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A Multiple-Dose Study of Bulevirtide in Participants With Normal and Impaired Renal Function

Phase 1
Completed
Conditions
Chronic Hepatitis D Infection
Interventions
Registration Number
NCT05760300
Lead Sponsor
Gilead Sciences
Brief Summary

The goals of this study are to compare the amount of study drug, bulevirtide (BLV), that gets into the bloodstream and how long it takes for the body to eliminate it, measure the effect of BLV on bile acids, and evaluate the safety and tolerability of multiple doses of BLV in participants with normal or impaired renal (kidney) function.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
41
Inclusion Criteria

All Individuals:

  • Body mass index (BMI) of at least ≥ 18.0 kg/m^2 and ≤ 40.0 kg/m^2 at screening.
  • No clinically significant abnormalities on electrocardiogram (ECG)
  • No known Liver Disease (Aspartate Aminotransferase (AST) and Alanine Aminotransferase (ALT)) ≤ 3 x upper limit of normal (ULN) at screening.

Individuals with Renal Impairment (RI):

  • Have RI classification at screening that has been unchanged during the 90 days prior to study drug dosing.

  • Estimated Glomerular Filtration Rate (eGFR) must be the following (using the Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) equation (Inker 2021)) based on serum creatinine as measured at the screening evaluation:

    • Severe RI (Groups A and B): eGFR ≥ 15 to ≤ 29 mL/min/1.73 m^2
    • Moderate RI (Group C): eGFR ≥ 30 to ≤ 59 mL/min/1.73 m^2
    • Mild RI (Group D): eGFR ≥ 60 to ≤ 89 mL/min/1.73 m^2
  • Hemoglobin ≥ 9 g/dL at screening.

  • Individuals with cardiovascular disease, hypertension, diabetes mellitus, hyperlipidemia, hypothyroidism, osteoporosis, and many others) may be included provided that these diseases/conditions are clinically stable.

Matched Control Individuals:

  • Have an eGFR of at least 90 mL/min/1.73 m^2 (using the CKD-EPI equation) based on serum creatinine as measured at screening evaluation.
  • Matched for sex, age (± 10 years), and BMI (± 20%, 18.0 ≤ BMI ≤ 40.0 kg/m^2) with the respective participant in the RI group.

Key

Exclusion Criteria

All Individuals:

  • Positive human immunodeficiency virus (HIV) test, hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV) antibody with detectable HCV viral ribonucleic acid (RNA) at screening.
  • Have any serious or active medical or psychiatric illness (including depression) that, in the opinion of the investigator, would interfere with participant treatment, assessment, or compliance with the protocol.

Individuals with RI:

  • Recent history of reception of any blood or blood products or history of major bleeding within 4 weeks of dosing.
  • Positive test for drugs of abuse, including alcohol at screening or admission, with the exception of opioids and tetrahydrocannabinol (THC, marijuana) under prescription and verified by the investigator as for pain management.
  • Received treatment with trimethoprim or cimetidine or tenofovir prodrugs (tenofovir disoproxil fumarate (TDF) or tenofovir alafenamide (TAF)) (affects elimination of creatinine) or with competitors of renal tubular excretion (eg, probenecid, chronic high-dose nonsteroidal anti-inflammatory drugs) within 28 days of Day -1.
  • Received known nephrotoxic drugs (eg, aminoglycosides, amphotericin B, vancomycin, cidofovir, foscarnet, cisplatin, pentamidine, cyclosporine, tacrolimus, herbal remedies (eg, compounds with aristolochic acid)) within 28 days of Day -1.
  • Individuals requiring or anticipated to require dialysis within 90 days of study entry.
  • Serum albumin concentration <25 g/L.
  • Uncontrolled treated/untreated hypertension (defined as a mean of 3 repeated measurements for systolic blood pressure ≥180 mmHg and/or diastolic blood pressure ≥110 mmHg); current or documented history of repeated clinically significant hypotension or severe episodes of orthostatic hypotension (systolic blood pressure <90 mmHg and/or diastolic blood pressure <50 mmHg).

Matched Control Individuals:

  • Have taken any prescription medications or over-the-counter medications, including herbal products, within 28 days prior to start of study drug dosing, with the exception of vitamins

Note: Other protocol defined Inclusion/Exclusion criteria may apply

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Group A: BLV, Normal Renal Function (Matched Control Participants)Bulevirtide (BLV)Participants with normal renal function will receive BLV 2 mg once daily for 6 days. Following completion and evaluation of PK and safety data from all participants in Group A, additional participant groups (Groups B, C, and D) and BLV doses (2 mg or 10 mg) may be initiated.
Group A: Bulevirtide (BLV), Severe Renal Impaired ParticipantsBulevirtide (BLV)Participants with severe renal impairment will receive BLV 2 mg once daily for 6 days. Following completion and evaluation of pharmacokinetics (PK) and safety data from all participants in Group A, additional participant groups (Groups B, C, and D) and BLV doses (2 mg or 10 mg) may be initiated.
Primary Outcome Measures
NameTimeMethod
Pharmacokinetic (PK) Parameter: AUCtau of Bulevirtide (BLV)Day 6: Predose up to 24 hours postdose

AUCtau is defined as area under the concentration versus time curve over the dosing interval at steady state.

PK Parameter: Cmax ss of BLVDay 6: Predose up to 24 hours postdose

Cmax is defined as the maximum observed concentration of drug at steady state.

Secondary Outcome Measures
NameTimeMethod
PK Parameter: Cmax of BLVDay 1: Predose up to 24 hours postdose

Cmax is defined as the maximum observed concentration of drug.

PK Parameter: Cmax of Total BADay 1 and Day 6: Predose up to 24 hours postdose

Cmax is defined as the maximum observed concentration of total BA.

PK Parameter: AUC0-24 of BLVDay 1: Predose up to 24 hours postdose

AUC0-24 is defined as the concentration of drug over time between time 0 hour and time 24 hours.

PK Parameter: Tmax of BLVDay 1 and Day 6: Predose up to 24 hours postdose

Tmax is defined as the time (observed time point) of Cmax.

PK Parameter: t1/2 of BLVDay 1: Predose up to 24 hours postdose and Day 6: Predose up to 48 hours postdose

t1/2 is defined as the estimate of the terminal elimination half-life of the drug.

PK Parameter: CLss/F of BLVDay 6: Predose up to 48 hours postdose

CLss/F is defined as the apparent clearance at steady state.

PK Parameter: Ctrough of Total Bile Acids (BA)Day 2 and Day 5 (predose), Day 7, and Day 8

Ctrough is defined as the concentration of total BA at the end of the dosing interval.

PK Parameter: AUC0-24 of Total BADay 1 and Day 6: Predose up to 24 hours postdose

AUC0-24 is defined as the concentration of total BA over time between time 0 hour and time 24 hours.

PK Parameter: Tmax of Total BADay 1 and Day 6: Predose up to 24 hours postdose

Tmax is defined as the time (observed time point) of Cmax of total BA.

Percentage of Participants With Treatment-Emergent Adverse EventsFirst dose date up to 6 days plus 7 days
Percentage of Participants With Laboratory AbnormalitiesFirst dose date up to 6 days plus 7 days
PK Parameter: Vss/F of BLVDay 6: Predose up to 48 hours postdose

Vss/F is defined as the apparent volume of distribution at steady state.

Trial Locations

Locations (9)

Velocity Clinical Research, New Smyrna Beach

🇺🇸

Edgewater, Florida, United States

Panax Clinical Research

🇺🇸

Miami Lakes, Florida, United States

Floridian Clinical Research, LLC

🇺🇸

Miami Lakes, Florida, United States

Clinical Pharmacology of Miami, LLC

🇺🇸

Miami, Florida, United States

Advanced Pharma CR, LLC

🇺🇸

Miami, Florida, United States

Global Clinical Professionals Research

🇺🇸

Saint Petersburg, Florida, United States

Genesis Clinical Research, LLC

🇺🇸

Tampa, Florida, United States

Massachusetts General Hospital - Renal Associates Clinic

🇺🇸

Boston, Massachusetts, United States

Nucleus Network

🇺🇸

Saint Paul, Minnesota, United States

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