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Study to Evaluate the Safety, PK, and Pharmacodynamics of LIB003

Phase 1
Completed
Conditions
Hypercholesterolemia
Interventions
Biological: LIB003
Registration Number
NCT03545438
Lead Sponsor
LIB Therapeutics LLC
Brief Summary

Randomized, double-blind, placebo-controlled, single ascending dose study in nine (9) separate and sequential dose cohorts (7 SC and 2 IV cohorts) to assess the safety and tolerability, pharmacokinetics and pharmacodynamics of LIB003 in subjects with moderately elevated LDL-C levels.

Detailed Description

After meeting eligibility criteria within each cohort subjects will be randomized to receive a single dose of LIB003. Seven (7) cohorts will receive LIB003 escalating doses of LIB003, or placebo, by SC injection and 2 cohorts LIB003 or placebo by IV infusion. Dose escalation will be based on the assessment of safety and tolerability data. All cohorts will each first enroll a sentinel group of subjects who will receive LIB003 or placebo in a double-blind fashion with the remaining subjects in that cohort only to be dosed after the safety data on day 4 from the sentinel subjects has been assessed and deemed safe.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
63
Inclusion Criteria
  • Men and women who are >/=18 and </=70 years of age. Female subjects must be of non-childbearing potential.
  • LDL-C >/=100 mg/dL who are either not on a lipid-lowering therapy or who are on stable statin therapy.
  • Body mass index (BMI) >18 and <38 kg/m2
  • Mild hypertensives on a stable dose of no more than one antihypertensive drug
Exclusion Criteria
  • History of any prior or concomitant clinical condition or acute and/or unstable systemic disease compromising subject inclusion
  • Systolic blood pressure <90 mmHg or >160 mmHg or diastolic blood pressure <50 or >100 mmHg at screening
  • Positive blood screen for human immunodeficiency virus (HIV), hepatitis B surface antigen, or hepatitis C virus antibody
  • Abnormal liver function test at Screening (aspartate aminotransferase [AST] or alanine aminotransferase [ALT] >2 × the upper limit of normal [ULN]
  • Estimated glomerular filtration rate <60 mL/min/1.73 m2 at screening, as determined by the CKD-EPI Equation
  • History of prescription drug abuse, illicit drug use (including marijuana), or alcohol abuse
  • Unable to spend 4 days in confinement unit
  • History of allergy to protein-based biologics including, but not limited to, mAbs and vaccine
  • Any other finding which, in the opinion of the Investigator, would compromise the subject's safety or participation in the study

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
cohort 7LIB003LIB003 dose 5 IV
cohort 2LIB003LIB003 dose 2 SC
cohort 4LIB003LIB003 dose 4 SC
cohort 1LIB003LIB003 dose 1 SC
cohort 5LIB003LIB003 dose 5 SC
cohort 9LIB003LIB003 dose 4 SC - statin treated
cohort 3LIB003LIB003 dose 4 SC
cohort 6LIB003LIB003 dose 4 IV
cohort 8LIB003LIB003 dose 3 SC - statin treated
Primary Outcome Measures
NameTimeMethod
The incidence and severity of treatment emergent adverse events (TEAEs)43 days

safety and tolerability will be assessed by the incidence and severity of treatment emergent adverse events

Secondary Outcome Measures
NameTimeMethod
Absolute change in serum unbound (free) proprotein convertase subtilisin/kexin type 9 (PCSK9) concentrations over time43 days

Serum free PCSK9 will be measured at baseline and various time points over 43 days

Absolute change in serum total PCSK9 over time43 days

Serum total PCSK9 will be measured at baseline and various time points over 43 days

Percent change in Low Density Lipoprotein cholesterol (LDL-C) over time43 days

Serum LDL-C will be measured at baseline and various time points over 43 days to derive percent change

Percent change in Apolipoprotein B (Apo B) over time43 days

Serum Apo B will be measured at baseline and various time points over 43 days to derive percent change

Changes in serum LIB003 concentrations over time43 days

serum LIB003 will be measured at various time points to derive AUC (area under curve)

Presence of anti LIB003 antibodies (ADAs)43 days

Measurement of ADAs will be done at baseline and various intervals after LIB003 administration

Trial Locations

Locations (1)

Medpace (MARC/CPU)

🇺🇸

Cincinnati, Ohio, United States

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