Telbivudine Tablets

1. Telbivudine is a synthetic thymidine nucleoside analog that has the activity of inhibiting hepatitis B virus deoxyribonucleic acid (HBVDNA) polymerase. Telbivudine can be phosphorylated by cellular kinases and converted into an active triphosphate form, and the half-life of the triphosphate in cells is 14 hours. Telbivudine-5-triphosphate inhibits the activity of the enzyme by competing with the natural substrate of HBVDNA polymerase (reverse transcriptase) - thymidine-5-triphosphate. The incorporation of Telbivudine-5-triphosphate into viral DNA can lead to the termination of DNA chain synthesis, thereby inhibiting HBV replication. Telbivudine is an inhibitor of the synthesis of both the first chain (EC50=0.4-1.3mu;M) and the second chain (EC50=0.12-0.24mu;M) of HBV, and the inhibitory effect on the second chain is more obvious. Telbivudine-5-triphosphate has no inhibitory effect on human cell DNA polymerase alpha, beta or gamma even at a concentration of 100 mu;M. Telbivudine showed no significant mitochondrial toxicity in HepG2 cells at a concentration of 10 mu;M. 2. In the human hepatoma cell line 2.2.15 expressing HBV and primary duck liver cells infected with duck hepatitis B virus (DHBV), the half effective concentration (EC50) of telbivudine to inhibit viral synthesis was about 0.2 mu;M. In cell culture, the anti-HBV activity of telbivudine and adefovir dipivoxil was additive and not antagonized by the HIV nucleoside reverse transcriptase inhibitors didanosine and stavudine. Telbivudine is inactive against human immunodeficiency virus (HIV) type I (EC50 value (200(M)), and does not antagonize the anti-HIV activity of abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir or zidovudine.

The main ingredient of this product is telbivudine.

This product is a film-coated tablet, which appears white to slightly yellowish after removing the coating.

1. Telbivudine is used for adult patients with chronic hepatitis B with evidence of viral replication and persistent elevation of serum aminotransferase (ALT or AST) or evidence of active liver tissue lesions. 2. This indication is based on the virological, serological, biochemical and histological response results of adult patients with chronic hepatitis B who are HBeAg-positive and HBeAg-negative and have compensated liver function who are naive to nucleoside analogs. The effect of telbivudine has not been evaluated in hepatitis B patients with concurrent HIV, HCV or HDV infection. The effect of telbivudine has not been evaluated in liver transplant patients or patients with decompensated liver disease. There are no well-designed controlled studies using telbivudine in patients with chronic hepatitis B who are resistant to nucleoside analog reverse transcriptase inhibitors, but it is estimated that it may have cross-resistance with lamivudine.

1. Adults and adolescents (>16 years old) The recommended dose of this product for the treatment of chronic hepatitis B is 600 mg, once a day, orally, before or after meals, and is not affected by food. The optimal course of treatment has not yet been determined. 2. Patients with impaired renal function This product can be used for patients with chronic hepatitis B with impaired renal function. For patients with creatinine clearance of ≥50ml/min, there is no need to adjust the recommended dose. For patients with creatinine clearance < 50ml/min and end-stage renal disease (ESRD) patients receiving hemodialysis, the dosing interval needs to be adjusted: 1. Creatinine clearance > 50ml/min: 600mg, once a day; 2. 30ml/min & le; creatinine clearance & le; le; 49ml/min: 600mg, once every 48 hours; 3. Creatinine clearance < 30ml/min (no dialysis required): 600mg, once every 72 hours; 4. End-stage renal disease: 600mg, once every 96 hours; For patients with end-stage renal disease, this product should be taken after hemodialysis. 3. Patients with impaired liver function For patients with impaired liver function, there is no need to adjust the recommended dose of telbivudine.

Common adverse reactions in foreign clinical studies include weakness, headache, abdominal pain, nausea, (gastrointestinal) flatulence, diarrhea and indigestion.

1. Patients who are allergic to telbivudine or any of its excipients are contraindicated. 2. Telbivudine 600 mg (once a day) is used in combination with peginterferon 180 mg (once a week).

Precautions for children: Telbivudine has not been studied in children under 16 years of age. Telbivudine is not currently recommended for use in children. Precautions for pregnancy and lactation: 1. Telbivudine is a Class B drug in the U.S. FDA drug safety classification for pregnancy. 2. Telbivudine was not teratogenic in preclinical studies and showed no adverse effects on embryonic and fetal development. Studies on pregnant rats and rabbits showed that telbivudine can cross the placenta. Developmental toxicology studies on rats and rabbits showed that no evidence of damage to the fetus was observed at doses of 1000 mg/kg per day, which was 6 times and 37 times higher than the human therapeutic dose (600 g/day), respectively. 3. There are not enough well-controlled studies on pregnant women. Because animal reproductive toxicity studies do not always predict human responses, telbivudine can be used during pregnancy only when the benefits outweigh the risks. 4. Delivery has not been studied in pregnant women, and there is no data on the effect of telbivudine on mother-to-child transmission of HBV. Therefore, appropriate intervention measures should be taken to prevent neonatal HBV infection. In rat studies, telbivudine was secreted in breast milk. It is not known whether telbivudine is secreted in human breast milk. Mothers should be instructed not to breastfeed if they are treated with telbivudine. Elderly precautions: There are no data to support specific recommended doses for patients over 65 years of age (see Precautions).

1. Telbivudine is eliminated mainly by passive diffusion, so the possibility of interaction between telbivudine and other drugs eliminated by renal excretion is very low. However, because telbivudine is eliminated mainly by renal excretion, taking drugs that can change renal function at the same time may affect the plasma concentration of telbivudine. 2. Under in vitro tests with concentrations 12 times higher than those in humans, telbivudine did not inhibit the metabolism of drugs mediated by the following human liver microsomal cytochrome P450 (CYP) isoenzymes: 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4. Based on the above results and the known elimination pathway of telbivudine, the possibility of interaction between telbivudine and other drugs metabolized by CYP450 is very low. 3. Lamivudine, adefovir dipivoxil, cyclosporine, peginterferon alpha;-2a or tenofovir disoproxil fumarate had no effect on the pharmacokinetics of telbivudine. In addition, telbivudine does not affect the pharmacokinetics of lamivudine, adefovir dipivoxil, cyclosporine or tenofovir disoproxil fumarate. Due to the large individual differences in the drug concentration of peginterferon alpha;-2a, it is impossible to make a definite conclusion on the effect of telbivudine on the pharmacokinetics of peginterferon alpha;-2a. 4. An exploratory clinical study suggests that the combined use of telbivudine 600 mg daily and subcutaneous injection of peginterferon alpha;-2a 180 mu; g once a week increases the risk of peripheral neuropathy.

Store below 30℃. Keep in original packaging. Keep out of reach of children.

600 mg

24 months.

Viatris Pharmaceuticals (DALIAN) Co., Ltd.

• Founded in:

  1989-10-07

• Address:

  No. 22 Daqing Road, Dalian Economic and Technological Development Zone, Liaoning Province

• Tax NO.:

  912102006048147187

• Registered Funds:

  $80.4 million

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