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Darunavir | CAS No: 206361-99-1 | GMP-certified suppliers
A medication that supports effective treatment of HIV‑1 infection in adults and children when used with other antiretroviral agents, including resistant cases.
Therapeutic categories
AmidesAnti-HIV AgentsAnti-Infective AgentsAnti-Retroviral AgentsAntiinfectives for Systemic UseAntiviral Agents
Generic name
Darunavir
Molecule type
small molecule
CAS number
206361-99-1
DrugBank ID
DB01264
Approval status
Approved drug
ATC code
J05AR14
Primary indications
- Darunavir, co-administered with ritonavir, and with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV) in children age 3 or above and adults with HIV-1 infection
Product Snapshot
- Darunavir is an oral small‑molecule antiviral supplied mainly as tablets and suspensions for co-formulation in combination regimens
- It is used for HIV‑1 management as part of boosted antiretroviral therapy
- It is approved in the US, EU, and Canada
Clinical Overview
Darunavir (CAS 206361-99-1) is an HIV-1 protease inhibitor indicated for use with ritonavir and other antiretroviral agents in adults and children aged three years and older with HIV‑1 infection. As a second‑generation agent within the aminobenzenesulfonamide class, it was developed to maintain activity against strains with resistance to earlier protease inhibitors. Darunavir has also been investigated in vitro and in early clinical research for activity against SARS‑CoV‑2, although its clinical relevance in this context has not been established.
Darunavir exerts antiviral activity by tightly binding to the HIV‑1 protease active site and preventing cleavage of Gag‑Pol precursor proteins. This inhibition blocks viral maturation and reduces the production of infectious virions. The compound interacts with key catalytic residues, including Asp‑29 and Asp‑30, and its molecular flexibility allows accommodation of certain protease mutations, supporting its use in resistant HIV‑1 variants.
When boosted with ritonavir, darunavir achieves pharmacologically sustained plasma concentrations due to reduced CYP3A-mediated metabolism. The drug is a CYP3A substrate and can also inhibit multiple cytochrome P450 isoenzymes and transporters, including CYP3A4, CYP2D6, OATP1B1, and P‑glycoprotein. These properties contribute to a high potential for clinically significant drug–drug interactions. Darunavir is primarily eliminated hepatically, and exposure increases in hepatic impairment.
Key safety considerations include hepatotoxicity risk, dyslipidemia, rash, and effects associated with immune reconstitution. Use requires monitoring for interactions with CYP3A substrates or strong inducers. Co-administration with ritonavir or cobicistat is required to achieve therapeutic concentrations.
Darunavir is marketed globally in fixed-dose combinations and as standalone formulations for use in combination antiretroviral therapy.
For API procurement, sourcing from manufacturers with demonstrated control of stereochemistry, impurity profiles, and particle characteristics is essential. Compliance with ICH guidelines, validated process controls, and transparent regulatory documentation supports reliable formulation development and global regulatory submissions.
Darunavir exerts antiviral activity by tightly binding to the HIV‑1 protease active site and preventing cleavage of Gag‑Pol precursor proteins. This inhibition blocks viral maturation and reduces the production of infectious virions. The compound interacts with key catalytic residues, including Asp‑29 and Asp‑30, and its molecular flexibility allows accommodation of certain protease mutations, supporting its use in resistant HIV‑1 variants.
When boosted with ritonavir, darunavir achieves pharmacologically sustained plasma concentrations due to reduced CYP3A-mediated metabolism. The drug is a CYP3A substrate and can also inhibit multiple cytochrome P450 isoenzymes and transporters, including CYP3A4, CYP2D6, OATP1B1, and P‑glycoprotein. These properties contribute to a high potential for clinically significant drug–drug interactions. Darunavir is primarily eliminated hepatically, and exposure increases in hepatic impairment.
Key safety considerations include hepatotoxicity risk, dyslipidemia, rash, and effects associated with immune reconstitution. Use requires monitoring for interactions with CYP3A substrates or strong inducers. Co-administration with ritonavir or cobicistat is required to achieve therapeutic concentrations.
Darunavir is marketed globally in fixed-dose combinations and as standalone formulations for use in combination antiretroviral therapy.
For API procurement, sourcing from manufacturers with demonstrated control of stereochemistry, impurity profiles, and particle characteristics is essential. Compliance with ICH guidelines, validated process controls, and transparent regulatory documentation supports reliable formulation development and global regulatory submissions.
Identification & chemistry
| Generic name | Darunavir |
|---|---|
| Molecule type | Small molecule |
| CAS | 206361-99-1 |
| UNII | YO603Y8113 |
| DrugBank ID | DB01264 |
Pharmacology
| Summary | Darunavir is an HIV‑1 protease inhibitor that blocks protease dimerization and catalytic activity, preventing cleavage of viral Gag‑Pol precursor proteins. This interruption halts maturation of infectious virions and reduces viral replication, including in strains with certain resistance‑associated mutations. Its pharmacodynamic effect is characterized by substantial suppression of HIV‑1 when used in combination antiretroviral regimens. |
|---|---|
| Mechanism of action | The HIV-1 protease enzyme is necessary for viral precursor protein processing and viral maturation in preparation for infection, and is therefore a target for antiretroviral therapy for HIV. Protease inhibitors are used as a part of highly active antiretroviral therapy (HAART) in patients diagnosed with HIV infection. It has been shown to effectively suppress the virus, leading to significantly decreased morbidity and mortality rates. Darunavir, a HIV protease inhibitor, prevents HIV replication through binding to the enzyme, stopping the dimerization and the catalytic activity of HIV-1 protease. In particular, it inhibits the cleavage of HIV encoded Gag-Pol proteinsin cells that have been infected with the virus, halting the formation of mature virus particles, which spread the infection. The close contact that darunavir makes with the primary chains of the active site amino acids (Asp-29 and Asp-30) on the protease likely contributes to its potency and efficacy against resistant variants of HIV-1. Darunavir is known to bind to different sites on the enzyme: the active site cavity and the surface of one of the flexible flaps in the protease dimer. Darunavir can adapt to changes in the shape of a protease enzyme due to its molecular flexibility. |
| Pharmacodynamics | Darunavir is an inhibitor of the human immunodeficiency virus (HIV) protease, which prevents HIV viral replication.When administered with ritonavir in combination antiretroviral therapy, darunavir significantly decreases viral load and increases CD4 cell counts, decreasing the morbidity and mortality of HIV infection. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Human immunodeficiency virus type 1 protease | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | The absolute oral bioavailability of one single 600 mg dose of darunavir alone and with 100 mg of ritonavir twice a day was 37% and 82%, respectively.Exposure to darunavir in boosted patients has been found to be 11 times higher than in unboosted patients.Tmax is achieved approximately 2.4 to 4 hours after oral administration. When darunavir is taken with food, the Cmax and AUC of darunavir given with ritonavir increase by 30% when compared to the fasted state. |
|---|---|
| Half-life | The terminal elimination half-life of darunavir is approximately 15 hours when it is combined with ritonavir. |
| Protein binding | Darunavir is approximately 95% bound to plasma proteins. Darunavir binds primarily to plasma alpha 1-acid glycoprotein (AAG). |
| Metabolism | Darunavir is heavily oxidized and metabolized by hepatic cytochrome enzymes, mainly CYP3A.Darunavir is extensively metabolized in subjects who do not receive a booster, primarily via carbamate hydrolysis, isobutyl aliphatic hydroxylation, and aniline aromatic hydroxylation, as well as both benzylic aromatic hydroxylation and glucuronidation. |
| Route of elimination | A mass balance study in healthy volunteers demonstrated that after single dose administration of 400 mg 14C-darunavir, given with 100 mg ritonavir, approximately 79.5% and 13.9% of the administered dose of radiolabeled darunavir was obtained in the feces and urine, respectively. Excretion of unchanged drug accounted for 8.0% of the darunavir dose in volunteers who were unboosted. In boosted darunavir administration, unchanged darunavir made up 48.8% of the excreted dose in boosted subjects due to inhibition of darunavir metabolism by ritonavir. Unchanged drug in the urine made up 1.2% of the administered dose in volunteers who where unboosted, and 7.7% in boosted volunteers. |
| Volume of distribution | The volume of distribution of darunavir in one pharmacokinetic study in conjunction with ritonavir was 206.5 L (with a range of 161.0–264.9) in healthy young adult volunteers.Another pharmacokinetic study revealed a volume of distribution of 220 L. |
| Clearance | Darunavir has a low renal clearance.After intravenous administration, the clearance darunavir administered alone and with 100 mg ritonavir twice daily, was 32.8 L/h and 5.9 L/h, respectively. |
Formulation & handling
- Oral small‑molecule protease inhibitor with low aqueous solubility, typically requiring solubility‑enhancing excipients for tablet and suspension formulations.
- Food enhances absorption, so formulations are designed to support administration with meals and mitigate variability in gastrointestinal uptake.
- Solid-state handling is straightforward, but attention to particle size control and dispersion is needed for consistent bioavailability in high‑load oral dosage forms.
Regulatory status
| Lifecycle | Core US patents expired between 2012 and 2016, with the last Canadian patent expiring in 2022, indicating that the active ingredient is now largely in a post‑expiry phase. With products marketed in Canada, the US, and the EU, the market is mature and likely characterized by established generic competition. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Darunavir’s supply landscape includes an established originator manufacturer with multiple repackagers and distributors supporting downstream availability. Branded formulations are marketed across the US, EU, and Canada, indicating broad global presence. With key US and Canadian patents already expired, the product is positioned for existing or expanding generic competition. |
|---|
Safety
| Toxicity | LD50 information for darunavir is not readily available in the literature.One-time doses of up to 3,200 mg of darunavir in an oral solution and up to 1,600 mg of the tablet formulation of darunavir with ritonavir have been given volunteers without significant symptoms. Information about an overdose with darunavir with ritonavir is limited. No specific antidote exists for this drug. Treatment of In the case of an overdose, employ general supportive measures. Monitor vital signs and clinical status. It is unlikely that darunavir not amenable to removal by dialysis due to its high level of protein binding. |
|---|
High Level Warnings:
- High oral doses (up to 3,200 mg solution
- 1,600 mg tablet with ritonavir) have shown low acute toxicity in volunteers, with no significant symptoms reported
- Extensive plasma protein binding suggests the compound is unlikely to be removed by dialysis and may exhibit prolonged systemic retention in overdose scenarios
Darunavir 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.
Frequently asked questions about Darunavir API
Sourcing
What matters most when sourcing GMP-grade Darunavir?
Key considerations include confirming that the API is manufactured under GMP and meets the regulatory expectations of Canada, the US, and the EU. It is also important to verify that the supplier has a reliable position within the established supply chain, which includes the originator manufacturer and multiple repackagers and distributors. Given expired patents in the US and Canada, ensuring clarity on the supplier’s authorization and product status within a competitive generic landscape is essential.
Which documents are typically required when sourcing Darunavir API?
Request the core API documentation set: CoA (14 companies), USDMF (10 companies), GMP (8 companies), WC (7 companies), ISO9001 (1 company). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Darunavir API?
Known or reported manufacturers for Darunavir: SETV Global, Sinoway industrial Co.,Ltd. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Darunavir API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Darunavir manufacturers?
Audit reports may be requested for Darunavir: 9 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Darunavir API on Pharmaoffer?
Reported supplier count for Darunavir: 14 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Darunavir API?
Production countries reported for Darunavir: India (10 producers), China (3 producers). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Darunavir usually hold?
Common certifications for Darunavir suppliers: CoA (14 companies), USDMF (10 companies), GMP (8 companies), WC (7 companies), ISO9001 (1 company). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Darunavir (CAS 206361-99-1) used for?
Darunavir is used with ritonavir and other antiretroviral agents to treat HIV‑1 infection in adults and children aged three years and older. It inhibits the HIV‑1 protease, blocking viral maturation and helping suppress replication, including in some resistant strains. It has also been studied for activity against SARS‑CoV‑2, but its clinical relevance for this purpose has not been established.
Which therapeutic class does Darunavir fall into?
Darunavir belongs to the following therapeutic categories: Amides, Anti-HIV Agents, Anti-Infective Agents, Anti-Retroviral Agents, Antiinfectives for Systemic Use. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Darunavir mainly prescribed for?
The primary indications for Darunavir: Darunavir, co-administered with ritonavir, and with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV) in children age 3 or above and adults with HIV-1 infection. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Darunavir work?
The HIV-1 protease enzyme is necessary for viral precursor protein processing and viral maturation in preparation for infection, and is therefore a target for antiretroviral therapy for HIV. Protease inhibitors are used as a part of highly active antiretroviral therapy (HAART) in patients diagnosed with HIV infection. It has been shown to effectively suppress the virus, leading to significantly decreased morbidity and mortality rates.
Darunavir, a HIV protease inhibitor, prevents HIV replication through binding to the enzyme, stopping the dimerization and the catalytic activity of HIV-1 protease. In particular, it inhibits the cleavage of HIV encoded Gag-Pol proteinsin cells that have been infected with the virus, halting the formation of mature virus particles, which spread the infection. The close contact that Darunavir makes with the primary chains of the active site amino acids (Asp-29 and Asp-30) on the protease likely contributes to its potency and efficacy against resistant variants of HIV-1.
Darunavir is known to bind to different sites on the enzyme: the active site cavity and the surface of one of the flexible flaps in the protease dimer. Darunavir can adapt to changes in the shape of a protease enzyme due to its molecular flexibility.
What should someone know about the safety or toxicity profile of Darunavir?
Darunavir has a generally low acute toxicity profile, with high oral doses in volunteers producing no notable symptoms. Key risks include hepatotoxicity, dyslipidemia, rash, and immune‑reconstitution effects, which warrant routine clinical monitoring. Because it is highly protein‑bound, it is unlikely to be removed by dialysis and may persist longer in overdose. Its inhibition of multiple CYP enzymes and transporters contributes to a high potential for drug–drug interactions.
What are important formulation and handling considerations for Darunavir as an API?
Important considerations include managing Darunavir’s low aqueous solubility by using solubility‑enhancing excipients and controlling particle size to support consistent dispersion and bioavailability. Formulations are typically designed for administration with food to reduce variability in gastrointestinal absorption. For high‑load oral dosage forms, uniform blending and solid‑state stability should be maintained. Handling should ensure protection from moisture and support reliable downstream processing.
Is Darunavir a small molecule?
Darunavir is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Darunavir?
Oral Darunavir has no unusual solid‑state stability issues, but its low aqueous solubility requires attention to physical stability in formulated products. Maintaining controlled particle size and adequate dispersion is important to ensure consistent bioavailability, particularly in high‑load tablets or suspensions. Formulations are also designed to remain stable while supporting administration with food, which affects absorption.
Regulatory
Where is Darunavir approved or in use globally?
Darunavir is reported as approved in the following major regions: Canada, US, EU. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Darunavir right now?
Darunavir is authorized for use in Canada, the United States, and the European Union. Its regulatory status in these regions reflects established review and approval pathways for antiretroviral agents. Patent protection varies by jurisdiction and by specific formulations or uses, and current status is determined through national or regional patent offices. For accurate patent details, reference the applicable patent registries.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Darunavir procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Darunavir. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Darunavir included in the PRO Data Insights coverage?
PRO Data Insights coverage for Darunavir: 843 verified transactions across 179 suppliers and 97 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Darunavir?
Market report availability for Darunavir: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
