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Study of Dolutegravir (DTG) on PK of Cenicriviroc (CVC), and CVC on PK of DTG & on a Single Dose of Midazolam

Phase 1
Completed
Conditions
HIV-infection/AIDS
Interventions
Registration Number
NCT01827540
Lead Sponsor
Tobira Therapeutics, Inc.
Brief Summary

To evaluate the PK, safety and tolerability of Cenicriviroc (CVC) administered with and without Dolutegravir (DTG) and CVC with and without a single dose of Midazolam in healthy subjects.

Detailed Description

Primary Objectives

* To evaluate the steady-state PK of CVC administered with and without DTG .

* To evaluate the steady-state PK of DTG administered with and without CVC .

* To evaluate the PK of a single dose of Midazolam administered with and without steady state CVC when both are administered orally.

Secondary Objectives

* To evaluate the safety and tolerability of CVC administered with and without DTG.

* To evaluate the safety and tolerability of CVC administered with and without Midazolam.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
20
Inclusion Criteria
  1. Provide written informed voluntary consent
  2. Adult male and female healthy volunteers
  3. Body mass index (BMI) ≥ 18.0 and ≤ 30.0 kg/m2.
  4. Be in good general health with no clinically relevant abnormalities
  5. Agree to comply with study procedures and restrictions
Exclusion Criteria
  1. Any disease or condition that might affect drug absorption, metabolism, or excretion, or clinically significant cardiovascular as determined by investigator
  2. History of stomach or intestinal surgery, except for fully healed appendectomy and/or cholecystectomy which will be allowed
  3. Clinically significant illness or clinically significant surgery within 4 weeks before the administration of study medication
  4. Known or suspected hypersensitivity or allergic reaction to any of the components of CVC or DTG tablets, or midazolam syrup
  5. Serum ALT, AST, or bilirubin values greater than or equal to Division of Acquired Immunodeficiency Syndrome (DAIDS) grade 1 at screening

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Dolutegravir , and DTG + CVCDolutegravirGrp 2: DTG 50 mg qd alone from Days 1-10, DTG 50 mg qd + CVC 150 mg qd from Days 11-20.
Cenicriviroc + Midazolam, and CVC + DTGMidazolamGrp 1: CVC 150mg qd alone from Days 1-10; CVC 150mg qd + DTG 50mg qd from Days 11-20. A single dose of midazolam 5mg administered alone on Day -1 \& w/ CVC 150mg on Day 9.
Cenicriviroc + Midazolam, and CVC + DTGCenicrivirocGrp 1: CVC 150mg qd alone from Days 1-10; CVC 150mg qd + DTG 50mg qd from Days 11-20. A single dose of midazolam 5mg administered alone on Day -1 \& w/ CVC 150mg on Day 9.
Cenicriviroc + Midazolam, and CVC + DTGDolutegravirGrp 1: CVC 150mg qd alone from Days 1-10; CVC 150mg qd + DTG 50mg qd from Days 11-20. A single dose of midazolam 5mg administered alone on Day -1 \& w/ CVC 150mg on Day 9.
Dolutegravir , and DTG + CVCCenicrivirocGrp 2: DTG 50 mg qd alone from Days 1-10, DTG 50 mg qd + CVC 150 mg qd from Days 11-20.
Primary Outcome Measures
NameTimeMethod
Pharmacokinetic Assessment of Cenicriviroc0 (predose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, & 24 hours postdose on Days 10 and 20

PK profile will be calculated based on CVC exposure. Trough (predose) CVC plasma samples will be obtained prior to dosing on Days 2-9 \& 12-19.

Pharmacokinetic Assessment of Dolutegravir0 (predose), 0.5, 1, 2, 3, 4, 6, 8, 10, 12, & 24 hours postdose on Days 10 and 20

PK profile will be calculated based on DTG exposure. Trough (predose) DTG plasma samples will be obtained prior to dosing on Days 2-9 \& 12-19.

Pharmacokinetic Assessment of Midazolam and alpha-hydroxymidazolam0 (predose), 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 & 18 hours postdose on Day -1 and Day 9

PK profile will be calculated (Group 1 only) based on plasma midazolam \& alpha-hydroxymidazolam exposure.

Secondary Outcome Measures
NameTimeMethod
Number of participants with adverse eventsParticipants will be followed upon taking first dose of study medication until the follow-up visit, an expected average of 5 weeks

Physical examinations, vital signs, ECGs, clinical laboratory tests, and AEs or serious AEs (SAEs) will be assessed at specified time points according to the Schedule of Procedures in the protocol. In addition, arterial oxygen saturation will be monitored by pulse oximetry for at least 2 hours after administration of midazolam on Days -1 and 9 in Group 1.

For both groups, a final follow-up visit will occur 14 days (±3 days) after the last dose of study medication, or at the time of early termination (if applicable) to evaluate any remaining safety issue(s).

Trial Locations

Locations (1)

SeaView Research, Inc.

🇺🇸

Miami, Florida, United States

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