Identification | |||||
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Name | Telbivudine | ||||
Accession Number | DB01265 | ||||
Type | small molecule | ||||
Description | Telbivudine is a synthetic thymidine nucleoside analog with specific activity against the hepatitis B virus. Telbivudine is orally administered, with good tolerance, lack of toxicity and no dose-limiting side effects. | ||||
Structure |
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Categories (*) | |||||
Molecular Weight | 242.2286 | ||||
Groups | approved | ||||
Monoisotopic Weight | 242.090271568 | ||||
Pharmacology | |||||
Indication | For the treatment of chronic hepatitis B in adult and adolescent patients >=16 years of age with evidence of viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease. | ||||
Mechanism of action | Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. This leads to the chain termination of DNA synthesis, thereby inhibiting viral replication. Incorporation of telbivudine 5'-triphosphate into viral DNA also causes DNA chain termination, resulting in inhibition of HBV replication. Telbivudine inhibits anticompliment or second-strand DNA. | ||||
Absorption | Absorbed following oral administration. Telbivudine absorption and exposure were unaffected when a single 600-mg dose was administered with a high-fat (~55 g), high-calorie (~950 kcal) meal. | ||||
Protein binding | In vitro binding of telbivudine to human plasma proteins is low (3.3%). | ||||
Biotransformation | No metabolites of telbivudine were detected following administration of [14C]-telbivudine in humans. Telbivudine is not a substrate, or inhibitor of the cytochrome P450 (CYP450) enzyme system. | ||||
Route of elimination | Telbivudine is eliminated primarily by urinary excretion of unchanged drug. | ||||
Toxicity | There is no information on intentional overdose of telbivudine, but one subject experienced an unintentional and asymptomatic overdose. Healthy subjects who received telbivudine doses up to 1800 mg/day for 4 days had no increase in or unexpected adverse events. A maximum tolerated dose for telbivudine has not been determined. | ||||
Affected organisms |
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Interactions | |||||
Drug Interactions |
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Food Interactions |
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P protein [Includes: DNA-directed DNA polymerase | |
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Name | P protein [Includes: DNA-directed DNA polymerase |
Gene Name | P |
Pharmacological action | yes |
Actions | Not Available |
References |
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DTHybrid score | 0.9888 |
DNA | |
Name | DNA |
Gene Name | Not Available |
Pharmacological action | yes |
Actions | Not Available |
References |
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DTHybrid score | Not Available |
Id | Partner name | Gene Name | Score |
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342 | P protein [Includes: DNA-directed DNA polymerase | P | 0.9888 |
677 | Choline-phosphate cytidylyltransferase A | PCYT1A | 0.0411 |
5626 | Nucleoside diphosphate kinase B | NME2 | 0.0342 |
702 | UMP-CMP kinase | CMPK1 | 0.0337 |
4773 | Deoxycytidine kinase | DCK | 0.0305 |
5294 | Nucleoside diphosphate kinase A | NME1 | 0.0262 |
1709 | Canalicular multispecific organic anion transporter 2 | ABCC3 | 0.0198 |
6147 | Solute carrier family 22 member 3 | SLC22A3 | 0.0197 |
2164 | Multidrug resistance-associated protein 4 | ABCC4 | 0.0187 |
6144 | Solute carrier family 22 member 2 | SLC22A2 | 0.0175 |
862 | Multidrug resistance-associated protein 1 | ABCC1 | 0.0171 |
6145 | Solute carrier family 22 member 1 | SLC22A1 | 0.0166 |
1735 | Canalicular multispecific organic anion transporter 1 | ABCC2 | 0.0161 |
1732 | ATP-binding cassette sub-family G member 2 | ABCG2 | 0.0159 |
1729 | Solute carrier family 22 member 6 | SLC22A6 | 0.0152 |
1588 | Multidrug resistance protein 1 | ABCB1 | 0.0123 |