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| Clinical data | |
|---|---|
| Trade names | Tyzeka, Sebivo |
| Other names | 1-(2-deoxy-β-L-ribofuranosyl)-5-methyluracil β-L-2-deoxythymidine β-L-thymidine (LdT) 1-[(2S,4R,5S)-4-hydroxy-5-hydroxymethyltetrahydrofuran-2-yl]-5-methyl-1H-pyrimidine-2,4-dione |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607045 |
| License data | |
| Pregnancy category | |
| Routes of administration | By mouth |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Protein binding | Low (3.3%in vitro) |
| Metabolism | Nil |
| Eliminationhalf-life | 40 to 49 hours (terminal phase) |
| Excretion | Kidney |
| Identifiers | |
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| CAS Number | |
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| DrugBank |
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| UNII | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.125.511 |
| Chemical and physical data | |
| Formula | C10H14N2O5 |
| Molar mass | 242.231 g·mol−1 |
| 3D model (JSmol) | |
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Telbivudine is anantiviral drug used in the treatment ofhepatitis B infection. It is marketed by Swiss pharmaceutical companyNovartis under the trade namesSebivo (European Union) andTyzeka (United States).Clinical trials have shown it to besignificantly more effective thanlamivudine oradefovir, and less likely to cause resistance.[1][2][3] However, HBV signature resistance mutation M204I (a change frommethionine toisoleucine at position 204 in thereverse transcriptase domain of the hepatitis B polymerase) or L180M+M204V have been associated with Telbivudine resistance.[4]
Telbivudine is a syntheticthymidineβ-L-nucleoside analogue; it is theL-isomer of thymidine. Telbivudine impairs hepatitis B virus (HBV) DNA replication by leading to chain termination. It differs from the natural nucleotide only with respect to the location of the sugar and base moieties, taking on an levorotatory configuration versus a dextrorotatory configuration as do the natural deoxynucleosides.[4] It is taken orally in a dose of 600 mg once daily with or without food.[5]
Telbivudine has no in vitro activity against HIV-1,[6] and in a case-series of three HIV-HBV co-infected patients, telbivudine did not produce sustained HIV-1 virologic suppression or induce any resistance mutations in HIV-1.[7]
Phase III clinical trials suggested that telbivudine put patients at greater risk formyopathy andperipheral neuropathy than the comparator druglamivudine.[8] FDA required a required arisk evaluation and mitigation strategy (REMS) aiming to increase awareness of peripheral neuropathy by requiring distribution of a medication guide.[9]
In 2016, Novartis posted a discontinuation notice.[10][11] Efficacy or safety concerns were not cited as rationale for discontinuation, but rather "availability of alternative medications"; presumably this refers totenofovir disoproxil, which became available as a generic medication in 2017, and is a safe and effective treatment for chronic HBV infection.
