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USDMF
CoA
Producer
Produced in
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Audit Report:
Certifications:
USDMF
|
CoAAll certificates
USDMF
CoA
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India|
Audit Report:
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CoAAll certificates
USDMF
CoA
Producer
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Audit Report:
Certifications:
USDMF
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CoAAll certificates
USDMF
CoA
Producer
Produced in
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Audit Report:
Certifications:
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CoAAll certificates
USDMF
CoA
Producer
Produced in
India|
Audit Report:
Certifications:
USDMF
|
CoAAll certificates
USDMF
CoA
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Dolutegravir | CAS No: 1051375-16-6 | GMP-certified suppliers
A medication that supports HIV‑1 treatment in adults and adolescents by enabling effective combination therapy and maintaining viral suppression across major global markets.
Therapeutic categories
Anti-HIV AgentsAnti-Infective AgentsAnti-Retroviral AgentsAntiinfectives for Systemic UseAntiviral AgentsAntivirals for Systemic Use
Generic name
Dolutegravir
Molecule type
small molecule
CAS number
1051375-16-6
DrugBank ID
DB08930
Approval status
Approved drug
ATC code
J05AR27
Primary indications
- Dolutegravir is indicated in combination with other antiretroviral agents for the treatment of patients with HIV-1 infection that comply with the characteristics of being adults or children aged 12 years and older and present at least a weight of 40 kg
- The FDA combination therapy approval of dolutegravir and [rilpivirine] is indicated for adults with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy
- Dolutegravir is also available in combination with [lamivudine] and [abacavir] for the treatment of adult and pediatric patients with HIV-1 who weigh ≥10kg
Product Snapshot
- Oral small‑molecule antiretroviral supplied primarily as film‑coated tablets and tablets for suspension
- Used in combination regimens for HIV‑1 management in adult and pediatric populations
- Approved in major regulated markets including the US, Canada, and the EU
Clinical Overview
Dolutegravir (CAS 1051375-16-6) is an HIV‑1 integrase strand transfer inhibitor used in combination antiretroviral therapy for adults and adolescents. It is indicated for patients aged 12 years and older weighing at least 40 kg and is also available in fixed‑dose combinations with lamivudine and abacavir for patients weighing 10 kg or more. When co‑formulated with rilpivirine, it is approved for adults with virologic suppression under defined stability and resistance criteria.
Dolutegravir selectively inhibits the HIV‑1 integrase enzyme by binding to its active site and preventing the strand transfer step required for integration of viral DNA into host chromosomal DNA. In cell‑based assays, mean EC50 values range from approximately 0.5 to 2.1 nM. This targeted mechanism has no known human homologs. The drug demonstrates tight integrase binding and a slow dissociative half‑life, contributing to a high barrier to resistance.
Pharmacodynamic studies show rapid, dose‑dependent declines in HIV‑1 RNA with effects persisting for several days after dosing cessation. Clinical investigations of the dolutegravir and rilpivirine two‑drug regimen have shown maintenance of viral suppression comparable to three‑drug regimens in appropriately selected patients.
Dolutegravir is metabolized primarily via UGT1A1, with contributions from UGT1A3, UGT1A9, and CYP3A. It is a substrate for transporters including P‑glycoprotein and BCRP. The compound exhibits moderate oral bioavailability and is commonly administered once daily, although actual dosing depends on co‑administered agents and resistance status. Elimination occurs through hepatic metabolism with minimal renal clearance of unchanged drug.
Safety considerations include attention to potential drug interactions involving UGT or transporter pathways. Reported adverse effects in clinical use have generally been consistent with other antiretroviral agents, though monitoring is recommended when used with interacting medications.
From a sourcing perspective, procurement of dolutegravir API requires verification of impurity controls, consistent polymorphic form, and compliance with regional pharmacopoeial and regulatory specifications to support global formulation and submission needs.
Dolutegravir selectively inhibits the HIV‑1 integrase enzyme by binding to its active site and preventing the strand transfer step required for integration of viral DNA into host chromosomal DNA. In cell‑based assays, mean EC50 values range from approximately 0.5 to 2.1 nM. This targeted mechanism has no known human homologs. The drug demonstrates tight integrase binding and a slow dissociative half‑life, contributing to a high barrier to resistance.
Pharmacodynamic studies show rapid, dose‑dependent declines in HIV‑1 RNA with effects persisting for several days after dosing cessation. Clinical investigations of the dolutegravir and rilpivirine two‑drug regimen have shown maintenance of viral suppression comparable to three‑drug regimens in appropriately selected patients.
Dolutegravir is metabolized primarily via UGT1A1, with contributions from UGT1A3, UGT1A9, and CYP3A. It is a substrate for transporters including P‑glycoprotein and BCRP. The compound exhibits moderate oral bioavailability and is commonly administered once daily, although actual dosing depends on co‑administered agents and resistance status. Elimination occurs through hepatic metabolism with minimal renal clearance of unchanged drug.
Safety considerations include attention to potential drug interactions involving UGT or transporter pathways. Reported adverse effects in clinical use have generally been consistent with other antiretroviral agents, though monitoring is recommended when used with interacting medications.
From a sourcing perspective, procurement of dolutegravir API requires verification of impurity controls, consistent polymorphic form, and compliance with regional pharmacopoeial and regulatory specifications to support global formulation and submission needs.
Identification & chemistry
| Generic name | Dolutegravir |
|---|---|
| Molecule type | Small molecule |
| CAS | 1051375-16-6 |
| UNII | DKO1W9H7M1 |
| DrugBank ID | DB08930 |
Pharmacology
| Summary | Dolutegravir is an HIV‑1 integrase inhibitor that binds the enzyme’s active site and blocks the strand‑transfer step required for viral DNA integration. This action produces potent suppression of viral replication and is associated with sustained antiviral activity due to slow dissociation from the integrase‑DNA complex. Its pharmacodynamic profile supports a high barrier to resistance when used as part of combination antiretroviral therapy. |
|---|---|
| Mechanism of action | Dolutegravir is an HIV-1 antiviral agent. It inhibits HIV integrase by binding to the active site and blocking the strand transfer step of retroviral DNA integration in the host cell. The strand transfer step is essential in the HIV replication cycle and results in the inhibition of viral activity. Dolutegravir has a mean EC50 value of 0.5 nM (0.21 ng/mL) to 2.1 nM (0.85 ng/mL) in peripheral blood mononuclear cells (PBMCs) and MT-4 cells. |
| Pharmacodynamics | HIV-1 infected subjects on dolutegravir monotherapy demonstrated rapid and dose-dependent reduction of antiviral activity with declines of HIV-1 RNA copies per ml. The antiviral response was maintained for 3 to 4 days after the last dose.The sustained response obtained in clinical trials indicates that dolutegravir has a tight binding and longer dissociative half-life providing it a high barrier to resistance.The combination therapy (ripivirine and dolutegravir) presented the same viral suppression found in previous three-drug therapies without integrase strand transfer inhibitor mutations or rilpivirine resistance. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Integrase | Human immunodeficiency virus 1 | inhibitor |
ADME / PK
| Absorption | When 50 mg of dolutegravir once daily was orally administered to HIV-1 infected adults, the AUC, Cmax, and Cmin is 53.6 mcg h/mL, 3.67 mcg/mL, and 1.11 mcg/mL, respectively. The peak plasma concentration was observed 2 to 3 hours post-dose. Steady state is achieved within approximately 5 days with average accumulation ratios for AUC, Cmax, and C24h ranging from 1.2 to 1.5. When 50 mg once daily is given to pediatric patients (12 to < 18 years and weighing ≥40 kg) the Cmax, AUC, and C24 is 3.49 mcg/mL, 46 mcg.h/mL, and 0.90 mcg/mL respectively. |
|---|---|
| Half-life | The half-life of dolutegravir is 14 hours. |
| Protein binding | Dolutegravir is highly protein bound to human plasma proteins reaching a percentage 98.9% of the administered dose. |
| Metabolism | Dolutegravir is highly metabolized through three main pathways and it forms no long-lived metabolites. The first pathway is defined by the glucuronidation by UGT1A1, the second pathway by carbon oxidation by CYP3A4 and the third pathway is what appears to be a sequential oxidative defluorination and glutathione conjugation. The main metabolite found in blood plasma is the ether glucuronide form (M2) and its chemical properties disrupt its ability to bind metal ions, therefore, it is inactive. |
| Route of elimination | When a single oral dose of dolutegravir is given, nearly all complete dose is recovered in a proportion of 53% excreted unchanged in the feces and 31% excreted in urine. The renal eliminated recovered dose consists of ether glucuronide of dolutegravir (18.9%), a metabolite formed by oxidation at the benzylic carbon (3.0%), a hydrolytic N-dealkylation product (3.6%) and unchanged drug (< 1%). |
| Volume of distribution | The administration of a dose of 50 mg of dolutegravir presents an apparent volume of distribution of 17.4 L. The median dolutegravir concentration in CSF was 18 ng/mL after 2 weeks of treatment. |
| Clearance | The apparent clearance rate of dultegravir is 1.0 L/h.[FDA label] |
Formulation & handling
- Oral small‑molecule integrase inhibitor with low aqueous solubility, typically formulated as solid tablets or tablets for suspension.
- Absorption is affected by multivalent cations, requiring separation strategies in formulations to limit chelation risk.
- Food can increase exposure, but the API is generally stable and suitable for standard solid‑dose handling conditions.
Regulatory status
| Lifecycle | Most US patent protections for the API have expired, with remaining coverage extending to 2028 and 2030, indicating a transition toward later‑stage market maturity. With availability in the US, Canada, and the EU, the ingredient is positioned in a broadly established market as remaining exclusivities near expiry. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Dolutegravir is produced primarily by a single originator group, with branded formulations marketed across the United States, Canada, and the European Union. While several earlier U.S. patents have expired, key protections remain active through 2028–2030, which limits broad generic entry in major markets until those dates. Existing expiries may support some regional or future pipeline activity, but large‑scale generic competition is largely constrained by the remaining patents. |
|---|
Safety
| Toxicity | Data from an ongoing birth outcome surveillance study has identified an increased risk of neural tube defects when dolutegravir is administered at the time of conception. As defects related to the closure of the neural tube occur from conception through the first 6 weeks of gestation, embryos exposed to dolutegravir from the time of conception through the first 6 weeks of gestation are at potential risk. Advise adolescents and adults of childbearing potential, including those actively trying to become pregnant, of the potential risk of neural tube defects with the use of TIVICAY and TIVICAY PD. Assess the risks and benefits of TIVICAY and TIVICAY PD and discuss with the patient to determine if an alternative treatment should be considered at the time of conception through the first trimester of pregnancy or if pregnancy is confirmed in the first trimester. A benefit-risk assessment should consider factors such as the feasibility of switching to another antiretroviral regimen, tolerability, ability to maintain viral suppression, and risk of HIV-1 transmission to the infant against the risk of neural tube defects associated with in-utero dolutegravir exposure during critical periods of fetal development [see Warnings and Precautions (5.3)]. There are insufficient human data on the use of dolutegravir during pregnancy to definitively assess a drug-associated risk for birth defects and miscarriage. The background risk for major birth defects for the indicated population is unknown. In the U.S. general population, the estimated background rate for major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. In animal reproduction studies, no evidence of adverse developmental outcomes was observed with dolutegravir at systemic exposures (AUC) less than (rabbits) and approximately 27 times (rats) the exposure in humans at the maximum recommended human dose (MRHD) of TIVICAY (see Data). There is no known specific treatment for an overdose with TIVICAY or TIVICAY PD. If an overdose occurs, the patient should be monitored, and standard supportive treatment applied as required. As dolutegravir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by dialysis. |
|---|
High Level Warnings:
- Embryonic exposure to dolutegravir during conception through the first 6 weeks of gestation has been associated with an increased incidence of neural tube defects in human surveillance data
- No developmental toxicity was observed in animal studies at exposures up to ~27-fold the human MRHD
- However, human data remain insufficient to define a definitive teratogenic risk profile
Dolutegravir 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.
Dolutegravir API manufacturers & distributors
Compare qualified Dolutegravir API suppliers worldwide. We currently have 13 companies offering Dolutegravir 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 |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Hangzhou Coben Pharmaceut... | Producer | China | China | CoA, GMP, ISO9001 | 7 products |
| Hetero Labs | Producer | India | India | CoA, USDMF | 90 products |
| Laurus Labs | Producer | India | India | CoA, GMP, USDMF, WC | 50 products |
| Lek Pharma | Producer | Slovenia | India | CoA, USDMF | 32 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| MSN Life Sciences | Producer | India | India | CoA, USDMF | 46 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Shanghai Acebright | Producer | China | China | CoA | 23 products |
| Shanghai Desano Chem. | Producer | China | China | CoA, USDMF | 22 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 66 products |
When sending a request, specify which Dolutegravir 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 Dolutegravir 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.
Frequently asked questions about Dolutegravir API
Sourcing
What matters most when sourcing GMP-grade Dolutegravir?
Key considerations include ensuring the API meets GMP requirements aligned with U.S., Canadian, and EU regulatory standards. Supply planning is important because production is concentrated with a single originator group. Patent protections active through 2028–2030 restrict broad generic availability, which affects sourcing options and timelines.
Which documents are typically required when sourcing Dolutegravir API?
Request the core API documentation set: CoA (13 companies), USDMF (10 companies), GMP (3 companies), WC (1 company), ISO9001 (1 company). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Dolutegravir API?
Known or reported manufacturers for Dolutegravir: Tianjin Pharmacn Medical Technology Co., ltd. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Dolutegravir 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 Dolutegravir manufacturers?
Audit reports may be requested for Dolutegravir: 8 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Dolutegravir API on Pharmaoffer?
Reported supplier count for Dolutegravir: 13 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Dolutegravir API?
Production countries reported for Dolutegravir: India (9 producers), China (4 producers). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Dolutegravir usually hold?
Common certifications for Dolutegravir suppliers: CoA (13 companies), USDMF (10 companies), GMP (3 companies), WC (1 company), ISO9001 (1 company). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Dolutegravir (CAS 1051375-16-6) used for?
Dolutegravir is used as an HIV‑1 integrase strand transfer inhibitor in combination antiretroviral therapy for adults and adolescents. It is indicated for patients aged 12 years and older weighing at least 40 kg, and is available in fixed‑dose combinations with lamivudine and abacavir for patients weighing 10 kg or more. When co‑formulated with rilpivirine, it is used to maintain virologic suppression in adults who meet defined stability and resistance criteria.
Which therapeutic class does Dolutegravir fall into?
Dolutegravir belongs to the following therapeutic categories: Anti-HIV Agents, Anti-Infective Agents, Anti-Retroviral Agents, Antiinfectives for Systemic Use, Antiviral Agents. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Dolutegravir mainly prescribed for?
The primary indications for Dolutegravir: Dolutegravir is indicated in combination with other antiretroviral agents for the treatment of patients with HIV-1 infection that comply with the characteristics of being adults or children aged 12 years and older and present at least a weight of 40 kg, The FDA combination therapy approval of Dolutegravir and [rilpivirine] is indicated for adults with HIV-1 infections whose virus is currently suppressed (< 50 copies/ml) on a stable regimen for at least six months, without history of treatment failure and no known substitutions associated to resistance to any of the two components of the therapy, Dolutegravir is also available in combination with [lamivudine] and [abacavir] for the treatment of adult and pediatric patients with HIV-1 who weigh ≥10kg. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Dolutegravir work?
Dolutegravir is an HIV-1 antiviral agent. It inhibits HIV integrase by binding to the active site and blocking the strand transfer step of retroviral DNA integration in the host cell. The strand transfer step is essential in the HIV replication cycle and results in the inhibition of viral activity. Dolutegravir has a mean EC50 value of 0.5 nM (0.21 ng/mL) to 2.1 nM (0.85 ng/mL) in peripheral blood mononuclear cells (PBMCs) and MT-4 cells.
What should someone know about the safety or toxicity profile of Dolutegravir?
Dolutegravir is generally well tolerated, but human surveillance data suggest an increased incidence of neural tube defects with exposure from conception through the first 6 weeks of gestation. Animal studies did not show developmental toxicity at exposures up to about 27‑fold the human maximum recommended dose, though available human data are insufficient to define the exact teratogenic risk. Safety monitoring is advised when the drug is used with agents that affect UGT1A1 or transporter pathways. Reported adverse effects are similar to those of other antiretroviral agents.
What are important formulation and handling considerations for Dolutegravir as an API?
Dolutegravir has low aqueous solubility, so formulations typically use solid‑dose approaches that support consistent dissolution. Because absorption is reduced by chelation with multivalent cations, formulations and administration instructions should minimize contact with aluminum, magnesium, calcium, or iron. The API is generally stable under standard solid‑oral handling conditions. Food can increase exposure, but this does not usually require special formulation adjustments.
Is Dolutegravir a small molecule?
Dolutegravir is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Dolutegravir?
Dolutegravir is generally stable under standard solid‑dose manufacturing and storage conditions. Its low aqueous solubility and tendency to chelate with multivalent cations are the primary formulation considerations, requiring strategies to limit cation interaction. No additional special stability concerns are noted for typical oral tablet or tablet‑for‑suspension presentations.
Regulatory
Where is Dolutegravir approved or in use globally?
Dolutegravir is reported as approved in the following major regions: US, Canada, EU. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Dolutegravir right now?
Dolutegravir is authorized for use in the United States, Canada, and the European Union. Its patent protection is held through originator intellectual property covering the compound and related formulations, with timelines determined by national filings and standard exclusivity periods. Because patent terms differ by jurisdiction, the status is evaluated through each region’s IP registry.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Dolutegravir procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Dolutegravir. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Dolutegravir included in the PRO Data Insights coverage?
PRO Data Insights coverage for Dolutegravir: 938 verified transactions across 248 suppliers and 136 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Dolutegravir?
Market report availability for Dolutegravir: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
