ethanolate

U.S. FDA Resources

Further study details as provided by Tibotec Pharmaceuticals, Ireland:

Primary Outcome Measures:

Plasma levels of TMC114 and TMC41629 will be determined up to 72 hours after administration.

Secondary Outcome Measures:

To determine short-term safety and tolerability of TMC114/TMC41629 following administration of 3 single oral doses (formulated as different coformulations of TMC114/TMC41629).


Enrollment:	12
Study Start Date:	November 2008
Study Completion Date:	January 2009
Primary Completion Date:	January 2009 (Final data collection date for primary outcome measure)

Detailed Description:

TMC41629 is a new investigational drug for the treatment of HIV. TMC114, is also known as Darunavir. In this randomized (study medication assigned by chance), open label trial (investigator and healthy volunteer know the name of the study medication), each healthy volunteer will receive a single dose of TMC114/TMC41629, in 3 subsequent sessions, Treatment A, Treatment B and Treatment C. Each capsule is equivalent to a dose of 200 mg of TMC114 and 23.67 mg of TMC41629. Treatment A (immediate-release formulation) will serve as reference formulation. All medication intakes will be orally and in fasted conditions.The study duration is at least 19 days, excluding screening and follow-up visits with three single intakes with 72 hours follow-up per intake. Each volunteer will receive a single dose of each formulation. TMC114/TMC41629 is formulated as an oral immediate-release hard-gelatin capsule, as an oral gastro-resistant hard-gelatin capsule, enteric-coated and as an oral gastro-resistant hard-gelatin capsule, colon-targeted. Each capsule is equivalent to a dose of 200 mg of TMC114 and 23.67 mg of TMC41629.

Eligibility


Ages Eligible for Study:	18 Years to 55 Years (Adult)
Genders Eligible for Study:	Male
Accepts Healthy Volunteers:	Yes

Criteria

Inclusion Criteria:

Non-smoking for at least 3 months prior to selection
Normal 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 before the first trial-related activity
Able to comply with protocol requirements
Healthy on the basis of a medical evaluation that confirms the absence of any clinically relevant abnormality and includes a physical examination, medical history, the results of blood biochemistry, coagulation, and hematology tests, a urinalysis, vital signs, and a 12-lead electrocardiogram (ECG) (in triplicate) with the following parameters carried out at screening: a. heart rate (HR) between 40 and 100 bpm
b. QTc interval = 450 ms
c. QRS interval lower than 120 ms
d. PR interval = 220 ms.

Exclusion Criteria:

Past history of heart arrhythmias
History or evidence of current use of alcohol, barbiturate, amphetamine, recreational or narcotic drug use, which in the investigator's opinion would compromise subject's safety and/or compliance with the trial procedures
Hepatitis A, B, or C infection or HIV-1 or HIV-2 infection at screening
Currently active or underlying gastrointestinal, cardiovascular, neurologic, psychiatric, metabolic, endocrinologic, genitourinary, renal, hepatic, respiratory, inflammatory, or infectious disease
Any history of significant skin disease and allergy to drugs

Contacts and Locations

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the Contacts provided below. For general information, see Learn About Clinical Studies.

Please refer to this study by its ClinicalTrials.gov identifier: NCT00854204

Sponsors and Collaborators

Tibotec Pharmaceuticals, Ireland

Investigators


Study Director:	Tibotec Pharmaceuticals Limited Clinical Trial	Tibotec Pharmaceutical Limited

More Information


ClinicalTrials.gov Identifier:	NCT00854204 History of Changes
Other Study ID Numbers:	CR015763
Study First Received:	January 15, 2009
Last Updated:	April 26, 2010
Health Authority:	Ireland: Irish Agriculture and Food Development Authority

Keywords provided by Tibotec Pharmaceuticals, Ireland:


Innovation-TiFP4-C101 Innovation-C101 Innovation TMC114/TMC41629	controlled-release coformulations immediate-release coformulation Pharmacokinetics

Additional relevant MeSH terms:


Darunavir HIV Protease Inhibitors Protease Inhibitors Enzyme Inhibitors Molecular Mechanisms of Pharmacological Action	Anti-HIV Agents Anti-Retroviral Agents Antiviral Agents Anti-Infective Agents

ClinicalTrials.gov processed this record on September 30, 2016