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Study Assessing the Effects of Darunavir/Ritonavir or Lopinavir/Ritonavir on the Pharmacokinetics of Daclatasvir in Healthy Participants

Phase 1
Completed
Conditions
Hepatitis C
Interventions
Registration Number
NCT02159352
Lead Sponsor
Bristol-Myers Squibb
Brief Summary

The purpose of this study is to determine whether multiple doses of darunavir/ritonavir or lopinavir/ritonavir affect the pharmacokinetics of daclatasvir in healthy participants.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
49
Inclusion Criteria
  • Healthy male and female participants, aged 18 to 49, as determined by medical history, physical examination, 12 lead electrocardiogram, vital signs, and clinical laboratory evaluations

Key

Exclusion Criteria
  • Any significant acute or chronic medical illness; donation of blood to a blood bank or in a clinical study (except a screening visit) within 4 weeks of study drug administration (within 2 weeks for plasma only); or blood screen findings positive for hepatitis C antibody, hepatitis B surface antigen, or HIV-1 and HIV-2 antibodies

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Group 2: Daclatasvir and Lopinavir/RitonavirLopinavir/RitonavirTreatment C: Daclatasvir oral tablet on specific days Treatment D: Daclatasvir tablet and Lopinavir/Ritonavir tablet orally on specific days
Group 1: Daclatasvir and Darunavir/RitonavirDaclatasvirTreatment A: Daclatasvir oral tablet on specific days Treatment B: Daclatasvir tablet and Darunavir Tablet/Ritonavir capsule orally on specific days
Group 1: Daclatasvir and Darunavir/RitonavirRitonavirTreatment A: Daclatasvir oral tablet on specific days Treatment B: Daclatasvir tablet and Darunavir Tablet/Ritonavir capsule orally on specific days
Group 2: Daclatasvir and Lopinavir/RitonavirDaclatasvirTreatment C: Daclatasvir oral tablet on specific days Treatment D: Daclatasvir tablet and Lopinavir/Ritonavir tablet orally on specific days
Group 1: Daclatasvir and Darunavir/RitonavirDarunavirTreatment A: Daclatasvir oral tablet on specific days Treatment B: Daclatasvir tablet and Darunavir Tablet/Ritonavir capsule orally on specific days
Group 2: Daclatasvir and Lopinavir/RitonavirRitonavirTreatment C: Daclatasvir oral tablet on specific days Treatment D: Daclatasvir tablet and Lopinavir/Ritonavir tablet orally on specific days
Primary Outcome Measures
NameTimeMethod
Maximum Observed Plasma Concentration (Cmax) for DaclatasvirPredose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Cmax was obtained from concentration-time plot using a noncompartmental method and a validated pharmacokinetic analysis program.

Area Under the Concentration-Time Curve in 1 Dosing Interval (AUC[TAU]) for DaclatasvirPredose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

AUC(TAU) was the area under the curve from time zero to end of dosing interval. AUC(TAU) was obtained from concentration-time plot of daclatasvir using noncompartmental method and a validated pharmacokinetic analysis program.

Secondary Outcome Measures
NameTimeMethod
Time of Maximum Observed Plasma Concentration (Tmax) of DaclatasvirPredose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Tmax was obtained from concentration-time plot of daclatasvir by using non-compartmental method by a validated pharmacokinetic analysis program.

Plasma Concentration Observed at 24 Hours Postdose (C24) of DaclatasvirPredose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

C24 was obtained from concentration time plot of daclatasvir by using noncompartmental method by a validated pharmacokinetic analysis program.

Dose-normalized Maximum Observed Plasma Concentration (Cmax/D) and Dose-normalized Plasma Concentration Observed at 24 Hours Postdose (C24/D) of DaclatasvirPredose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

Cmax/D and C24/D are obtained from concentration-time plot of daclatasvir by using noncompartmental method by a validated pharmacokinetic analysis program.

Dose-normalized Area Under the Concentration-Time Curve in 1 Dosing Interval (AUC[TAU]/D) of DaclatasvirPredose (0 hour) on Day 2, 3 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 4 (Period 1); Predose (0 hour) on Day 12, 13 and 0, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hour on Day 14 (Period 2)

AUC(TAU)/D was obtained from concentration-time plot of daclatasvir by using noncompartmental method by a validated pharmacokinetic analysis program.

Number of Participants With Serious Adverse Events (SAEs) and Discontinuations Due to Adverse Events (AEs) and Who DiedFrom start of study treatment (Day 1) to study discharge for AEs (up to 15 days); Day 1 to 30 days after last dose of study treatment for SAEs (up to 44 days)

AE was defined as any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that does not necessarily have a causal relationship with treatment. SAE was defined as a medical event that at any dose resulted in death, persistent or significant disability/incapacity, or drug dependency/abuse; was life threatening, an important medical event, or a congenital anomaly/birth defect; or required or prolonged hospitalization.

Number of Participants With Abnormalities in Vital Sign MeasurementsFrom start of study treatment (Day 1) to study discharge (up to 15 days)

Criteria for abnormalities in vital sign measurements: Diastolic blood pressure: Value \>90 and change from baseline \> 0 or value \< 55 and change from baseline \<-10. Systolic blood pressure: Value \>140 and change from baseline \>20 or value \<90 and change from baseline \<-20. Heart rate: Value \>100 and change from baseline \>30 or value \<55 and change from baseline \<-15. Respiration: Value \>16 or change from baseline \>10. Temperature: Value \>38.3°C or change from baseline \>1.6°C.

Number of Participants With Abnormalities in Urinalysis and Other Chemistry Testing ResultsFrom start of study treatment (Day 1) to study discharge (up to 15 days)

Criteria for marked abnormalities on laboratory test results: urinary dipstick blood: ≥2 if pretreatment (PreRx) \<1, ≥2 if PreRx is missing or ≥2\*PreRx if PreRx ≥1. Urinary microscopic red blood cell (RBC): ≥2 if PreRx \<2, ≥2 if PreRx is missing or ≥4 if PreRx ≥2. Urinary microscopic white blood cell (WBC): ≥2 if PreRx \<2, ≥2 if PreRx is missing or ≥4 if PreRx ≥2. Lactate dehydrogenase \>1.25\*upper limit of normal (ULN) if PreRx ≤ULN, \>1.25\*ULN if PreRx is missing and \>1.5\*PreRx if PreRx \>ULN.

Number of Participants With Abnormalities in Electrocardiogram (ECG) FindingsFrom start of study treatment (Day 1) to study discharge (up to 15 days)

Abnormalities in ECG findings included: PR ≥210 msec, QRS ≥120 msec, QT ≥500 msec, QTcF ≥450 msec, and second- or third-degree heart block.

Number of Participants With Marked Abnormalities in Hematology Laboratory Test ResultsFrom start of study treatment (Day 1) to study discharge (up to 15 days)

Criteria for marked abnormalities in test results: Platelet count \>1.5\*upper limits of normal (ULN) value, \>1.5\*ULN if pretreatment (PreRx) value is missing, \<0.85\*lower limit of normal (LLN) if PreRx ≥LLN, \<0.85\*LLN if PreRx is missing, \<0.85\*PreRx if PreRx \<LLN. Leukocytes \>1.2\*ULN if LLN ≤PreRx ≤ULN, \>1.2\*ULN if PreRx is missing, \>1.5\*PreRx if PreRx \>ULN, \>ULN if PreRx \<LLN, \<0.85\*PreRx if PreRx \<LLN, \<0.9\*LLN if LLN ≤PreRx ≤ULN, \<0.9\*LLN if PreRx is missing and \<LLN if PreRx \>ULN. Lymphocytes \>7.5\*10\^3 c/uL and \<0.75\*10\^3 c/uL. Neutrophils \<0.85\*PreRx if PreRx \<1.5\*ULN, \<1.5\*ULN if PreRx ≥1.5\*ULN and \<1.5\*ULN if PreRx is missing.

Trial Locations

Locations (1)

Healthcare Discoveries, Llc D/B/A Icon Development Solutions

🇺🇸

San Antonio, Texas, United States

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