- Raw materials
- Anti-HIV
- Lenacapavir
Filters
Filter
Custom request?
Type
Production region
Qualifications
Country of origin
Lenacapavir API Manufacturers & Suppliers
3 verified results
When insight is your advantage
Full data, full access, full negotiation power
Total market transparency
|
Supplier trade data access
|
Buyer / supplier flow comparison
Commercial-scale Suppliers
Distributor
Produced in
China|
Employees: 200+
|
Audit Report:
Certifications:
CoA
All certificates
CoA
Producer
Produced in
China|
Employees: 60
|
Audit Report:
Certifications:
GMP
|
CoAAll certificates
GMP
CoA
Take control of your API sourcing
Submit a Special Inquiry and have Pharmaoffer activate verified suppliers.
Producer
Produced in
China|
Employees: 3500
|
Audit Report:
Certifications:
GMP
|
MSDS|
ISO9001|
WC|
CoAAll certificates
GMP
MSDS
ISO9001
WC
CoA
Get full market intelligence report
€399,-
All Lenacapavir data. Full access. Full negotiation power
When insight is your advantage
Full data, full access, full negotiation power
Total market transparency
|
Supplier trade data access
|
Buyer / supplier flow comparison
Trusted by 30,000+ registered pharma professionals:
Reach multinationals, SMEs, compounding pharmacies & more!
Lenacapavir | CAS No: 2189684-44-2 | GMP-certified suppliers
A medication that treats multidrug-resistant HIV-1 infection in heavily treatment-experienced adults by improving viral suppression when combined with other antiretroviral agents.
Therapeutic categories
Anti-HIV AgentsAntiinfectives for Systemic UseAntiviral AgentsAntivirals for Systemic UseCytochrome P-450 CYP3A InhibitorsCytochrome P-450 CYP3A Substrates
Generic name
Lenacapavir
Molecule type
small molecule
CAS number
2189684-44-2
DrugBank ID
DB15673
Approval status
Approved drug, Investigational drug
ATC code
J05AX31
Primary indications
- Lenacapavir, in combination with other antiretroviral(s), is indicated for the treatment of multidrug-resistant human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults who are experiencing a failure of their current antiretroviral regimen due to resistance, intolerance, or safety considerations
Product Snapshot
- Lenacapavir is available as an oral tablet and a subcutaneous injection formulation
- It is indicated for use in the treatment of multidrug-resistant HIV-1 infection in heavily treatment-experienced adults
- Lenacapavir is approved or investigational in key regulatory markets including the US, EU, and Canada
Clinical Overview
Lenacapavir (CAS Number 2189684-44-2) is an antiviral agent approved for the treatment of multidrug-resistant human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults. It is indicated in combination with other antiretroviral agents for patients experiencing failure of current regimens due to resistance, intolerance, or safety issues. Regulatory approvals include the European Commission (August 2022) and the US FDA (December 2022).
Pharmacologically, lenacapavir is a first-in-class HIV-1 capsid inhibitor that disrupts multiple essential stages of the viral lifecycle, including viral uptake, assembly, and release. It exhibits potent picomolar-level inhibition of HIV-1 replication in vitro and shows little to no cross-resistance with other available antiretrovirals. Single subcutaneous doses achieve plasma concentrations exceeding the 95% effective concentration (EC95) for up to 24 weeks, supporting extended dosing intervals.
The mechanism of action involves binding with high affinity to the phenylalanine-glycine binding pocket located between the N-terminal and C-terminal domains of capsid protein hexamers. Lenacapavir competitively inhibits interactions between HIV-1 capsid and host nuclear pore proteins CPSF6 and Nup153, thereby blocking nuclear entry of the virus. Additionally, lenacapavir stabilizes capsid assembly and alters capsid morphology, which further impairs the viral replication process. Resistance mutations have been identified at the binding site but generally reduce viral fitness and do not confer cross-resistance to other antiretrovirals.
Pharmacokinetic data demonstrate extended plasma half-life with subcutaneous administration, allowing for infrequent dosing. Lenacapavir is both a substrate and moderate inhibitor of CYP3A4 enzymes and interactions with drug-metabolizing cytochrome P450 pathways should be considered. Safety assessment in clinical studies identified adverse effects consistent with underlying HIV infection and antiretroviral therapy.
From an API procurement perspective, lenacapavir’s chemical complexity, including its difluorobenzyl moiety and multiring heterocyclic structure, necessitates stringent quality control and compliance with regulatory standards. Manufacturers should ensure batch-to-batch consistency, impurity profiling, and validated analytical methods conforming to internationally recognized pharmacopeial guidelines. Reliable sourcing and supply chain transparency are critical given the therapeutic role of lenacapavir in treatment-experienced populations with limited options.
Pharmacologically, lenacapavir is a first-in-class HIV-1 capsid inhibitor that disrupts multiple essential stages of the viral lifecycle, including viral uptake, assembly, and release. It exhibits potent picomolar-level inhibition of HIV-1 replication in vitro and shows little to no cross-resistance with other available antiretrovirals. Single subcutaneous doses achieve plasma concentrations exceeding the 95% effective concentration (EC95) for up to 24 weeks, supporting extended dosing intervals.
The mechanism of action involves binding with high affinity to the phenylalanine-glycine binding pocket located between the N-terminal and C-terminal domains of capsid protein hexamers. Lenacapavir competitively inhibits interactions between HIV-1 capsid and host nuclear pore proteins CPSF6 and Nup153, thereby blocking nuclear entry of the virus. Additionally, lenacapavir stabilizes capsid assembly and alters capsid morphology, which further impairs the viral replication process. Resistance mutations have been identified at the binding site but generally reduce viral fitness and do not confer cross-resistance to other antiretrovirals.
Pharmacokinetic data demonstrate extended plasma half-life with subcutaneous administration, allowing for infrequent dosing. Lenacapavir is both a substrate and moderate inhibitor of CYP3A4 enzymes and interactions with drug-metabolizing cytochrome P450 pathways should be considered. Safety assessment in clinical studies identified adverse effects consistent with underlying HIV infection and antiretroviral therapy.
From an API procurement perspective, lenacapavir’s chemical complexity, including its difluorobenzyl moiety and multiring heterocyclic structure, necessitates stringent quality control and compliance with regulatory standards. Manufacturers should ensure batch-to-batch consistency, impurity profiling, and validated analytical methods conforming to internationally recognized pharmacopeial guidelines. Reliable sourcing and supply chain transparency are critical given the therapeutic role of lenacapavir in treatment-experienced populations with limited options.
Identification & chemistry
| Generic name | Lenacapavir |
|---|---|
| Molecule type | Small molecule |
| CAS | 2189684-44-2 |
| UNII | A9A0O6FB4H |
| DrugBank ID | DB15673 |
Pharmacology
| Summary | Lenacapavir is an antiviral agent targeting the HIV-1 capsid protein, specifically binding to a conserved pocket at the interface of capsid monomers to disrupt interactions with host proteins CPSF6 and Nup153 essential for nuclear entry. This binding inhibits multiple early steps of the viral lifecycle, including capsid nuclear import, viral DNA synthesis, and reverse transcription, while also stabilizing capsid assembly and altering capsid morphology. Lenacapavir demonstrates potent inhibition of HIV-1 replication, with a distinct resistance profile localized to its capsid binding site and minimal cross-resistance with other antiretrovirals. |
|---|---|
| Mechanism of action | HIV-1 co-opts various host factors during its replicative cycle, including during host cell entry, nuclear integration, replication, and virion assembly. Following the initial fusion with the host cell membrane, the viral capsid is released into the host cell cytoplasm. The capsid comprises approximately 250 hexamers and exactly 12 pentamers, each composed of monomeric capsid proteins (CA). Each CA monomer has an N-terminal and C-terminal domain (NTD/CTD) and offers an interaction surface for host cell machinery. Several important protein-protein interaction interfaces occur between CA monomers in the assembled multimers; the binding constants of these proteins are substantially lower for assembled multimers than individual capsid monomers. To facilitate HIV-1 genomic integration, the capsid must cross the nuclear envelope, for which it utilizes the nuclear pore complex (NPC). Two host proteins shown to be essential for capsid nuclear entry that directly bind to the capsid are cleavage and polyadenylation specificity factor subunit 6 (CPSF6) and nucleoporin 153 (Nup153, an NPC protein present on the nucleoplasmic face of the complex). Both proteins bind the same phenylalanine-glycine binding pocket between the NTD and CTD of neighbouring CA monomers in multimeric CA assemblies.[A244170, A244175, A244180, A244185] Lenacapavir contains a difluorobenzyl ring that occupies the same binding pocket as CPSF6/Nup153, overlapping with the benzyl group of F321 in CPSF6 and F1417 in Nup153 in the overlayed structures.[A244170, A244175, A244180, A244185] Crystal structures of lenacapavir bound to CA hexamers reveal that six lenacapavir molecules bind to each hexamer, establishing extensive hydrophobic interactions, two cation-π interactions, and seven hydrogen bonds, contacting ~2,000 Å<sup>2</sup> of buried protein surface area.[A244175, A244180] Strong binding of lenacapavir, therefore competitively interrupts capsid interactions with CPSF6 and Nup153. _In vitro_ HIV-1 replication inhibition experiments in a variety of cell lines show EC<sub>50</sub> values of ~12-314 pM, with greater efficacy against early steps over later steps.[A244175, A244180] At very low concentrations (0.5 nM), lenacapavir inhibits viral nuclear entry, while at higher concentrations (5-50 nM), it additionally inhibits viral DNA synthesis and reverse transcription. As CPSF6 and Nup153 are essential for nuclear entry, it is likely that lenacapavir binding inhibits these interactions and blocks capsid nuclear entry. Lenacapavir may have additional effects beyond blocking interactions with host cell factors. Lenacapavir increases the rate and extent of CA assembly, dramatically extends the lifetime of assembled CA structures, even at high salt concentrations, and alters assembled capsid morphology.[A244175, A244180] The stabilizing concentration is ~1:1, closely mimicking the observed binding stoichiometry to isolated CA hexamers. Further analysis suggests that lenacapavir binding alters intra- and inter-hexamer interactions, altering the structure and stability of the resulting assemblies. Serial passage of HIV-1 in increasing concentrations of lenacapavir resulted in the appearance of major resistance mutations Q67H and N74D, which remain sensitive to other antiretroviral drugs. Extended passage resulted in the additional mutations L56I, M66I, K70N, N74S, and T107N. All identified resistance mutations map to the lenacapavir binding site, and all but the Q67H variant show reduced replication capacity _in vitro_. Additional studies have shown no lenacapavir resistance in variants associated with resistance to other antiretrovirals or naturally occurring polymorphisms, suggesting a very low potential for cross-resistance in combination therapy. |
| Pharmacodynamics | Lenacapavir is an antiviral drug with an extended pharmacokinetic profile. Lenacapavir works against the HIV-1 virus by inhibiting viral replication: it interferes with a number of essential steps of the viral lifecycle, including viral uptake, assembly, and release. Single subcutaneous doses ≥100 mg in healthy volunteers resulted in plasma concentrations exceeding the 95% effective concentration (EC<sub>95</sub>) for ≥12 weeks while doses ≥300 mg exceeded the EC<sub>95</sub> for ≥24 weeks. In treatment-naive HIV-1-infected patients, a single subcutaneous dose of 20-450 mg resulted in a mean maximum log<sub>10</sub>-transformed reduction in plasma HIV-1 RNA of 1.35-2.20 by the ninth-day post-injection. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gag-Pol polyprotein | inhibitor |
ADME / PK
| Absorption | Following subcutaneous administration, lenacapavir is slowly released but completely absorbed, with peak plasma concentrations occurring at 84 days post-dose. Absolute bioavailability following oral administration is low, approximately 6 to 10%. T<sub>max</sub> after oral administration is about four hours. The mean steady-state C<sub>max</sub> (%CV) is 97.2 (70.3) ng/ mL following oral and subcutaneous administration. According to population pharmacokinetics analysis, lenacapavir exposures (AUC<sub>tau</sub>, C<sub>max</sub> and C<sub>trough</sub>) were 29% to 84% higher in heavily treatment-experienced patients with an HIV-1 infection compared to subjects without an HIV-1 infection. A low-fat meal had negligible effects on drug absorption. |
|---|---|
| Half-life | The median half-life ranged from 10 to 12 days following following oral administration, and 8 to 12 weeks following subcutaneous administration. |
| Protein binding | _In vitro_, lenacapavir is approximately 99.8% bound to plasma proteins. |
| Metabolism | Metabolism played a lesser role in lenacapavir elimination. It undergoes CYP3A4- and UGT1A1-mediated oxidation, N-dealkylation, hydrogenation, amide hydrolysis, glucuronidation, hexose conjugation, pentose conjugation, and glutathione conjugation. The metabolites of lenacapavir have not been fully characterized. No single circulating metabolite accounted for >10% of plasma drug-related exposure. |
| Route of elimination | Following a single intravenous dose of radiolabelled-lenacapavir in healthy subjects, 76% of the total radioactivity was recovered from feces and less than 1% from urine. Unchanged lenacapavir was the predominant moiety in plasma (69%) and feces (33%). |
| Volume of distribution | The steady state volume of distribution was 976 L in heavily treatment-experienced patients with an HIV-1 infection. |
| Clearance | Lenacapavir clearance was 3.62 L/h in heavily treatment experienced patients with HIV-1 infection. |
Formulation & handling
- Lenacapavir is available in both oral tablet and subcutaneous injectable formulations, requiring consideration of route-specific formulation parameters.
- The compound is a small molecule with low water solubility and high lipophilicity (LogP 6.4), which may impact formulation strategies for bioavailability enhancement.
- Oral lenacapavir can be administered with or without food as food intake does not significantly affect its absorption.
Regulatory status
| Lifecycle | The API is currently under patent protection in the United States with key patents expiring between 2034 and 2038, indicating an early to mid-stage lifecycle in this market. Its presence in the US, EU, and Canada suggests established market entry, with potential for generic competition in the future as patents expire. |
|---|
| Markets | US, EU, Canada |
|---|
Supply Chain
| Supply chain summary | Lenacapavir is supplied primarily by a single originator company with branded products available in the US, EU, and Canada. Multiple patents active until 2034–2038 indicate that generic competition is currently limited or not yet present in these markets. This suggests the supply chain remains focused on proprietary manufacturing and distribution. |
|---|
Safety
| Toxicity | There is limited information available regarding the acute toxicity and overdose of lenacapavir. If overdose occurs the patient must be monitored for signs or symptoms of adverse reactions. Treatment of overdose with lenacapavir consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. As lenacapavir is highly protein bound, it is unlikely to be significantly removed by dialysis. |
|---|
High Level Warnings:
- Limited acute toxicity data available
- Handle with caution to avoid unintentional exposure
- Highly protein-bound compound
Lenacapavir is a type of Anti-HIV
The Anti-HIV category of pharmaceutical APIs comprises a range of active pharmaceutical ingredients (APIs) specifically designed to combat the human immunodeficiency virus (HIV). These APIs play a critical role in the development and production of antiretroviral drugs, which are used to treat HIV infections and prevent the progression to acquired immunodeficiency syndrome (AIDS).
Anti-HIV APIs work by targeting various stages of the HIV life cycle, inhibiting viral replication and reducing the viral load in the body. Some commonly used APIs in this category include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), and integrase inhibitors (INIs).
NRTIs, such as tenofovir and emtricitabine, act by blocking the reverse transcriptase enzyme, an essential component in the replication of the virus. NNRTIs, such as efavirenz and nevirapine, bind to the reverse transcriptase enzyme, preventing its proper functioning. PIs, like ritonavir and atazanavir, inhibit the protease enzyme, crucial for viral maturation and assembly. INIs, such as raltegravir and dolutegravir, target the integrase enzyme, impeding viral integration into the host's DNA.
These APIs are carefully synthesized and undergo rigorous quality testing to ensure their safety, efficacy, and compliance with regulatory standards. Pharmaceutical companies utilize these APIs as key building blocks to formulate antiretroviral medications, which are then prescribed to individuals living with HIV/AIDS worldwide.
Overall, the Anti-HIV API category plays a vital role in the ongoing battle against HIV/AIDS, offering effective treatment options and improved quality of life for patients affected by this challenging condition.
Lenacapavir API manufacturers & distributors
Compare qualified Lenacapavir API suppliers worldwide. We currently have 3 companies offering Lenacapavir API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Arshine Pharmaceutical Co... | Distributor | China | China | CoA | 176 products |
| ChemExpress | Producer | United States | China | CoA, GMP, ISO9001, MSDS, WC | 197 products |
| Hangzhou Jinlan Pharm-Dru... | Producer | China | China | CoA, GMP | 40 products |
When sending a request, specify which Lenacapavir API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Lenacapavir API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
