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Entecavir Tablets are an antiviral drug mainly used to treat chronic hepatitis B (HBV) infection. It is a guanine nucleoside analogue with the chemical name 2-amino-9- [(1S, 3R, 4S) -4-hydroxy-3-hydroxymethyl-2-methylcyclopentyl] -1,9-dihydro-6H-purin-6-one monohydrate. The molecular formula is C ₁ H ₁ N ₅ O ∝ · H ₂ O, with a molecular weight of 295.3. It is a thin film coated tablet and appears white after removing the coating. Suitable for active virus replication and sustained elevation of serum alanine aminotransferase (ALT). Liver histology shows active lesions (including compensated and decompensated liver disease patients). The inhibitory constant (Ki) of entecavir triphosphate on HBV DNA polymerase is 0.0012 μ M, while its inhibitory effect on cellular DNA polymerase (α, β, δ) and mitochondrial DNA polymerase γ is weak (Ki values range from 18 to 160 μ M).
Additional information of chemical compound:
| Product Name | Entecavir Tablets | Entecavir Capsules | Entecavir Injection |
| Product Type | Tablet | Capsules | liquid |
| Product Purity | ≥99% | ≥99% | ≥99% |
| Product Specifications | 0.1mg/1mg | 0.5mg | 0.1mg/2.5mg |
| Product Form | Take Orally | Take Orally | Organic synthesis |
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Entecavir COA
Entecavir Tablets, The Chinese name is entecavir, which is a widely used antiviral drug for the treatment of chronic hepatitis B (CHB). Since its launch, entecavir has become a first-line drug for the treatment of chronic hepatitis B worldwide due to its strong antiviral activity, good safety, and low resistance rate. The following is a detailed explanation of its purpose:
Core indication: Treatment of chronic hepatitis B (HBV) infection
Entecavir tablets are the first-line antiviral therapy for chronic hepatitis B (HBV), with the core use of inhibiting virus replication, improving liver function, and delaying disease progression. Specific indications include:
Suitable for patients with active virus replication (high levels of HBV DNA), sustained elevation of serum alanine aminotransferase (ALT) (usually exceeding twice the upper limit of normal), or active liver tissue lesions (such as moderate to severe inflammation and fibrosis).
Including patients with compensatory liver disease (liver function is basically normal) and decompensated liver disease (liver function is severely impaired, such as jaundice, ascites, hepatic encephalopathy and other complications).
Chronic hepatitis B in children
Suitable for children and adolescents under the age of 2 to 18 with compensatory liver disease caused by chronic HBV infection, and those who have received initial treatment with nucleosides (i.e. have not received antiviral therapy with other nucleoside analogues).
One of the following conditions must be met:
Virus replication is active (HBV DNA levels are high) and serum ALT levels continue to rise (usually exceeding the upper limit of normal by 2 times).
Liver histology shows moderate to severe inflammation and/or fibrosis.
Mechanism of action: key link in inhibiting HBV replication
Entecavir is a guanine nucleoside analogue that exerts antiviral effects through the following mechanisms:
Phosphorylation activation&Highly selective inhibition of HBV
Entecavir is phosphorylated into triphosphate (ETV-TP) in cells, with a half-life of approximately 15 hours, and can maintain activity for a long time.
Competitive inhibition of HBV polymerase
ETV-TP competes with the natural substrate of HBV polymerase, deoxyguanosine triphosphate (dGTP), to inhibit the three activities of viral polymerase:
Activation of HBV polymerase: prevents the initiation of viral RNA synthesis.
Formation of reverse transcription negative strand of pre genomic mRNA: Blocking the reverse transcription of viral RNA into negative strand of DNA.
Synthesis of HBV DNA positive strand: Inhibits the extension of viral DNA positive strand, thereby blocking the viral replication cycle.
The inhibition constant (Ki) of ETV-TP on HBV DNA polymerase is 0.0012 μ M, indicating a strong inhibitory effect.
The inhibitory effect on cellular DNA polymerase (α, β, δ) and mitochondrial DNA polymerase γ is weak (Ki value of 18-160 μ M), reducing toxicity to host cells.
Clinical efficacy: Effectively inhibits viruses and improves liver function
Multiple clinical trials have confirmed the significant efficacy of entecavir in the treatment of chronic hepatitis B:
Adult initial treatment patients
Virological response: After 48 weeks of treatment, approximately 67% to 76% of patients' HBV DNA levels decreased to undetectable levels (<300 copies/mL), significantly better than lamivudine (approximately 36%).
Biochemical response: Approximately 68% to 72% of patients have their ALT levels returned to normal, which is higher than that of lamivudine (approximately 55%).
Organizational improvement: After 48 weeks of treatment, approximately 70% to 72% of patients showed a reduction in liver inflammation and fibrosis.
Patients who have failed lamivudine treatment
For patients with lamivudine resistance or treatment failure, the dose of entecavir is doubled to 1 mg/day, and after 48 weeks of treatment:
About 22% to 39% of patients have HBV DNA levels that are undetectable.
About 38% to 40% of patients have their ALT levels returned to normal.
Long term treatment data
After 5 years of continuous treatment, the cumulative incidence of drug resistance in newly treated patients is only 1.2%, while the cumulative incidence of drug resistance in patients who have failed lamivudine treatment is 51%.
Long term treatment can significantly reduce the risk of liver cirrhosis and liver cancer.
Pediatric patients
The efficacy of pediatric patients aged 2 to 18 years old is similar to that of adults. After 48 weeks of treatment:
About 46% of pediatric patients with a weight ≥ 32.6 kg in the 0.5 mg dose group had their HBV DNA levels reduced to undetectable levels.
Children with a weight<32.6 kg have a virological response rate comparable to adults after using entecavir oral solution.
Usage and dosage adjustment for special populations
The use and dosage of entecavir in different special populations need to be adjusted according to specific circumstances:
Patients with renal insufficiency
Entecavir is mainly excreted through the kidneys, and the clearance rate of patients with renal insufficiency decreases. The dosage needs to be adjusted:
Creatinine clearance rate ≥ 50 mL/min: No dose adjustment required (0.5 mg/day).
Creatinine clearance rate of 30-50 mL/min: 0.5 mg every 48 hours.
Creatinine clearance rate 10-30 mL/min: 0.5 mg every 72 hours.
Creatinine clearance rate<10 mL/min or hemodialysis/CAPD: once every 5-7 days, 0.5 mg each time.
Hemodialysis patients should take it after dialysis.
Patients with liver dysfunction
Patients with liver dysfunction (including decompensated cirrhosis) do not need to adjust their dosage, but close monitoring of liver function indicators (such as ALT, bilirubin, albumin, etc.) is necessary.
pregnant women
The research on the effects of entecavir on pregnant women is not sufficient, and it is only used when it is clearly needed, with a thorough consideration of its pros and cons.
Pregnant women using entecavir may increase the risk of fetal resistance to HIV nucleoside reverse transcriptase inhibitors, therefore HIV/HBV co infected patients need to receive highly active antiretroviral therapy (HAART) before using entecavir.
lactating women
Entecavir tablets may be secreted through breast milk, and lactating women should pause breastfeeding and switch to artificial feeding.
pediatric patients
The safety and efficacy of children under 2 years old have not been established and are not recommended for use.
Children aged 2 to 18 should adjust their dosage according to their weight:
Weight ≥ 32.6 kg: 0.5 mg/day (tablet or oral solution).
Weight range from 10 kg to<32.6 kg: Use entecavir oral solution, with dosage calculated based on body weight.
Elderly patients
The renal function of elderly patients over 65 years old may decline, and the dosage should be adjusted according to creatinine clearance rate, and renal function should be closely monitored.
Medication precautions and monitoring
To ensure the safe and effective use of entecavir, the following precautions should be taken:
Timing of medication：Entecavir should be taken on an empty stomach (at least 2 hours before or after meals) to avoid food affecting absorption.
Duration of treatment：Chronic hepatitis B requires long-term treatment, and the specific course of treatment depends on the patient's condition (such as HBeAg status, virological response, liver histology, etc.) and is determined by the doctor's evaluation.
HBeAg positive patients: Treatment should be continued for at least 12 months after HBV DNA undetectable and HBeAg seroconversion (disappearance of HBeAg and positive anti HBe).
HBeAg negative patients: Treatment should continue until HBsAg seroconversion or loss of efficacy (such as viral rebound).
Monitoring after discontinuation of medication：Sudden discontinuation of medication may lead to acute exacerbation of hepatitis, especially in patients with decompensated liver disease. Close monitoring of liver function (ALT, bilirubin, etc.) and HBV DNA levels should be conducted for at least 4 months after discontinuation of medication.
Drug interactions：Entecavir is not a substrate, inhibitor, or inducer of the CYP450 enzyme system and has less interaction with other drugs.
However, when used in combination with drugs that reduce kidney function or compete for active secretion through the glomerulus (such as certain antibiotics and immunosuppressants), it may increase blood drug concentrations and require close monitoring.
Resistance surveillance：Long term treatment patients need to regularly monitor HBV DNA levels and promptly detect drug-resistant variants (such as rtT184, rtS202, rtM250 and other site substitutions).After drug resistance, the treatment plan should be adjusted according to the doctor's advice (such as adding other antiviral drugs).
Taboos and Caution
The following situations prohibit or use entecavir with caution:
Contraindication
It is contraindicated for individuals who are allergic to entecavir or any ingredients in the formulation.
Patients with HIV/HBV co infection who have not received HAART treatment are contraindicated (which may induce HIV resistance).
Use with caution
Patients with renal insufficiency need to adjust their dosage.
Patients with decompensated liver function need to be closely monitored.
Pregnant and lactating women need to weigh the pros and cons.
Children patients need to strictly control the indications and dosage.
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