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Saquinavir | CAS No: 127779-20-8 | GMP-certified suppliers
A medication that treats HIV-1 infection in patients aged 16 and older by inhibiting viral protease, used in combination with ritonavir and other antiretroviral agents.
Therapeutic categories
Agents Causing Muscle ToxicityAnti-HIV AgentsAnti-Infective AgentsAnti-Retroviral AgentsAntiinfectives for Systemic UseAntiviral Agents
Generic name
Saquinavir
Molecule type
small molecule
CAS number
127779-20-8
DrugBank ID
DB01232
Approval status
Approved drug, Investigational drug
ATC code
J05AE01
Primary indications
- Saquinavir is indicated, in combination with ritonavir and other antiretroviral agents, for the treatment of HIV-1 infection in patients 16 years of age and older
Product Snapshot
- Saquinavir is available as oral capsules and tablets in various coated and liquid-filled formulations
- It is primarily used as an antiretroviral agent for the treatment of HIV-1 infection in combination with ritonavir and other agents
- Saquinavir is approved for use in major regulatory markets including the US, Canada, and the EU
Clinical Overview
Saquinavir (CAS Number 127779-20-8) is an HIV-1 protease inhibitor indicated in combination with ritonavir and other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in patients aged 16 years and older. It was the first protease inhibitor approved by the FDA in 1995 and remains in clinical use primarily due to its relatively manageable safety profile compared to other antiretroviral therapies.
Pharmacologically, saquinavir belongs to the class of quinoline carboxamides. It exerts antiviral activity by selectively inhibiting the HIV-1 protease enzyme, a dimeric aspartic protease essential for the cleavage of the viral Gag polyprotein during the HIV lifecycle. This process is critical for viral maturation; inhibition results in the formation of immature, non-infectious viral particles. The molecular design of saquinavir incorporates a hydroxyethylene scaffold that mimics the peptide bond normally targeted by the protease but resists cleavage, thereby blocking enzyme activity.
Saquinavir’s oral bioavailability is limited (approximately 4%), but co-administration with ritonavir—a potent cytochrome P450 3A enzyme inhibitor—increases saquinavir plasma concentrations significantly by reducing its metabolic clearance and improving exposure. This pharmacokinetic boosting optimizes therapeutic antiviral efficacy.
Key ADME characteristics include metabolism primarily via CYP3A4 enzymes with substantial involvement in drug transport systems such as P-glycoprotein and organic anion transporting polypeptides. Saquinavir itself is a substrate and inhibitor of multiple cytochrome P450 enzymes and transporters, contributing to its well-documented potential for drug-drug interactions.
Safety considerations include risks of QTc interval prolongation, requiring caution when used with other QTc-prolonging agents or in patients with cardiac disease. Metabolic disturbances such as hyperglycemia and dyslipidemia have been reported, as have hepatic adverse effects, necessitating regular monitoring of liver function and metabolic parameters during treatment.
From an API sourcing perspective, quality control of saquinavir must ensure compliance with regulatory standards for purity, potency, and polymorphic form due to its complex chemical structure and significant clinical implications. Suppliers should provide robust certificates of analysis and ensure manufacturing processes minimize impurities and maintain batch-to-batch consistency given saquinavir’s narrow therapeutic index and critical role in combination antiretroviral regimens.
Pharmacologically, saquinavir belongs to the class of quinoline carboxamides. It exerts antiviral activity by selectively inhibiting the HIV-1 protease enzyme, a dimeric aspartic protease essential for the cleavage of the viral Gag polyprotein during the HIV lifecycle. This process is critical for viral maturation; inhibition results in the formation of immature, non-infectious viral particles. The molecular design of saquinavir incorporates a hydroxyethylene scaffold that mimics the peptide bond normally targeted by the protease but resists cleavage, thereby blocking enzyme activity.
Saquinavir’s oral bioavailability is limited (approximately 4%), but co-administration with ritonavir—a potent cytochrome P450 3A enzyme inhibitor—increases saquinavir plasma concentrations significantly by reducing its metabolic clearance and improving exposure. This pharmacokinetic boosting optimizes therapeutic antiviral efficacy.
Key ADME characteristics include metabolism primarily via CYP3A4 enzymes with substantial involvement in drug transport systems such as P-glycoprotein and organic anion transporting polypeptides. Saquinavir itself is a substrate and inhibitor of multiple cytochrome P450 enzymes and transporters, contributing to its well-documented potential for drug-drug interactions.
Safety considerations include risks of QTc interval prolongation, requiring caution when used with other QTc-prolonging agents or in patients with cardiac disease. Metabolic disturbances such as hyperglycemia and dyslipidemia have been reported, as have hepatic adverse effects, necessitating regular monitoring of liver function and metabolic parameters during treatment.
From an API sourcing perspective, quality control of saquinavir must ensure compliance with regulatory standards for purity, potency, and polymorphic form due to its complex chemical structure and significant clinical implications. Suppliers should provide robust certificates of analysis and ensure manufacturing processes minimize impurities and maintain batch-to-batch consistency given saquinavir’s narrow therapeutic index and critical role in combination antiretroviral regimens.
Identification & chemistry
| Generic name | Saquinavir |
|---|---|
| Molecule type | Small molecule |
| CAS | 127779-20-8 |
| UNII | L3JE09KZ2F |
| DrugBank ID | DB01232 |
Pharmacology
| Summary | Saquinavir is a peptidomimetic inhibitor of the HIV-1 protease enzyme, preventing the proteolytic cleavage of the Gag polyprotein essential for viral maturation. By inhibiting this enzyme, saquinavir disrupts the production of infectious HIV particles, impairing viral replication. Its pharmacodynamic profile includes potential for drug interactions and effects on cardiac conduction and metabolic parameters. |
|---|---|
| Mechanism of action | The HIV lifecycle is comprised of 3 distinct stages: assembly, involving creation and packaging of essential viral components; budding, wherein the viral particle crosses the host cell plasma membrane and forms a lipid envelope; and maturation, wherein the viral particle alters its structure and becomes infectious. At the center of this lifecycle is the Gag polyprotein which, along with the products of its proteolysis, coordinate these stages and function as the major structural proteins of the virus. The HIV-1 protease enzyme, a dimeric aspartic protease, is the enzyme responsible for cleaving the Gag polyprotein and thus plays a critical role in many aspects of the HIV viral lifecycle. Saquinavir is an inhibitor of the HIV-1 protease enzyme. Its design is based on the "peptidomimetic" principle, wherein the molecule contains a hydroxyethylene scaffold that mimics the normal peptide linkage (cleaved by HIV protease) but which itself cannot be cleaved. By preventing HIV-1 protease activity, and thus the proteolysis of the Gag polyprotein, saquinavir results in the production of immature, non-infectious viral particles. |
| Pharmacodynamics | Saquinavir exerts its antiviral activity by inhibiting an enzyme critical for the HIV-1 viral lifecycle. Like other protease inhibitors, saquinavir has a propensity for participating in drug interactions - use caution when administering saquinavir to patients maintained on other pharmaceutical agents as pharmacodynamic and pharmacokinetic interactions are common. Saquinavir is known to increase the QTc-interval in otherwise healthy individuals, and should therefore be used with caution in patients maintained on other QTc-prolonging medications or for whom prolongation of the QTc-interval may be of particular consequence (e.g. patients with pre-existing heart disease). Careful and regular monitoring of patient bloodwork is recommended, as saquinavir has been associated with the development of metabolic complications (e.g. diabetes mellitus, hyperlipidemia) and worsening of pre-existing liver disease. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Human immunodeficiency virus type 1 protease | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | The absolute bioavailability of orally administered saquinavir is only ~4%, thought to be a consequence of incomplete absorption and extensive first-pass metabolism. It is co-administered with ritonavir, another protease inhibitor and a potent inhibitor of the enzymes responsible for saquinavir's first-pass metabolism, in order to dramatically boost its serum concentrations and, by extension, its therapeutic efficacy. Following administration of saquinavir 1000mg twice daily with ritonavir 100mg twice daily the AUC<sub>24h</sub> at steady-state was 39026 ng.h/mL. |
|---|---|
| Protein binding | Saquinavir is approximately 98% plasma protein-bound independent of serum concentration. |
| Metabolism | Saquinavir is extensively metabolized in the liver following oral administration, and _in vitro_ studies have shown that >90% of its biotransformation is mediated by the CYP3A4 isoenzyme. Saquinavir is rapidly metabolized to a number of inactive mono- and di-hydroxylated compounds. |
| Route of elimination | The primary means of elimination of saquinavir appears to be extensive hepatic metabolism followed by fecal excretion of both the parent drug and metabolic products. Following the administration of radiolabeled saquinavir (both orally and intravenously), approximately 81-88% of radioactivity is recovered in the feces within 5 days of dosing while only 1-3% is recovered in the urine. Mass balance studies indicate that only 13% of orally-administered plasma radioactivity is attributed to unchanged parent drug, with the remainder comprising metabolic products of saquinavir's hepatic metabolism. In contrast, intravenous administration resulted in approximately 66% of the circulating plasma radioactivity being attributed to unchanged parent drug, suggesting a high degree of first-pass metabolism with oral administration. |
| Volume of distribution | The steady-state volume of distribution of saquinavir is approximately 700 L, suggesting extensive distribution into tissues. |
| Clearance | The systemic clearance of saquinavir is approximately 1.14 L/h/kg following intravenous administration. |
Formulation & handling
- Saquinavir is administered orally in various solid dosage forms including coated tablets and capsules.
- It is a small molecule with low water solubility (2.47 mg/L) and moderate lipophilicity (LogP 3.16), requiring formulation strategies to enhance bioavailability.
- Co-administration with grapefruit products should be avoided due to inhibition of metabolism, and dosing is recommended after meals to optimize absorption.
Regulatory status
| Lifecycle | The API has reached post-patent expiration phase in the United States and Canada, with key patents having expired between 2010 and 2020, indicating a mature market with generic availability; patent status in the EU is not specified. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Saquinavir is manufactured and packaged by multiple firms, including both originator and third-party packagers, indicating a diversified supply base. The drug is marketed in the US, Canada, and the EU under several branded products, such as Fortovase and Invirase. Patents in key markets have expired or are near expiry, supporting the presence of existing generic competition. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> of saquinavir in both rats and mice is >5 g/kg. Data regarding overdose with saquinavir are limited. No acute toxicities or sequelae were noted in a patient ingesting 8 grams of saquinavir as a single dose, and a second subject ingesting 2.4 grams as a single dose experienced throat pain that lasted for 6 hours and subsequently resolved. Treatment of overdose should consist of symptomatic and supportive measures. Dialysis is unlikely to be of benefit given saquinavir's extensive protein-binding. |
|---|
High Level Warnings:
- Saquinavir demonstrates low acute toxicity with oral LD50 values exceeding 5 g/kg in rodent models
- Limited clinical data indicate mild transient adverse effects upon high single-dose exposure
- Due to extensive protein binding, dialysis is not considered effective for saquinavir overdose management
Saquinavir 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.
