- Raw materials
- Anti-HIV
- Enfuvirtide
Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Enfuvirtide API Manufacturers & Suppliers
2 verified results
Commercial-scale Suppliers
Employees: 200+
All certificates
Employees: 1500+
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Enfuvirtide | CAS No: 159519-65-0 | GMP-certified suppliers
A medication that provides antiretroviral fusion inhibition in combination therapy for managing HIV-1 infection and AIDS, primarily used in treatment-experienced patients.
Therapeutic categories
Primary indications
- Enfuvirtide is an antiretroviral drug used in combination therapy for the treatment of HIV-1/AIDS
Product Snapshot
- Enfuvirtide is a parenteral injectable peptide formulated as a lyophilized powder for subcutaneous administration
- It is primarily utilized as an antiretroviral agent in combination therapy for the treatment of HIV-1/AIDS
- Enfuvirtide holds approval status in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Mechanistically, enfuvirtide binds specifically to the first heptad-repeat region (HR1) of the gp41 subunit within the HIV-1 envelope glycoprotein complex. This interaction interrupts the conformational rearrangements necessary for fusion between the viral and cellular membranes, a critical step required for viral entry into CD4-positive T cells. By mimicking natural components of the HIV fusion machinery and competitively disrupting their function, enfuvirtide thereby inhibits the incorporation and spread of the virus within the host.
Pharmacokinetic data indicate that enfuvirtide is administered via subcutaneous injection due to its peptide structure, which limits oral bioavailability. Its metabolism is primarily proteolytic degradation rather than hepatic enzymatic pathways, and no significant cytochrome P450 mediated metabolism has been reported. The elimination half-life supports twice-daily dosing regimens.
From a safety perspective, enfuvirtide is generally well-tolerated with injection site reactions being the most commonly observed adverse effect. Given its novel mechanism, drug-drug interactions through CYP450 enzymes are minimal; however, monitoring for hypersensitivity and local tolerance is advised. Toxicity concerns are largely related to its peptide nature and immunogenic potential.
Enfuvirtide is marketed under brand names including Fuzeon and is utilized predominantly in treatment-experienced HIV-1 patients with resistance to other antiretroviral classes.
For formulation scientists and sourcing professionals, it is critical to ensure the peptide API conforms to stringent quality attributes such as purity, peptide sequence integrity, and absence of immunogenic contaminants. Due to its complex synthesis, sourcing from reliable manufacturers with validated peptide synthesis and characterization protocols is essential to maintain batch-to-batch consistency and regulatory compliance.
Identification & chemistry
| Generic name | Enfuvirtide |
|---|---|
| Molecule type | Biotech |
| CAS | 159519-65-0 |
| UNII | 19OWO1T3ZE |
| DrugBank ID | DB00109 |
Pharmacology
| Summary | Enfuvirtide is an antiretroviral peptide that targets the gp41 subunit of the HIV-1 envelope glycoprotein. It inhibits viral entry by binding to the heptad-repeat 1 (HR1) region, blocking the conformational changes required for membrane fusion between the virus and host cell. This mechanism disrupts the late stage of HIV-1 fusion, reducing viral replication and spread. |
|---|---|
| Mechanism of action | Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. By disrupting the HIV-1 molecular machinery during its final stage of fusion with the target cell, enfuvirtide limits the spread of further infection. Enfuvirtide is a biomimetic peptide that was rationally designed to mimic components of the HIV-1 fusion machinery and displace them, preventing normal fusion. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Envelope glycoprotein | Human immunodeficiency virus 1 |
ADME / PK
| Absorption | After a 90 mg single subcutaneous injection of Enfuvirtide into the abdomen in 12 HIV-1 infected subjects, the mean peak concentration is 4.59+/-1.5 ug/ml and the median time to peak concentration was 8 hours (ranged from 3 to12 hours). |
|---|---|
| Half-life | 3.8 +/- 0.6 hrs |
| Protein binding | 92% |
| Metabolism | Expected to undergo catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool. |
| Volume of distribution | * 5.5 ± 1.1 L |
| Clearance | * 24.8 +/- 4.1 mL/h/kg [HIV-1 infected adult and pediatric subjects following a 90-mg single SC dose of enfuvirtide] * 30.6 +/- 10.6 mL/h/kg [Following 90-mg twice daily dosing of FUZEON SC in combination with other antiretroviral agents in HIV-1 infected subjects] * 40 +/- 17 mL/h/kg [pediatric patients in the presence of concomitant medications including antiretroviral agents receiving the 2 mg/kg twice daily dose] |
Formulation & handling
- Enfuvirtide is a biotech peptide formulated as a lyophilized powder for subcutaneous injection requiring reconstitution prior to administration.
- Due to its peptide nature, it requires careful handling to maintain stability, including protection from moisture and temperature extremes.
- Formulation development should consider its parenteral route and potential sensitivity to proteolytic degradation.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's key patents in the United States and Canada expired between 2013 and 2016, resulting in an established market presence in the US, Canada, and the EU. The product is now in a mature phase with generic competition available across these regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Enfuvirtide is primarily manufactured by a single originator company with packaging handled by multiple entities. Its branded product, Fuzeon, is distributed across the US, Canada, and EU markets. Patent expirations between 2013 and 2016 indicate the presence of existing generic competition in these regions. |
|---|
Enfuvirtide 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.
Enfuvirtide API manufacturers & distributors
Compare qualified Enfuvirtide API suppliers worldwide. We currently have 2 companies offering Enfuvirtide API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Chengdu Shengnuo Biopharm... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 33 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
When sending a request, specify which Enfuvirtide 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 Enfuvirtide 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.
