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Details

Stereochemistry ABSOLUTE
Molecular Formula C10H14N2O5
Molecular Weight 242.229
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TELBIVUDINE

SMILES

Cc1cn([C@]2([H])C[C@]([H])([C@]([H])(CO)O2)O)c(=O)nc1O

InChI

InChIKey=IQFYYKKMVGJFEH-CSMHCCOUSA-N
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

HIDE SMILES / InChI

Description
Curator's Comment:: description was created based on several sources, including: http://www.drugbank.ca/drugs/DB01265

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. Telbivudine is a synthetic thymidine nucleoside analogue; it is the L-isomer of thymidine. It is taken orally in a dose of 600 mg once daily with or without food. TYZEKA is the trade name for telbivudine, a synthetic thymidine nucleoside analogue with activity against hepatitis B virus (HBV). The chemical name for telbivudine is 1-((2S,4R,5S)-4-hydroxy-5-hydroxymethyltetrahydrofuran-2-y1)-5-methyl-1H-pyrimidine-2,4-dione, or 1-(2-deoxy-β-L-ribofuranosyl)-5-methyluracil. Telbivudine is a synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. It is phosphorylated by cellular kinases to the active triphosphate form, which has an intracellular half-life of 14 hours. Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination, resulting in inhibition of HBV replication. Telbivudine is an inhibitor of both HBV first strand (EC50 value = 1.3 ± 1.6 µM) and second strand synthesis (EC50 value = 0.2 ± 0.2 µM). Telbivudine 5'-triphosphate at concentrations up to 100 µM did not inhibit human cellular DNA polymerases α, β, or γ. No appreciable mitochondrial toxicity was observed in HepG2 cells treated with telbivudine at concentrations up to 10 µM.

CNS Activity

Originator

Curator's Comment:: Telbivudine was originally developed by US company Idenix, and Novartis licensed rights to the product in 2003 in a 25 million deal. Novartis is also working with Idenix on another hepatitis B product candidate, valtorcitabine, which is in Phase II testing.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: Q05486
Gene ID: NA
Gene Symbol: P
Target Organism: Hepatitis B virus genotype F2 (isolate Brazil/w4B) (HBV-F)
1.3 µM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TYZEKA

Approved Use

TYZEKA™ (telbivudine) is indicated for the treatment of chronic hepatitis B in adult patients with evidence of viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.

Launch Date

1.20009602E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.2 μg/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.22 μg/mL
25 mg 1 times / day steady-state, oral
dose: 25 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.61 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.97 μg/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.46 μg/mL
800 mg 1 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.82 μg/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.99 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1.24 μg/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.69 μg/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
0.56 μg × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
0.75 μg × h/mL
25 mg 1 times / day steady-state, oral
dose: 25 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2.91 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
20.94 μg × h/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29.73 μg × h/mL
800 mg 1 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.14 μg × h/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.02 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.67 μg × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
26.1 μg × h/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
44.5 h
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
96.7%
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TELBIVUDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1800 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1800 mg, 1 times / day
Sources:
healthy, adult
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Sources:
Other AEs: Acute hepatitis B, Lactic acidosis...
Other AEs:
Acute hepatitis B (severe)
Lactic acidosis (severe|grade 5)
Hepatomegaly (severe|grade 5)
Sources:
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
Disc. AE: CK increased, Nausea...
AEs leading to
discontinuation/dose reduction:
CK increased (4%)
Nausea (4%)
Diarrhea (4%)
Fatigue (4%)
Myalgia (4%)
Myopathy (4%)
Sources:
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Disc. AE: CK increased, Nausea...
AEs leading to
discontinuation/dose reduction:
CK increased (6 patients)
Nausea (2 patients)
Diarrhea (4 patients)
Fatigue (2 patients)
Myalgia (2 patients)
Myopathy (1 patient)
Pain in extremity (1 patient)
Nasopharyngitis (1 patient)
Hepatic pain (1 patient)
Gastroenteritis (1 patient)
Gastritis (1 patient)
Dyspnea (1 patient)
Dizziness (1 patient)
Blood potassium decreased (1 patient)
Asthenia (1 patient)
Anosmia (1 patient)
Amenorrhea (1 patient)
ALT increased (1 patient)
Abdominal tenderness (1 patient)
Abdominal pain (1 patient)
Sources: Page: p. 158
AEs

AEs

AESignificanceDosePopulation
Acute hepatitis B severe
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Sources:
Hepatomegaly severe|grade 5
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Sources:
Lactic acidosis severe|grade 5
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Sources:
CK increased 4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
Diarrhea 4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
Fatigue 4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
Myalgia 4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
Myopathy 4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
Nausea 4%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 847
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 847
Sources:
ALT increased 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Abdominal pain 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Abdominal tenderness 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Amenorrhea 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Anosmia 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Asthenia 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Blood potassium decreased 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Dizziness 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Dyspnea 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Gastritis 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Gastroenteritis 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Hepatic pain 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Myopathy 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Nasopharyngitis 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Pain in extremity 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Fatigue 2 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Myalgia 2 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Nausea 2 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Diarrhea 4 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
CK increased 6 patients
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources: Page: p. 158
unhealthy, adult
n = 849
Health Status: unhealthy
Condition: chronic hepatitis B
Age Group: adult
Population Size: 849
Sources: Page: p. 158
Overview

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer





Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Pegylated interferon alpha-2a (40 kDa) in the treatment of chronic hepatitis B.
2006
Special considerations and treatment of patients with HBV-HIV coinfection.
2007
Enantio-selectivity of human nucleoside monophosphate kinases.
2007
Telbivudine.
2007
In vitro susceptibility of adefovir-associated hepatitis B virus polymerase mutations to other antiviral agents.
2007
Entecavir: a new nucleoside analogue for the treatment of chronic hepatitis B.
2007 Apr
Telbivudine.
2007 Apr
Time for an active antiviral therapy for hepatitis B: An update on the management of hepatitis B virus infection.
2007 Aug
Customizing the management of chronic hepatitis B virus infection.
2007 Aug
The role of entecavir in the treatment of chronic hepatitis B.
2007 Dec
Clinical implications of resistance patterns against HBV-polymerase inhibitors for the treatment of chronic hepatitis B.
2007 Dec
Treatment of Hepatitis B e Antigen-negative Patients.
2007 Dec
Telbivudine for the management of chronic hepatitis B virus infection.
2007 Dec
[The efficacy and safety of telbivudine in korean patients with chronic hepatitis B].
2007 Dec
Telbivudine versus lamivudine in patients with chronic hepatitis B.
2007 Dec 20
Drug profile: telbivudine (Tyzeka).
2007 Jan
Telbivudine (Tyzeka) for chronic Hepatitis B.
2007 Jan 29
New hepatitis B treatment.
2007 Jan-Feb
New drugs: sitagliptin phosphate, telbivudine, and panitumumab.
2007 Jan-Feb
[Treatment in every detected virus replication. New guideline for therapy of hepatitis B publicized].
2007 Jul 19
[New first line therapy of chronic hepatitis B. Primary therapy goal: effective virus suppression].
2007 Jul 19
Treatment paradigms on hepatitis B e antigen-negative chronic hepatitis B patients.
2007 Jun
Treatment of chronic hepatitis B in HIV-infected patients in 2007.
2007 Mar
Diagnosis and treatment of chronic hepatitis B: an update.
2007 Mar
Molecular mechanisms of resistance to antiviral therapy in patients with chronic hepatitis B.
2007 Mar
Improving outcomes for patients with chronic hepatitis B.
2007 Mar
[The degree of HBV suppression with 24 week telbivudine- or lamivudine-treatment in hepatitis B patients predicts the efficacy of the treatment at week 52].
2007 May
Telbivudine: a new option for the treatment of chronic hepatitis B.
2007 May
[Diagnosis and treatment of chronic hepatitis B. Recommendations of the Czech Hepatology Society of the J. E. Purkinje Medical Society and the Society of Infectious Medicine of the J.E. Purkinje Medical Society].
2007 Nov
Gateways to clinical trials.
2007 Nov
Therapy of chronic hepatitis B: focus on telbivudine.
2007 Nov
Management and treatment of chronic hepatitis B virus: Belgian Association for the Study of the Liver (BASL) 2007 guidelines.
2007 Oct-Dec
[Several important issues on drug resistance of hepatitis B virus].
2007 Sep
[Telbivudine in the treatment of the chronic B hepatitis].
2008 Apr
Telbivudine versus lamivudine in patients with chronic hepatitis B.
2008 Apr 3
Telbivudine: new drug. Chronic hepatitis B: similar to lamivudine.
2008 Feb
Telbivudine versus lamivudine in Chinese patients with chronic hepatitis B: Results at 1 year of a randomized, double-blind trial.
2008 Feb
[Current data on the treatment of chronic hepatitis B].
2008 Feb
[Anti-viral therapy of type B chronic hepatitis. 3. Future of anti-viral agents].
2008 Jan 10
Gateways to clinical trials.
2008 Jan-Feb
Review article: current antiviral therapy of chronic hepatitis B.
2008 Jul
Current antiviral therapies for chronic hepatitis B.
2008 Jun
[New treatment options in chronic hepatitis B].
2008 Mar
[Pharmacological agents for the treatment of chronic hepatitis B].
2008 Mar
Chronic hepatitis B: preventing, detecting, and managing viral resistance.
2008 Mar
Therapeutic strategies in the management of patients with chronic hepatitis B virus infection.
2008 Mar
New drugs for chronic hepatitis B: a review.
2008 Mar-Apr
[Chinese roadmap for treating chronic hepatitis B with telbivudine].
2008 May
Hepatitis B goes globe: Telbivudine as a new treatment option.
2008 May
[New data and recommendations of antiviral therapy of chronic hepatitis B and C].
2008 Oct
Patents

Sample Use Guides

600 mg once-daily
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment:: This in vitro report confirms that telbivudine shows no in vitro antiviral effect against a broad range of wild-type and multi-drug resistant HIV isolates at IC50 values >600 μM, a value well above physiologically relevant concentrations and known to inhibit HBV activity in vitro (EC50 value = 200 nM). These results support further investigation in a clinical trial setting, of the efficacy and safety of telbivudine, for treatment of CHB in HIV-HBV co-infected patients who do not concurrently require anti-HIV treatment and for whom there are few available treatment options.
up to 600 μM
Name Type Language
TELBIVUDINE
EMA EPAR   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
LDT600
Code English
TELBIVUDINE [ORANGE BOOK]
Common Name English
TELBIVUDINE [INN]
Common Name English
LDT-600
Code English
TELBIVUDINE [VANDF]
Common Name English
2,4(1H,3H)-PYRIMIDINEDIONE,1-(2-DEOXY-.BETA.-L-ERYTHRO-PENTOFURANOSYL)-5-METHYL-
Common Name English
TYZEKA
Brand Name English
2'-DEOXY-L-THYMIDINE
Common Name English
TELBIVUDINE [USAN]
Common Name English
TELBIVUDINE [EMA EPAR]
Common Name English
TELBIVUDINE [MI]
Common Name English
TELBIVUDINE [WHO-DD]
Common Name English
NV-02B
Code English
SEBIVO
Brand Name English
TELBIVUDINE [MART.]
Common Name English
Classification Tree Code System Code
LIVERTOX 928
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
NCI_THESAURUS C97452
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
NDF-RT N0000175656
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
NDF-RT N0000175459
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
NDF-RT N0000175459
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
NDF-RT N0000009947
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
WHO-ATC J05AF11
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
EMA ASSESSMENT REPORTS SEBIVO (AUTHORIZED: HEPATITIS B, CHRONIC)
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
WHO-VATC QJ05AF11
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
NDF-RT N0000175459
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C66584
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
DRUG BANK
DB01265
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
CAS
3424-98-4
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
EPA CompTox
3424-98-4
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
FDA UNII
2OC4HKD3SF
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
LACTMED
Telbivudine
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
PUBCHEM
159269
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
WIKIPEDIA
TELBIVUDINE
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
EVMPD
SUB25231
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
ChEMBL
CHEMBL374731
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
RXCUI
474128
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
4220
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
MERCK INDEX
M10528
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY Merck Index
INN
8296
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY
MESH
C487779
Created by admin on Sat Jun 26 10:57:50 UTC 2021 , Edited by admin on Sat Jun 26 10:57:50 UTC 2021
PRIMARY