Entecavir Monohydrate Antiviral API CAS 209216-23-9 scientific research use

Entecavir Monohydrate (CAS 209216-23-9) is a potent and selective nucleoside analogue with significant antiviral activity against hepatitis B virus (HBV). It is the monohydrate crystalline form of Entecavir, a synthetic guanosine analogue with the molecular formula C₁₂H₁₅N₅O₃·H₂O and a molecular weight of 295.29 g/mol. As an active pharmaceutical ingredient (API), it serves as a first-line treatment for chronic hepatitis B.

Pharmacological Profile & Clinical Studies:

• Mechanism of Action: Entecavir is a deoxyguanosine nucleoside analogue that is efficiently phosphorylated intracellularly to its active 5′-triphosphate form. The active triphosphate competes with the natural substrate deoxyguanosine triphosphate (dGTP), inhibiting the HBV polymerase (reverse transcriptase) at three distinct stages: base priming, reverse transcription of the negative strand from the pregenomic messenger RNA, and synthesis of the positive strand of HBV DNA. Importantly, Entecavir exhibits no significant activity against HIV-1, influenza, or herpes simplex viruses at clinically relevant concentrations.

• Potent Antiviral Activity: Entecavir is a highly potent inhibitor of wild-type HBV polymerase, with an EC₅₀ of 3.75 nM in HepG2 cells. It is 100- to 300-fold more potent than lamivudine triphosphate against lamivudine-resistant HBV Pol mutants. The intracellular half-life of Entecavir is approximately 15 hours, supporting once-daily dosing.

• Clinical Efficacy: In clinical trials, Entecavir has demonstrated superior virological, biochemical, and histological outcomes compared to lamivudine in both nucleoside-naïve and lamivudine-refractory patients with chronic hepatitis B. Daily oral administration at doses ranging from 0.02 to 0.5 mg/kg for 1 to 3 months effectively reduces woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks.

• Drug Resistance: Resistance to Entecavir requires multiple substitutions in the HBV polymerase, specifically at residues M204V/I and L180M, in addition to T184, S202, or M250 changes. The high genetic barrier to resistance makes Entecavir a robust long-term treatment option.

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Product Applications:

• Pharmaceutical Manufacturing: As a high-quality API for the production of Entecavir-containing antiviral formulations for chronic hepatitis B

• Analytical R&D: Serves as a reference standard for quality control (QC), analytical method development and validation (AMV), and impurity profiling studies

• Regulatory Submissions: Used as a reference standard in ANDA and DMF filings for HBV antiviral drugs

• Antiviral Research: Suitable for use in HBV replication studies, combination therapy research, and drug resistance mechanism investigations

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Packaging: ___ (e.g.: 1g, 5g, 10g per package, as per customer's request)

Storage: Store in a cool, dry, well-ventilated area, away from direct sunlight and moisture. Recommended storage temperature: below 15°C (cool and dark place). For long-term storage, 2-8°C (Refrigerator) is recommended.

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