DB01265 - Telbivudine
| Identification | |||||
|---|---|---|---|---|---|
| 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. | ||||
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| Interactions | |||||
| Drug Interactions |
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| Food Interactions |
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Targets
| P protein [Includes: DNA-directed DNA polymerase | |
|---|---|
| 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 |
Predictions
| Id | Partner name | Gene Name | Score |
|---|---|---|---|
| 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 |