Entecavir Maleate 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.

This product is a film-coated tablet, which appears white or off-white after removing the coating.

For the treatment of chronic hepatitis B that is HBeAg positive or negative.

Recommended dose: Adults and youth over 16 years old should take this product orally, once a day, 0.5 mg (one tablet) each time. Patients with viremia or lamivudine-resistant mutations during lamivudine treatment should take it once a day, 1.0 mg (two tablets) each time. This product should be taken on an empty stomach (at least 2 hours before or after a meal). For details, see the inner package insert.

In studies conducted abroad, the most common adverse events of this product are: headache, fatigue, dizziness, and nausea. Common adverse events in patients treated with lamivudine are: headache, fatigue, and dizziness. In these four 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. Please refer to the inner package insert for details.

People who are allergic to this product are prohibited from using it, and those with allergic constitutions should use it with caution.

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 of approximately 10,000 times the concentration in humans, entecavir does not inhibit any of the major human CYP450 enzymes: 1A2, 2C9, 2C19, 2D6, 3A4, 2B6 and 2E1. At concentrations of approximately 340 times the concentration in humans, entecavir does not induce human CYP450 enzymes: 1A2, 2C9, 2C19, 3A4, 3A5 and 2B6. See the inner package insert for details.

Keep in a cool place.

0.5mg

24 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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