Assessment of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of a New Formulation of Inclisiran Containing Polysorbate 80 Compared to the Currently Marketed Formulation

Purpose

The purpose of this study is to compare safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of the currently marketed formulation of inclisiran with a new formulation containing polysorbate 80 (PS80), after a single 284 mg subcutaneous (SC) administration.

Condition

  • Inclisiran Formulation

Eligibility

Eligible Ages
Between 18 Years and 60 Years
Eligible Sex
All
Accepts Healthy Volunteers
Yes

Inclusion Criteria

  • Healthy male and female (non-childbearing potential) participants between 18 and 60 years of age (inclusive) with fasting serum LDL-C between 100 and 189 mg/dL (2.6 to 4.89 mmol/L) and fasting triglyceride <400 mg/dL (<4.52 mmol/L) that are not on statin or any other lipid lowering therapy. - Body mass index (BMI) between 18 and 35 kg/m2, inclusive, at screening with a body weight of at least 50 kg.

Exclusion Criteria

  • Participants with homozygous and heterozygous familial hypercholesterolemia will be excluded. - Historical or current use of any statin (i.e. study participants must be statin naive), other oral LDL-C-lowering medication or supplements that in investigators' judgment may affect serum LDL-C levels. Other protocol inclusion/exclusion criteria may apply

Study Design

Phase
Phase 1
Study Type
Interventional
Allocation
Randomized
Intervention Model
Parallel Assignment
Primary Purpose
Treatment
Masking
None (Open Label)

Arm Groups

ArmDescriptionAssigned Intervention
Active Comparator
Arm A (inclisiran - currently marketed formulation) 		Inclisiran 284 mg × 1 single dose on Day 1
  • Drug: Currently marketed inclisiran formulation
    Inclisiran 284 mg
    Other names:
    • KJX839
Experimental
Arm B (inclisiran - formulation containing PS80) 		Inclisiran 284 mg × 1 single dose on Day 1
  • Drug: Inclisiran formulation containing PS80
    Inclisiran 284 mg
    Other names:
    • KJX839

Recruiting Locations

Lenexa Research Unit
Lenexa, Kansas 66219

Cardiovasular Renal Metabolism
San Antonio, Texas 78232

Salt Lake City Research Unit
Salt Lake City, Utah 84124

More Details

Status
Recruiting
Sponsor
Novartis Pharmaceuticals

Study Contact

Novartis Pharmaceuticals
1-888-669-6682
novartis.email@novartis.com

Detailed Description

This is a randomized, single-dose, open-label, parallel-group, study to evaluate the PK, safety, and tolerability of inclisiran 284 mg. The study drug will be administered as a single SC injection to the abdomen administered as 2 different formulations (the marketed formulation and a test formulation containing PS80). Approximately 152 adult participants (76 per formulation) with elevated serum LDL-C, but otherwise healthy, are planned to be enrolled. The duration of the study for each participant will be approximately 118 days including the screening, up to 28 days, baseline period, and treatment period of 90 days.