Entecavir Dispersible Tablets

This product is a guanine nucleoside analog that has an inhibitory effect on hepatitis B virus (HBV) polymerase. It can be converted into an active triphosphate through phosphorylation, and the half-life of the triphosphate in the cell is 15 hours. By competing with the natural substrate of HBV polymerase, deoxyguanosine triphosphate, entecavir triphosphate can inhibit all three activities of viral polymerase (reverse transcriptase): (1) the initiation of HBV polymerase; (2) the formation of the negative strand of pregenomic mRNA reverse transcription; (3) the synthesis of the positive strand of HBVDNA. Entecavir triphosphate has a weak inhibitory effect on cellular alpha, beta, delta DNA polymerase and mitochondrial gamma DNA polymerase, with a Ki value of 18 to greater than 160muM.

The main ingredients of this product are: Entecavir Chemical name: 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl]-1,9-dihydro-6H-purine-6-one monohydrate Chemical structure: Molecular formula: C12H15N5O3H2O Molecular weight: 295.3

This product is white or off-white tablets.

This product is suitable for the treatment of chronic hepatitis B in adults with active viral replication, persistent elevation of serum transaminase ALT, or active lesions shown in liver histology.

Patients should take this product under the guidance of an experienced physician. Recommended dose: Adults and adolescents aged 16 years and above should take this product orally once a day, 0.5 mg each time. Patients who develop viremia or lamivudine-resistant mutations during lamivudine treatment should take 1 mg (two 0.5 mg tablets) once a day. This product should be taken on an empty stomach (at least 2 hours before or after a meal). Renal insufficiency In patients with renal insufficiency, the apparent oral clearance of entecavir decreases with decreasing creatinine clearance (see Pharmacokinetics, Special Populations). Patients with creatinine clearance < 50 mL/min (including patients receiving hemodialysis or CAPD) should adjust the dosage. Hepatic insufficiency No dosage adjustment is required for patients with hepatic insufficiency. Treatment period The optimal treatment time for this product and its relationship with long-term treatment outcomes, such as cirrhosis and liver cancer, are not yet clear.

The evaluation of adverse reactions is based on 4 global clinical trials: AI463014, AI463022, AI463026, AI463027 and 3 clinical trials conducted in China (AI463012, AI463023, AI463056). A total of 2596 patients with chronic hepatitis B were enrolled in these 7 studies. In studies compared with lamivudine, the adverse events and laboratory abnormalities of entecavir and lamivudine were similar. In studies conducted abroad, the most common adverse events of this product were: headache, fatigue, dizziness, and nausea. Common adverse events in patients treated with lamivudine were: headache, fatigue, and dizziness. In these 4 studies, 1% of patients treated with entecavir and 4% of patients treated with lamivudine withdrew from the study due to adverse events and abnormal laboratory test indicators.

It is contraindicated for patients who are allergic to entecavir or any ingredient in the preparation.

Precautions for children: The safety and efficacy data of this product for children under 16 years old have not been established. Precautions for pregnancy and lactation: The effects of entecavir on pregnant women have not been fully studied. This product can only be used when the potential risks and benefits to the fetus have been fully weighed. There is currently no information suggesting that this product can affect the mother-to-child transmission of HBV, so appropriate intervention measures should be taken to prevent neonatal HBV infection. Entecavir can be secreted from rat milk. However, it is still unclear whether it is secreted in human milk, so it is not recommended for mothers taking this product to breastfeed. Precautions for the elderly: Since there are not enough elderly patients aged 65 and above to participate in clinical studies of this product, it is not clear how elderly patients and younger patients respond to this product. Other clinical trial reports have not found differences between elderly and young patients. Entecavir is mainly excreted by the kidneys, and the risk of toxic reactions may be higher in patients with renal impairment. Because most elderly patients have decreased renal function, attention should be paid to the selection of drug doses and renal function should be monitored.

The metabolism of entecavir was evaluated in vivo and in vitro. Entecavir is not a substrate, inhibitor, or inducer of the cytochrome P450 (CYP450) enzyme system. At concentrations approximately 10,000 times the human concentration, entecavir does not inhibit any of the major human CYP450 enzymes: 1A2, 2C9, 2C19, 2D6, 3A4, 2B6, and 2E1. At concentrations approximately 340 times the human concentration, entecavir does not induce human CYP450 enzymes: 1A2, 2C9, 2C19, 3A4, 3A5, and 2B6. Concomitant administration of drugs that are metabolized by inhibiting or inducing the CYP450 system has no effect on the pharmacokinetics of entecavir. In addition, concomitant administration of entecavir has no effect on the pharmacokinetics of known CYP substrates. When studying the interaction of entecavir with lamivudine, adefovir, and tenofovir, it was found that the steady-state pharmacokinetics of entecavir and the interacting drugs were not altered. Because entecavir is primarily cleared by the kidneys, taking entecavir with drugs that reduce renal function or compete for active glomerular secretion may increase the plasma concentrations of these two drugs. Concomitant use of entecavir with lamivudine, adefovir, and tenofovir does not cause significant drug interactions. The interaction of concomitant use of entecavir with other drugs that are cleared by the kidneys or are known to affect renal function has not been studied. Patients should be closely monitored for the occurrence of adverse reactions when taking entecavir and such drugs at the same time.

Seal tightly and store in a dry place below 25℃.

1.0mg

18 months

CHIA TAI Tianqing Pharmaceutical Group Co., Ltd.

• Founded in:

  1997-04-16

• Address:

  No. 369, Yuzhou South Road, Lianyungang City, Jiangsu Province

• Tax NO.:

  91320000608398264T

• Registered Funds:

  890 million yuan

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