テルビブジン
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2012/11/18 15:50:28」(JST)
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Telbivudine
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Systematic (IUPAC) name |
1-(2-deoxy-β-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione |
Clinical data |
Trade names |
Tyzeka |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a607045 |
Licence data |
EMA:Link, US FDA:link |
Pregnancy cat. |
B (US) |
Legal status |
POM (UK) ℞-only (US) |
Routes |
Oral |
Pharmacokinetic data |
Protein binding |
Low (3.3% in vitro) |
Metabolism |
Nil |
Half-life |
40 to 49 hours (terminal phase) |
Excretion |
Renal |
Identifiers |
CAS number |
3424-98-4 Y |
ATC code |
J05AF11 |
PubChem |
CID 159269 |
DrugBank |
DB01265 |
ChemSpider |
140081 Y |
UNII |
2OC4HKD3SF Y |
ChEMBL |
CHEMBL374731 N |
Synonyms |
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 |
Chemical data |
Formula |
C10H14N2O5 |
Mol. mass |
242.23 g/mol |
SMILES
- O=C/1NC(=O)N(\C=C\1C)[C@H]2O[C@H]([C@H](O)C2)CO
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InChI
-
InChI=1S/C10H14N2O5/c1-5-3-12(10(16)11-9(5)15)8-2-6(14)7(4-13)17-8/h3,6-8,13-14H,2,4H2,1H3,(H,11,15,16)/t6-,7+,8+/m1/s1 Y
Key:IQFYYKKMVGJFEH-CSMHCCOUSA-N Y
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N (what is this?) (verify)
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Telbivudine is an antiviral drug used in the treatment of hepatitis B infection. It is marketed by Swiss pharmaceutical company Novartis under the trade names Sebivo (Europe) and Tyzeka (United States). Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance.[1][2][3]
Telbivudine is a synthetic thymidine nucleoside analogue; it is the L-isomer of thymidine. It is taken once daily.
References
- ^ Lai CL, Leung N, Teo EK, et al. (2005). "A 1-year trial of telbivudine, lamivudine, and the combination in patients with hepatitis B e antigen-positive chronic hepatitis B". Gastroenterology 129 (2): 528–36. doi:10.1016/j.gastro.2005.05.053. PMID 16083710.
- ^ Lai CL, Gane E, Liaw YF, et al. (2007). "Telbivudine versus lamivudine in patients with chronic hepatitis B". N Engl J Med 357 (25): 2576–88. doi:10.1056/NEJMoa066422. PMID 18094378.
- ^ Chan HL, Heathcote EJ, Marcellin P, et al. (4 December 2007). "Treatment of hepatitis B e antigen positive chronic hepatitis with telbivudine or adefovir: a randomized trial". Ann Intern Med 147 (11): 745–54. PMID 17909201. http://www.annals.org/cgi/content/full/147/11/745.
External links
- Tyzeka official website run by Novartis Pharmaceuticals Corporation
- Telbivudine entry in RxList
- Sebivo Summary of Product Characteristics (from the EMEA website)
DNA virus antivirals (primarily J05, also S01AD and D06BB)
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Baltimore I |
Herpesvirus
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DNA-synthesis
inhibitor
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TK activated
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Purine analogue
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- guanine (Aciclovir#/Valacyclovir
- Ganciclovir/Valganciclovir
- Penciclovir/Famciclovir)
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Pyrimidine analogue
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- uridine (Idoxuridine
- Trifluridine
- Edoxudine)
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Not TK activated
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Other
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- Docosanol
- early protein (Fomivirsen)
- Tromantadine
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HPV/MC
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- Imiquimod/Resiquimod
- Podophyllotoxin
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Vaccinia
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Poxviridae
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Hepatitis B (VII) |
- Nucleoside analogues/NARTIs: Entecavir
- Lamivudine
- Telbivudine
- Clevudine
- Nucleotide analogues/NtRTIs: Adefovir
- Tenofovir
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Multiple/general |
Nucleic acid inhibitors
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Interferon
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- Interferon alfa-2b
- Peginterferon alfa-2a
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Multiple/unknown
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- Ribavirin#/Taribavirin†
- Moroxydine
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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cutn/syst (hppv/hiva, infl/zost/zoon)/epon
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drug(dnaa, rnaa, rtva, vacc)
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UpToDate Contents
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English Journal
- Reduction of Hepatitis B Surface Antigen and Covalently Closed Circular DNA by Nucleos(t)ide Analogues of Different Potency.
- Wong DK, Seto WK, Fung J, Ip P, Huang FY, Lai CL, Yuen MF.SourceDepartment of Medicine, University of Hong Kong, Queen Mary Hospital, Hong Kong SAR, China; State Key Laboratory for Liver Research, University of Hong Kong, Queen Mary Hospital, Hong Kong SAR, China.
- Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association.Clin Gastroenterol Hepatol.2013 Aug;11(8):1004-1010.e1. doi: 10.1016/j.cgh.2013.01.026. Epub 2013 Feb 1.
- BACKGROUND & AIMS: Few studies have investigated the effects of different nucleos(t)ide analogues against hepatitis B virus (HBV) on levels of covalently closed circular DNA (cccDNA) and hepatitis B surface antigen (HBsAg) in patients. We measured the magnitude of reduction of cccDNA and HBsAg b
- PMID 23376799
- Telbivudine and adefovir combination therapy for patients with chronic lamivudine-resistant hepatitis B virus infections.
- Lin MT, Chou YP, Hu TH, Yu HC, Hsu YC, Tsai MC, Tseng PL, Chang KC, Yen YH, Chiu KW.SourceDivision of Hepato-Gastroenterology, Department of Internal Medicine, Kaohsiung Chang Gung Memorial Hospital, Chang Gung University College of Medicine, 123, Ta-Pei Road, Niao-Sung Dist., Kaohsiung, 833, Taiwan.
- Archives of virology.Arch Virol.2013 Jul 16. [Epub ahead of print]
- We evaluated second-line salvage therapy with adefovir + telbivudine (group 1), adefovir followed by adefovir + telbivudine (group 2), or lamivudine + adefovir followed by adefovir + telbivudine (group 3) in hepatitis B patients with an inadequate virologic response to lamivudine treatment. Simple l
- PMID 23857507
- Efficacy and safety of telbivudine therapy in liver failure patients with chronic hepatitis B virus infection.
- Wang L, Chen H, Fan C, Gong Z.SourceDepartment of Infectious Diseases, Renmin Hospital of Wuhan University, Wuhan, China.
- Journal of medical virology.J Med Virol.2013 Jul 12. doi: 10.1002/jmv.23689. [Epub ahead of print]
- The objective of this study was to evaluate the short-term efficacy and safety of telbivudine therapy as compared to lamivudine therapy in liver failure patients with chronic hepatitis B virus (HBV) infection. These data were collected from 38 liver failure patients with chronic HBV infection who we
- PMID 23852947
Japanese Journal
- 妊娠後期におけるtelbivudineまたはラミブジンの投与は周産期のB型肝炎ウイルス母子感染を安全に抑制する : 臨床実地
- Hepatology : official journal of the American Association for the Study of Liver Diseases 9(3), 10-18, 2014-12
- NAID 40020321307
- 新規抗HBV薬 (特集 抗ウイルス薬) -- (新規抗ウイルス薬の開発動向と展望)
- LIVER, PANCREAS, AND BILIARY TRACT GLOBE試験2年間の結果--B型慢性肝炎患者においてtelbivudineはラミブジンより優れている
- Review of gastroenterology & clinical gastroenterology and hepatology 4(2), 56-59, 2009-08
- NAID 40016795574
Related Links
- Idenix/ノバルティス社のtelbivudineとギリアド社のtenofovir(Viread)の2つの新規 NAsが、今後数年以内に上市されようとしており、これらは、他剤との差別化を図り、 十分な治療を受けていない莫大な患者人口に対する新治療としての地位を確立しよう として ...
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