A Study of PCSK9 Inhibitor AK102 in Healthy Subjects

A First-in-Human,Randomized, Double-Blind, Placebo-Controlled, Single Dose Escalation,Phase 1 Study to Evaluate the Safety,Tolerability, Pharmacokinetics and Pharmacodynamics of AK102 in Healthy Subjects

This is a first-in-human,randomized, double-blind, placebo-controlled, single dose escalation, phase 1 study to evaluate the safety, tolerability, PK/PD and immunogenicity of AK102 administered subcutaneously in healthy subjects. Subjects will be randomized into 4 planned single dose escalation cohorts or placebo cohort.

Study Overview

• Status: Completed
• Conditions: Hypercholesterolaemia
• Intervention / Treatment: Drug: AK102; Drug: Placebo

• Study Type: Interventional
• Enrollment (Actual): 32
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Peking, China
    • Peking Union Medical College Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Signed Informed Consent.
• No clinically significant abnormalities judged by the principal investigator based on the medical history, physical examination, electrocardiogram and routine laboratory evaluations.
• Low-density lipoprotein cholesterol (LDL-C) level of 70-190 mg/dL (inclusive).
• Body mass index (BMI) ≥18 and ≤ 28 kg/m^2 , body weight >= 50 kg for male or >= 45 kg for female.

Exclusion Criteria:

• Triglyceride concentration >400 mg/dL (4.5 mmol/L).
• History of hypersensitivity reactions to any substance of the investigation drug or other monoclonal antibodies.
• Drug or alcohol abuse within 6 months prior to dosing.
• Blood pressure >140 mmHg (systolic) or > 90 mmHg (diastolic)

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Triple

Number of Arms

5

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo; Matching placebo	Drug: Placebo; Placebo single dose administered subcutaneously
Experimental: AK102 75mg	Drug: AK102; AK102 single dose administered subcutaneously
Experimental: AK102 150mg	Drug: AK102; AK102 single dose administered subcutaneously
Experimental: AK102 300mg	Drug: AK102; AK102 single dose administered subcutaneously
Experimental: AK102 500mg	Drug: AK102; AK102 single dose administered subcutaneously

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Incidence of treatment emergent AE	An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product temporally associated with the use of study treatment, whether or not considered related to the study treatment.	From single dose of AK102 through 12 weeks

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetic characteristics of AK102	Serum concentrations of AK102 at different timepoints before and after AK102 single dose.	over 12 weeks
Percent Change From Baseline in Low-Density Lipoprotein Cholesterol (LDL-C)	Low-Density Lipoprotein Cholesterol (LDL-C) blood concentrations before and after AK102 single dose.	At different time points from baseline through 12 weeks
Percent Change From Baseline in PCSK9	PCSK9 blood concentrations before and after AK102 single dose.	At different time points from baseline through 12 weeks
Number of subjects who develop detectable anti-drug antibodies (ADAs)	The immunogenicity of AK102 will be assessed by summarizing the number of subjects who develop detectable ADAs.	At different time points from baseline through 12 weeks

Collaborators and Investigators

• Sponsor: Akeso
• Collaborators: AD Pharmaceuticals Co., Ltd.
• Investigators: Principal Investigator: Rui Chen, MD, Peking Union Medical College Hospital

Study record dates

Study Major Dates

• Study Start (Actual): May 23, 2018
• Primary Completion (Actual): November 22, 2018
• Study Completion (Actual): November 22, 2018

Study Registration Dates

• First Submitted: November 17, 2019
• First Submitted That Met QC Criteria: November 17, 2019
• First Posted (Actual): November 19, 2019

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: February 27, 2025
• Last Verified: February 1, 2025

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Metabolic Diseases; Hyperlipidemias; Dyslipidemias; Lipid Metabolism Disorders; Hypercholesterolemia
• Other Study ID Numbers: AK102-101

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No