Category:
Other Antibiotics
CAS NO:
142217-69-4
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Basic Info
CAS Number
142217-69-4
Pharmacopoeia
In-house Standards
Grade
Pharmaceutical Grade
Is Manufacturer
No
Samples Provided
NO
Product Description
-
AI Product Description
*The following content is generated by AI and is for reference only.
Entecavir, chemically designated as 9-[(1R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl]guanine, is a potent antiviral medication primarily utilized in the management of chronic hepatitis B virus (HBV) infection. With the molecular formula C8H11N5O3 and a CAS registry number of 130697-18-6, this synthetic nucleoside analogue functions by specifically inhibiting viral DNA polymerase, also known as reverse transcriptase. This mechanism effectively blocks both the priming of HBV DNA synthesis and its subsequent elongation, thereby preventing viral replication without significantly affecting human cellular DNA polymerases at therapeutic concentrations.
Clinically, Entecavir is indicated for adults with compensated liver disease who exhibit evidence of active viral replication and ongoing inflammation or fibrosis. It has also been approved for patients with decompensated liver disease, although caution is required regarding potential lactic acidosis. The drug demonstrates high specificity for the HBV polymerase enzyme, resulting in a robust antiviral effect that leads to significant reductions in serum HBV DNA levels and normalization of liver enzymes. Its high barrier to resistance makes it particularly valuable for treatment-naive patients, though prior exposure to lamivudine may reduce efficacy due to cross-resistance mutations.
Pharmacokinetically, Entecavir exhibits rapid absorption following oral administration, with peak plasma concentrations reached within one hour. Food intake can slightly delay absorption but does not significantly alter overall bioavailability, though administration on an empty stomach is recommended for optimal results. The drug is eliminated primarily unchanged by renal excretion via glomerular filtration and active tubular secretion, necessitating dosage adjustments in patients with impaired kidney function. Common side effects include headache, fatigue, dizziness, and nausea, while rare but serious adverse events involve lactic acidosis and severe hepatomegaly with steatosis. As a cornerstone therapy in modern hepatology, Entecavir offers a favorable safety profile and sustained viral suppression, contributing to improved long-term outcomes for individuals living with chronic hepatitis B.
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