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Cabotegravir
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Looking for Cabotegravir API 1051375-10-0?
- Description:
- Here you will find a list of producers, manufacturers and distributors of Cabotegravir. You can filter on certificates such as GMP, FDA, CEP, Written Confirmation and more. Send inquiries for free and get in direct contact with the supplier of your choice.
- API | Excipient name:
- Cabotegravir
- Synonyms:
- Cas Number:
- 1051375-10-0
- DrugBank number:
- DB11751
- Unique Ingredient Identifier:
- HMH0132Z1Q
General Description:
Cabotegravir, identified by CAS number 1051375-10-0, is a notable compound with significant therapeutic applications. Cabotegravir, or GSK1265744, is an HIV-1 integrase inhibitor that is prescribed with the non-nucleoside reverse transcriptase inhibitor, . Early research into cabotegravir showed it had lower oral bioavailability than , which resulted in the development of long acting monthly intramuscular injection formulation for cabotegravir. Cabotegravir was granted FDA approval on 21 January 2021 in combination with rilpivirine to treat HIV-1 infection in virologically suppressed individuals. While previously administered once monthly only, this combination product was granted FDA approval for dosing every two months on February 01, 2022 and without the need for an oral lead-in period prior.
Indications:
This drug is primarily indicated for: Oral cabotegravir is indicated in combination with for the short-term treatment of HIV-1 in virologically suppressed adults with no history of treatment failure to assess tolerability of cabotegravir or who have missed an injected dose of cabotegravir. Intramuscular extended-release cabotegravir in combination with rilpivirine is indicated as a complete regimen for the treatment of HIV-1 infection in adults and adolescents 12 years of age and older weighing at least 35 kg to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine. An extended-release injectable suspension formulation of cabotegravir is also indicated for the prevention of sexually-acquired HIV-1 infection (i.e. for pre-exposure prophylaxis, PrEP) in at-risk adults and adolescents weighing at least 35kg. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Metabolism:
Cabotegravir undergoes metabolic processing primarily in: Cabotegravir is O-glucuronidated to the M1 and M2 metabolites, with 67% of glucuronidation performed by UGT1A1, and 33% by UGT1A9. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.
Absorption:
The absorption characteristics of Cabotegravir are crucial for its therapeutic efficacy: Oral cabotegravir has a Tmax of 3 hours, reaches a Cmax of 8.0 µg/mL, and has an AUC of 145 µg\*h/mL. Intramuscular extended-release cabotegravir has a Tmax of 7 days, reaches a Cmax of 8.0 µg/mL, and has an AUC of 1591 µg\*h/mL. The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Half-life:
The half-life of Cabotegravir is an important consideration for its dosing schedule: The mean half life of oral cabotegravir is 41 hours. The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5 weeks. This determines the duration of action and helps in formulating effective dosing regimens.
Protein Binding:
Cabotegravir exhibits a strong affinity for binding with plasma proteins: Cabotegravir is >99.8% bound to proteins in plasma, usually alubmin. This property plays a key role in the drug's pharmacokinetics and distribution within the body.
Route of Elimination:
The elimination of Cabotegravir from the body primarily occurs through: An oral radiolabelled dose of cabotegravir is 58.5% recovered in the feces and 26.8% recovered in the urine. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.
Volume of Distribution:
Cabotegravir is distributed throughout the body with a volume of distribution of: Data regarding the volume of distribution of cabotegravir is not readily available. This metric indicates how extensively the drug permeates into body tissues.
Clearance:
The clearance rate of Cabotegravir is a critical factor in determining its safe and effective dosage: Data regarding the clearance of cabotegravir is not readily available. Clearance in dogs was 0.34 mL/min/kg and in cynomolgus monkeys was 0.32 mL/min/kg. It reflects the efficiency with which the drug is removed from the systemic circulation.
Pharmacodynamics:
Cabotegravir exerts its therapeutic effects through: Cabotegravir is an inhibitor of HIV integrase, which reduces viral replication. It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly. Patients should be counselled regarding the risk of hypersensitivity, hepatotoxicity, and depression. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Cabotegravir functions by: Cabotegravir binds to the active site of HIV integrase, preventing strand transfer of the viral genome into the host genome, and preventing replication of the virus. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Toxicity:
Classification:
Cabotegravir belongs to the class of organic compounds known as pyridinecarboxylic acids and derivatives. These are compounds containing a pyridine ring bearing a carboxylic acid group or a derivative thereof, classified under the direct parent group Pyridinecarboxylic acids and derivatives. This compound is a part of the Organic compounds, falling under the Organoheterocyclic compounds superclass, and categorized within the Pyridines and derivatives class, specifically within the Pyridinecarboxylic acids and derivatives subclass.
Categories:
Cabotegravir is categorized under the following therapeutic classes: Anti-HIV Agents, Anti-Infective Agents, Anti-Retroviral Agents, Antiinfectives for Systemic Use, Antiviral Agents, Antivirals for Systemic Use, BCRP/ABCG2 Substrates, Direct Acting Antivirals, Enzyme Inhibitors, HIV Integrase Inhibitors, Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor, Integrase Inhibitors, OAT1/SLC22A6 inhibitors, OAT3/SLC22A8 Inhibitors, Organic Anion Transporter 1 Inhibitors, P-glycoprotein substrates, Piperazines, Pyridines, UGT1A1 Substrates, UGT1A9 Substrates. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.
Cabotegravir 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.
