A Phase I, Open-label Trial to Explore the Pharmacokinetics, Safety and Tolerability of TMC278 (Rilpivirine) 25 mg Once Daily Following a 2-week Period Receiving Efavirenz, in Healthy Male and Female Volunteers

NCT01268839 | Completed Phase 1

• 2 other identifiers: CR016984TMC278HIV1001
• Study Type: interventional
• Target: 20
• Locations: 0 countries
• Sites: N/A

Brief Summary

The purpose of this study is to investigate the pharmacokinetics of TMC278 (rilpivirine) 25 mg once daily following a preceding 2-week treatment period with efavirenz 600 mg once daily in healthy volunteers

Conditions

HIV

Keywords

TMC278, rilpivirine, efavirenz, healthy volunteer

Outcome Measures

Primary Outcomes (1)

• Pharmacokinetics of TMC278 25 mg once daily (q.d.) following a preceding 2-week treatment period with EFV 600 mg q.d., in healthy volunteers

  70-77 days

Secondary Outcomes (3)

• To evaluate the EFV inducing effect on TMC278 metabolism after EFV intake cessation, through comparison of TMC278 plasma concentrations with and without preceding EFV intake

  70-77 days

• To evaluate EFV plasma concentrations over time after cessation of EFV intake

  70-77 days

• To assess the safety (including vital signs and electrocardiogram [ECG] measurements, laboratory assessments, and incidence of overall AEs and tolerability) of TMC278 at a dose of 25 mg q.d administered alone and after switching from EFV over a period of

  70-77 days

Study Arms (1)

001

EXPERIMENTAL

Efavirenz 600mg tablet once daily for 14 days,TMC278 25mg tablet once daily for 14 days,TMC278 25mg tablet once daily for 28 days

Drug: TMC278; Drug: Efavirenz

Interventions

TMC278 DRUG

25mg tablet once daily for 28 days

001

Efavirenz DRUG

600mg tablet once daily for 14 days

001

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Non-vasectomized heterosexually active male volunteers with female partner of childbearing potential must be using a highly effective method of birth control (i.e., male condom with either female intrauterine device, diaphragm, cervical cap or hormonal based contraceptives) and must agree to use these birth control methods during the trial and until 30 days after the end of the trial
• Able to comply with all protocol requirements
• Normal resting ECG at screening including
• Volunteers must have signed an Informed Consent Form (ICF) voluntarily before the first trial-related activity indicating that they understand the purpose of and procedures required for the trial and are willing to participate in the trial
• To participate in the optional pharmacogenomic component of this trial, volunteers must have signed the ICF for pharmacogenomic research indicating willingness to participate in the pharmacogenomic component of the trial. Refusal to give consent for this component does not exclude a volunteers from participation in the clinical trial
• Healthy on the basis of a medical evaluation that confirms the absence of any clinically relevant abnormality and includes a physical examination (including skin examination), medical history, vital signs, the results of blood biochemistry and hematology tests and a urinalysis carried out at screening.

You may not qualify if:

• A positive HIV-1 or -2 test at trial screening
• Females of childbearing potential
• Hepatitis A infection (confirmed by hepatitis A antibody IgM), hepatitis B infection (confirmed by hepatitis B surface antigen), or hepatitis C infection (confirmed by hepatitis C virus antibody) diagnosed at trial screening
• Currently active clinically significant disease (e.g., pancreatitis, cardiac dysfunction) or findings during screening of medical history, laboratory or physical examination that in the investigator's opinion would compromise subject safety or the outcome of the trial
• Current or recent (within 3 months prior to the first administration of trial medication) gastrointestinal disease
• Any history of significant skin disease such as but not limited to rash or eruptions, drug allergies, food allergy, dermatitis, eczema, psoriasis, or urticaria
• A positive alcohol test or urine drug test at study screening

Sponsors & Collaborators

• Tibotec, Inc: lead
• Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA: collaborator

MeSH Terms

Interventions

Rilpivirine; efavirenz

Intervention Hierarchy (Ancestors)

Nitriles; Organic Chemicals; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Tibotec, Inc. Clinical Trial

  Tibotec, Inc

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: December 30, 2010
• First Posted: December 31, 2010
• Study Start: January 1, 2010
• Primary Completion: May 1, 2010
• Study Completion: May 1, 2010
• Last Updated: September 4, 2013

Record last verified: 2013-09