Lerodalcibep API | PCSK9 Inhibitor API Manufacturer in India

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Lerodalcibep API

Lerodalcibep is a recombinant lipid-lowering biologic designed to inhibit proprotein convertase subtilisin/kexin type 9 (PCSK9). By binding PCSK9, lerodalcibep helps increase the availability of low-density lipoprotein receptors (LDL receptors) on hepatocytes, thereby enhancing the removal of LDL cholesterol from the bloodstream.

Lerodalcibep is being developed for the management of hypercholesterolemia and cardiovascular risk, particularly in patients requiring additional LDL-cholesterol lowering.

Lerodalcibep API Manufacturer in India

Lerodalcibep is a specialized biological pharmaceutical ingredient requiring recombinant production, purification and extensive characterization.

Important quality attributes include identity, purity, molecular integrity, aggregation, charge variants, binding activity, biological potency, host-cell proteins, residual DNA, endotoxins, bioburden and sterility.

Biological Information

CAS Number: 2656799-04-1
Molecular Formula: Not applicable as a conventional small molecule
Molecular Weight: Approximately 85 kDa
Drug Class: Lipid-Lowering Biologic
Pharmacological Class: PCSK9 Inhibitor
Therapeutic Class: Lipid-Modifying Agent
Therapeutic Area: Cardiovascular / Metabolic

Mechanism of Action

Lerodalcibep binds to PCSK9 and prevents PCSK9 from promoting degradation of hepatic LDL receptors.

Increased LDL-receptor availability allows the liver to remove more LDL cholesterol from circulation.

The mechanism results in:

  • Increased hepatic LDL-receptor recycling
  • Enhanced LDL-cholesterol clearance
  • Reduction in circulating LDL cholesterol
  • Improvement of lipid control
  • Potential reduction of cardiovascular risk

Pharmaceutical Applications

Lerodalcibep is being developed for patients requiring substantial LDL-cholesterol reduction, including those with:

  • Hypercholesterolemia
  • Heterozygous familial hypercholesterolemia
  • Atherosclerotic cardiovascular disease
  • Patients requiring additional LDL-C lowering despite standard lipid-lowering therapy

Specific indications depend on the applicable regulatory approval and product labeling.

PCSK9 Inhibitor Characteristics

Lerodalcibep is a long-acting PCSK9-binding biologic designed to provide sustained inhibition of circulating PCSK9.

Its long-acting characteristics support an extended dosing interval compared with many conventional lipid-lowering therapies.

Manufacturing Process

Typical recombinant biologic manufacturing may involve:

  1. Recombinant cell-line development
  2. Mammalian cell-culture production
  3. Harvest and clarification
  4. Protein capture
  5. Chromatographic purification
  6. Viral inactivation
  7. Viral filtration
  8. Ultrafiltration/diafiltration
  9. Formulation
  10. Sterile filtration
  11. Aseptic filling
  12. Final quality-control testing

Quality and Analytical Testing

Lerodalcibep quality evaluation may include:

  • Identity testing
  • Molecular-weight determination
  • Protein concentration
  • Purity
  • Aggregate analysis
  • Fragment analysis
  • Charge-variant analysis
  • Peptide mapping
  • Structural characterization
  • PCSK9-binding assay
  • Biological potency assay
  • Host-cell protein
  • Residual host-cell DNA
  • Endotoxins
  • Bioburden
  • Sterility
  • Subvisible particles
  • Stability testing

Storage

Lerodalcibep drug substance and finished product should be stored according to validated stability data and approved product requirements, generally under controlled refrigerated conditions where specified. Protection from freezing, excessive heat and inappropriate light exposure is important for maintaining protein stability.

Pharmaceutical Research and Development

Lerodalcibep is relevant to research involving:

  • PCSK9
  • LDL receptors
  • LDL cholesterol
  • Hypercholesterolemia
  • Familial hypercholesterolemia
  • Atherosclerotic cardiovascular disease
  • Lipid metabolism
  • Cardiovascular risk reduction
  • Long-acting biologics
  • PCSK9-targeted therapies

Detailed Specifications

Parameter Specification
Appearance White to off-white crystalline powder
Identification IR & HPLC compliant
Assay (HPLC) 98.0% – 102.0%
Loss on Drying NMT 1.0%
Residue on Ignition NMT 0.5%
Heavy Metals NMT 10 ppm
pH (1% Solution) 2.0 – 4.0
Individual Impurity ≤ 0.5%
Total Impurities ≤ 1.5%
Water Content NMT 1.0%
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