telbivudine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
uridine derivatives used as antiviral agents and as antineoplastics 4220 3424-98-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sebivo
  • telbivudine
  • beta-L-Thymidine
  • epavudine
  • L-Thymidine
A thymidine derivative and antiviral agent that inhibits DNA synthesis by HEPATITIS B VIRUS and is used for the treatment of CHRONIC HEPATITIS B.
  • Molecular weight: 242.23
  • Formula: C10H14N2O5
  • CLOGP: -1.38
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 99.10
  • ALOGS: -0.56
  • ROTB: 2

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 68 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
April 24, 2007 EMA
Oct. 25, 2006 FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug resistance 86.05 71.01 20 259 17348 46668435
Maternal exposure during pregnancy 84.96 71.01 29 250 102520 46583263
Blood creatine phosphokinase increased 76.76 71.01 20 259 27704 46658079

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood creatine phosphokinase increased 418.76 53.92 144 1943 43704 29906687
Myalgia 203.47 53.92 101 1986 76566 29873825
Hepatitis B DNULL increased 131.76 53.92 24 2063 503 29949888
Myoglobin blood increased 118.45 53.92 27 2060 1766 29948625
Blood creatine phosphokinase MB increased 105.58 53.92 25 2062 1931 29948460
Muscular weakness 101.48 53.92 60 2027 63585 29886806
Lactic acidosis 84.91 53.92 42 2045 31171 29919220
Rhabdomyolysis 78.57 53.92 51 2036 63529 29886862
Blood lactic acid increased 78.55 53.92 25 2062 5805 29944586
Myopathy 78.41 53.92 29 2058 10557 29939834
Blood lactate dehydrogenase increased 62.82 53.92 30 2057 20571 29929820
Alpha hydroxybutyrate dehydrogenase increased 60.01 53.92 7 2080 0 29950391
Hypoaesthesia 58.48 53.92 40 2047 54190 29896201

Pharmacologic Action:

SourceCodeDescription
ATC J05AF11 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIVIRALS FOR SYSTEMIC USE
DIRECT ACTING ANTIVIRALS
Nucleoside and nucleotide reverse transcriptase inhibitors
FDA MoA N0000009947 Nucleoside Reverse Transcriptase Inhibitors
FDA EXT N0000175459 Nucleoside Analog
FDA EPC N0000175656 Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
CHEBI has role CHEBI:36044 anti-virus drug
CHEBI has role CHEBI:59897 rna-dependent dna polymerase inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic type B viral hepatitis indication 61977001
Myositis contraindication 26889001 DOID:633
Kidney disease contraindication 90708001 DOID:557
Lactic acidosis contraindication 91273001 DOID:3650
Disorder of muscle contraindication 129565002 DOID:423
Steatosis of liver contraindication 197321007
Peripheral nerve disease contraindication 302226006
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.46 acidic
pKa2 13.02 acidic
pKa3 13.7 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Protein P Polyprotein INHIBITOR EC50 5.89 DRUG LABEL DRUG LABEL

External reference:

IDSource
4025782 VUID
N0000179779 NUI
D06675 KEGG_DRUG
4025782 VANDF
C1453933 UMLSCUI
CHEBI:63624 CHEBI
LLT PDB_CHEM_ID
DB01265 DRUGBANK_ID
CHEMBL374731 ChEMBL_ID
D000077712 MESH_DESCRIPTOR_UI
159269 PUBCHEM_CID
8296 INN_ID
2OC4HKD3SF UNII
474128 RXNORM
22372 MMSL
d05912 MMSL
011809 NDDF
424071004 SNOMEDCT_US
425347005 SNOMEDCT_US

Pharmaceutical products:

None