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

Stem definition	Drug id	CAS RN
uridine derivatives used as antiviral agents and as antineoplastics	4220	3424-98-4

Description:

Molecule	Description
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 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.60	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	68 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	66.80 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	1 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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Approvals:

Date	Agency	Company	Orphan
April 24, 2007	EMA
Oct. 25, 2006	FDA	NOVARTIS

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug resistance	97.63	91.29	20	145	22913	63465944

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Blood creatine phosphokinase increased	152.55	72.89	50	665	44807	34911409
Drug resistance	117.27	72.89	36	679	25891	34930325
Hepatitis B DNA increased	92.70	72.89	15	700	550	34955666
Myalgia	85.43	72.89	39	676	84071	34872145

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Blood creatine phosphokinase increased	203.28	62.78	57	694	66033	79677604
Drug resistance	118.42	62.78	34	717	42179	79701458
Hepatitis B DNA increased	106.46	62.78	16	735	799	79742838
Viral mutation identified	93.95	62.78	18	733	3840	79739797
Myalgia	91.15	62.78	41	710	185600	79558037
Pathogen resistance	90.50	62.78	22	729	14320	79729317

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AF11	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Nucleoside and nucleotide reverse transcriptase inhibitors
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:59897	reverse transcriptase inhibitors
FDA EPC	N0000175656	Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor
FDA EXT	N0000175459	Nucleoside Analog
FDA MoA	N0000009947	Nucleoside Reverse Transcriptase Inhibitors
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000998	Antiviral Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D019384	Nucleic Acid Synthesis Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.46	acidic
pKa2	13.02	acidic
pKa3	13.7	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
100MG/5ML	TYZEKA	NOVARTIS	N022154	April 28, 2009	DISCN	SOLUTION	ORAL	7858594	Sept. 11, 2023	TREATMENT OF CHRONIC HEPATITIS B IN ADULT PATIENTS
600MG	TYZEKA	NOVARTIS	N022011	Oct. 25, 2006	DISCN	TABLET	ORAL	7589079	Sept. 11, 2023	TREATMENT OF CHRONIC HEPATITIS B IN ADULT PATIENTS
600MG	TYZEKA	NOVARTIS	N022011	Oct. 25, 2006	DISCN	TABLET	ORAL	7858594	Sept. 11, 2023	TREATMENT OF CHRONIC HEPATITIS B IN ADULT PATIENTS