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Fosamprenavir | CAS No: 226700-79-4 | GMP-certified suppliers
A medication that supports combination antiretroviral therapy for treating HIV-1 infection and postexposure prophylaxis by inhibiting viral replication with noted safety considerations.
Therapeutic categories
Primary indications
- Indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection, as well as postexposure prophylaxis of HIV infection in individuals who have had occupational or nonoccupational exposure to potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission
- The use of fosamprenavir is pending revision due to a potential association between the drug and myocardial infarction and dyslipidemia in HIV infected adults
Product Snapshot
- Fosamprenavir is an oral small molecule available in tablet and suspension formulations
- It is primarily indicated for the treatment and postexposure prophylaxis of HIV-1 infection in combination with other antiretroviral agents
- Fosamprenavir is approved in key regulatory markets including the US, Canada, and the EU
Clinical Overview
Pharmacodynamically, fosamprenavir undergoes enzymatic hydrolysis by cellular phosphatases to release the active protease inhibitor amprenavir. This bioconversion allows for a sustained release of the active moiety, which can reduce dosing frequency compared to direct amprenavir administration. Amprenavir acts specifically by inhibiting the HIV-1 protease enzyme, which is essential in viral replication. HIV protease cleaves the Gag and Gag-Pol polyprotein precursors into functional viral proteins. Inhibition of this enzyme by amprenavir results in the production of immature, non-infectious viral particles, thereby interfering with viral maturation.
Key absorption, distribution, metabolism, and excretion (ADME) parameters include oral absorption with rapid conversion to amprenavir, which is a substrate and moderate inhibitor of cytochrome P450 3A4. This interaction profile necessitates careful consideration of potential drug-drug interactions, especially with agents metabolized by CYP3A4. Safety concerns predominantly relate to metabolic disturbances such as dyslipidemia and hyperglycemia, as well as cardiovascular risks that may contraindicate use in susceptible populations.
Fosamprenavir is marketed under various brand names globally and is employed primarily within combination antiretroviral therapy regimens. From a sourcing perspective, procurement of fosamprenavir API requires strict adherence to pharmaceutical quality standards, including rigorous control of purity, residual solvents, and polymorphic form. Suppliers must ensure compliance with regulatory guidelines relevant to antiviral agents, alongside robust documentation to support risk management related to safety and stability profiles.
Identification & chemistry
| Generic name | Fosamprenavir |
|---|---|
| Molecule type | Small molecule |
| CAS | 226700-79-4 |
| UNII | WOU1621EEG |
| DrugBank ID | DB01319 |
Pharmacology
| Summary | Fosamprenavir is a prodrug converted to amprenavir, an inhibitor of the HIV-1 protease enzyme. By binding to the active site of HIV-1 protease, amprenavir blocks the cleavage of viral polyproteins necessary for the maturation of infectious virions. This mechanism disrupts viral replication, resulting in the production of immature, non-infectious viral particles. |
|---|---|
| Mechanism of action | Fosamprenavir is a prodrug that is rapidly hydrolyzed to amprenavir by cellular phosphatases in the gut epithelium as it is absorbed. Amprenavir is an inhibitor of HIV-1 protease. During HIV replication, HIV protease cleaves viral polypeptide products of the Gag and Gag-Pol genes to form structural proteins of the virion core and essential viral enzymes. Amprenavir interferes with this process by binding to the active site of HIV-1 protease, thereby preventing the processing of viral Gag and Gag-Pol polyprotein precursors, resulting in the formation of immature non-infectious viral particles. |
| Pharmacodynamics | Fosamprenavir is hydrolyzed by cellular phosphatases to the antiretroviral protease inhibitor amprenavir. This hydrolysis allows for the slow release of amprenavir, reducing the number of pills a patient must take. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Human immunodeficiency virus type 1 protease | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | The absolute oral bioavailability of amprenavir after administration of fosamprenavir in humans has not been established. After administration of a single 1,400 mg dose in the fasted state, fosamprenavir oral suspension (50 mg/mL) and fosamprenavir tablets (700 mg) provided similar amprenavir exposures (AUC), however, the C<sub>max</sub> of amprenavir after administration of the suspension formulation was 14.5 % higher compared with the tablet. |
|---|---|
| Half-life | The plasma elimination half-life of amprenavir (the active metabolite) is approximately 7.7 hours. |
| Protein binding | Very high (approximately 90%); primarily bound to alpha 1 -acid glycoprotein. Higher amounts of unbound amprenavir present as amprenavir serum concentrations increase. |
| Metabolism | In the gut epithelium during absorption, fosamprenavir is rapidly and almost completely hydrolyzed to amprenavir and inorganic phosphate prior to reaching the systemic circulation. Amprenavir is metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system. |
| Route of elimination | Excretion of unchanged amprenavir in urine and feces is minimal. The renal elimination of unchanged amprenavir represents approximately 1% of the administered dose; therefore, renal impairment is not expected to significantly impact the elimination of amprenavir. Amprenavir, the active metabolite of fosamprenavir, is metabolized in the liver by the cytochrome P450 enzyme system. |
Formulation & handling
- Fosamprenavir is a small molecule API intended for oral administration in tablet or suspension form.
- The compound has moderate lipophilicity (LogP 1.92) and limited water solubility, requiring careful consideration in formulation design for bioavailability.
- Food interactions include avoidance of alcohol and fatty foods, though dosing can occur with or without food, indicating formulation stability under gastric conditions.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is currently in a mature market phase, with key patents expired or expiring between 2018 and 2020 in the US and Canada, while patent status in the EU suggests approaching or recent exclusivity loss. Products containing this API are marketed across the US, Canada, and EU regions. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Fosamprenavir is manufactured and repackaged by multiple companies, including original manufacturers and third-party packagers, with branded products such as Lexiva available across the US, Canada, and EU markets. The presence of patents in the US and Canada with expiration dates between 2016 and 2020 indicates that generic competition is likely established or imminent in these regions. This suggests a mature supply environment with both originator and generic manufacturers contributing to the API supply. |
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Fosamprenavir 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.
