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Elvucitabine | CAS No: 181785-84-2 | GMP-certified suppliers

A medication that is investigated for treating HIV infection and hepatitis B by inhibiting viral replication through nucleoside reverse transcriptase inhibition.

Therapeutic categories

Anti-HIV AgentsAnti-Infective AgentsAnti-Retroviral AgentsAntiviral AgentsDeoxycytidineDeoxyribonucleosides
Generic name
Elvucitabine
Molecule type
small molecule
CAS number
181785-84-2
DrugBank ID
DB06236
Approval status
Investigational drug

Primary indications

  • Investigated for use/treatment in hepatitis (viral, B) and HIV infection

Product Snapshot

  • Elvucitabine is an oral small molecule nucleoside reverse transcriptase inhibitor
  • It is primarily investigated for antiviral applications targeting hepatitis B virus and HIV infections
  • The compound remains in the investigational stage without current FDA or EMA approval

Clinical Overview

Elvucitabine (CAS Number 181785-84-2) is a nucleoside analogue belonging to the class of nucleoside and nucleotide analogues. It is structurally related to L-cytosine and functions as a nucleoside reverse transcriptase inhibitor (NRTI). Elvucitabine has been investigated primarily for its potential antiviral activity against human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections.

The mechanism of action of elvucitabine involves inhibition of the viral RNA-directed DNA polymerase, commonly known as reverse transcriptase. By competing with natural nucleosides, elvucitabine incorporates into the viral DNA chain during reverse transcription, leading to chain termination and preventing production of proviral DNA necessary for viral replication. As a result, the propagation of HIV is suppressed but not eradicated, as NRTIs are virustatic agents rather than virucidal.

Pharmacokinetic details such as absorption, distribution, metabolism, and excretion (ADME) parameters for elvucitabine have not been extensively characterized in publicly available literature, reflecting its investigative status. However, like other NRTIs, intracellular phosphorylation to the active triphosphate form is essential for its antiviral activity. Elvucitabine has been evaluated in clinical settings but remains an investigational compound without regulatory approval or marketed formulations.

Safety and toxicity profiles remain incompletely defined. Given its pharmacological class, potential adverse effects might include mitochondrial toxicity, lactic acidosis, and hepatic concerns, which are common considerations with nucleoside reverse transcriptase inhibitors. Close monitoring and comprehensive evaluation are necessary in clinical trials to establish its tolerance and safety margins.

No notable brand names are currently associated with elvucitabine due to its investigational classification. Its development focuses on treatment-resistant HIV and co-infections involving hepatitis B virus.

For pharmaceutical formulation scientists and API sourcing professionals, ensuring high purity and consistent quality standards is critical when procuring elvucitabine. Quality control should involve comprehensive identity testing, impurity profiling, and stability assessment aligned with regulatory guidelines to support investigational use. Reliable synthetic routes and robust supply chain validation are important considerations given the compound’s complexity and developmental status.

Identification & chemistry

Generic name Elvucitabine
Molecule type Small molecule
CAS 181785-84-2
UNII M09BUF90C0
DrugBank ID DB06236

Pharmacology

SummaryElvucitabine is a nucleoside reverse transcriptase inhibitor (NRTI) that targets HIV reverse transcriptase, disrupting viral RNA-directed DNA polymerase activity. By inhibiting reverse transcriptase, it impairs the conversion of viral RNA into DNA, blocking viral replication. Elvucitabine demonstrates virustatic effects without eradicating HIV, and has also been investigated for hepatitis B treatment.
Mechanism of actionElvucitabine is a L-cytosine Nucleoside analog Reverse Transcriptase Inhibitor (NRTIs) anti-HIV drug. NRTI's inhibit the activity of viral RNA-directed DNA polymerase (i.e., reverse transcriptase). It is believed that inhibition of reverse transcriptase interferes with the generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes subsequently eliminate the HIV particle that previously had been uncoated, and left unprotected, during entry into the host cell. Thus, reverse transcriptase inhibitors are virustatic and do not eliminate HIV from the body.
Targets
TargetOrganismActions
Reverse transcriptase/RNaseHHuman immunodeficiency virus 1inhibitor

Formulation & handling

  • Elvucitabine is a small molecule nucleoside analogue intended for oral formulation due to its physicochemical properties.
  • Its moderate water solubility supports aqueous formulation but requires consideration for stability in liquid media.
  • Handling precautions should include protection from moisture and light to maintain compound integrity during storage.

Regulatory status

Elvucitabine 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.