Lenacapavir API | HIV Capsid Inhibitor API Manufacturer in India

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Lenacapavir API

Lenacapavir is a long-acting HIV-1 capsid inhibitor that targets the HIV capsid protein at multiple stages of the viral life cycle. It is a highly potent antiretroviral agent developed for the treatment and prevention of HIV-1 infection in approved clinical settings.

Lenacapavir has a distinctive mechanism compared with conventional antiretroviral classes because it directly targets the HIV capsid, interfering with both early and late stages of viral replication.

Lenacapavir API Manufacturer in India

Lenacapavir is a specialized antiretroviral pharmaceutical API requiring controlled multi-step chemical synthesis, purification and extensive solid-state characterization.

Important quality attributes include identity, assay, related substances, stereochemical purity, water content, residual solvents, elemental impurities, polymorphic form and stability.

Chemical Information

CAS Number: 2188589-43-6
Molecular Formula: C39H32ClF10N7O5S2
Molecular Weight: 968.34 g/mol
Drug Class: Antiretroviral Agent
Pharmacological Class: HIV-1 Capsid Inhibitor
Therapeutic Class: Antiviral
Therapeutic Area: Infectious Diseases / HIV

Mechanism of Action

Lenacapavir binds directly to the HIV-1 capsid protein and interferes with capsid function.

Its activity affects multiple stages of the viral life cycle, including:

  • Viral capsid disassembly/uncoating
  • Nuclear transport and trafficking of viral material
  • HIV replication-complex function
  • Assembly of new viral particles
  • Capsid formation and maturation
  • Production of infectious virions

This multi-stage mechanism distinguishes lenacapavir from reverse transcriptase, protease and integrase inhibitors.

Pharmaceutical Applications

Lenacapavir is used in approved settings for:

  • Treatment of multidrug-resistant HIV-1 infection as part of an appropriate combination regimen
  • HIV-1 pre-exposure prophylaxis (PrEP) in approved populations and formulations

The specific indication, dosing schedule and formulation depend on the applicable regulatory approval.

Long-Acting Antiretroviral Characteristics

Lenacapavir has a very long pharmacokinetic half-life, enabling extended dosing intervals. Depending on the approved regimen, it may be administered using subcutaneous injection and/or oral administration as part of an initiation or maintenance regimen.

Its long-acting characteristics make it particularly relevant to HIV treatment and prevention strategies where infrequent dosing may improve adherence.

Manufacturing Process

Typical API manufacturing may involve:

  1. Preparation of substituted heterocyclic intermediates
  2. Controlled multi-step chemical synthesis
  3. Construction of the capsid-binding pharmacophore
  4. Introduction of fluorinated structural components
  5. Coupling of advanced intermediates
  6. Purification
  7. Crystallization
  8. Filtration
  9. Drying
  10. Polymorphic-form characterization
  11. Final analytical testing
  12. Controlled packaging

Quality and Analytical Testing

Lenacapavir API quality evaluation may include:

  • Identification by IR
  • Identification by HPLC
  • Mass spectrometry
  • Assay
  • Related substances
  • Organic impurities
  • Stereochemical purity
  • Water content
  • Residual solvents
  • Elemental impurities
  • Residue on ignition
  • Polymorphic-form characterization
  • Particle-size distribution where required
  • Stability testing

Storage

Lenacapavir should be stored in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive heat, moisture and direct light. Final storage requirements should be established through validated stability studies.

Pharmaceutical Research and Development

Lenacapavir is relevant to research involving:

  • HIV-1 capsid
  • HIV replication
  • Capsid inhibitors
  • Long-acting antiretroviral therapy
  • HIV drug resistance
  • Multidrug-resistant HIV
  • HIV prevention
  • Pre-exposure prophylaxis
  • Antiviral drug development
  • Viral assembly and maturation

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 NMT 0.5%
Total Impurities NMT 1.0%
Water Content NMT 1.0%
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