Details of the Drug

General Information of Drug (ID: DMSWUGE)

• Drug Name: Telbivudine
• Synonyms: Epavudine; LLT; LdT; Sebivo; Telbivudin; Tyzeka; Telbivudine [USAN]; LDT600; NB 02B; NV 02B; L-Deoxythymidine; L-Thymidine; L-dT; LDT-600; NV-02B; Tyzeka (TN); Beta-L-Thymidine; Telbivudine (USAN/INN); Tyzake/Sebivo (TN); Tyzeka, Sebivo, Telbivudine; 1-(2-Deoxy-beta-L-erythro-pentofuranosyl)-5-methylpyrimidine-2,4(1H,3H)-dione; 1-(2-Deoxy-beta-L-erythropentafuranosyl)-5-methyl-2,4(1H,3H)-pyrimidinedione; 1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione; 2'-Deoxy-L-thymidine

Indication

Disease Entry	ICD 11	Status	REF
Hepatitis B virus infection	1E51.0	Approved	[1]

• Therapeutic Class: Antiviral Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 242.23
  Logarithm of the Partition Coefficient (xlogp); -1.2
  Rotatable Bond Count (rotbonds); 2
  Hydrogen Bond Donor Count (hbonddonor); 3
  Hydrogen Bond Acceptor Count (hbondacc); 5
• ADMET Property:
  Bioavailability: 68% of drug becomes completely available to its intended biological destination(s) [2]
  Half-life: The concentration or amount of drug in body reduced by one-half in 15 hours [3]
• Chemical Identifiers:
  Formula: C10H14N2O5
  IUPAC Name: 1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione
  Canonical SMILES: CC1=CN(C(=O)NC1=O)[C@@H]2C[C@H]([C@@H](O2)CO)O
  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
  InChIKey: IQFYYKKMVGJFEH-CSMHCCOUSA-N
• Cross-matching ID:
  PubChem CID: 159269
  ChEBI ID: CHEBI:63624
  CAS Number: 3424-98-4
  DrugBank ID: DB01265
  TTD ID: D0CL9S
  ACDINA ID: D00655

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Hepatitis B virus Polymerase (HBV P)	TTT4SY6	Q67889_HBV	Inhibitor	[4]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cytochrome c oxidase subunit 2 (COX2)	OTTMVBJJ	COX2_HUMAN	Gene/Protein Processing	[5]
NADH dehydrogenase 1 beta subcomplex subunit 8, mitochondrial (NDUFB8)	OTW4A4Q0	NDUB8_HUMAN	Gene/Protein Processing	[5]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Telbivudine (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Brentuximab vedotin	DMWLC57	Moderate	Increased risk of peripheral neuropathy by the combination of Telbivudine and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[6]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Magnesium stearate	E00208	11177	lubricant
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Telbivudine 600 mg tablet	600 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Nucleoside and nucleotide analogs in the treatment of chronic hepatitis B. Enferm Infecc Microbiol Clin. 2008 May;26 Suppl 7:32-8.
• [2] Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches
• [3] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [4] Nucleos(t)ide analogues for hepatitis B virus: strategies for long-term success. Best Pract Res Clin Gastroenterol. 2008;22(6):1081-92.
• [5] Insights into the mechanisms of telbivudine-induced myopathy associated with mitochondrial dysfunction. Chem Biol Interact. 2023 Sep 25;383:110692. doi: 10.1016/j.cbi.2023.110692. Epub 2023 Sep 1.
• [6] Carrion C, Espinosa E, Herrero A, Garcia B "Possible vincristine-isoniazid interaction." Ann Pharmacother 29 (1995): 201. [PMID: 7756727]