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

Stem definition	Drug id	CAS RN
antivirals phosphonic acid derivatives	2592	147127-20-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tenofovir hydrate tenofovir tenefovir	An adenine analog REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone. Molecular weight: 287.22 Formula: C9H14N5O4P CLOGP: -1.16 LIPINSKI: 0 HAC: 9 HDO: 3 TPSA: 136.38 ALOGS: -2.19 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tenofovir hydrate
tenofovir
tenefovir

An adenine analog REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone.

Molecular weight: 287.22
Formula: C9H14N5O4P
CLOGP: -1.16
LIPINSKI: 0
HAC: 9
HDO: 3
TPSA: 136.38
ALOGS: -2.19
ROTB: 5

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	5.80 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	3.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ
BA (Bioavailability)	25 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	2 mg/mL	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.93 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.83 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
March 25, 2004	PMDA	Japan Tobacco Inc.
Nov. 5, 2009	FDA	HETERO DRUGS LTD

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
Maternal exposure during pregnancy	219.60	30.98	128	2555	219934	63266405
Drug resistance	140.71	30.98	48	2635	22885	63463454
Rebound effect	122.02	30.98	30	2653	4496	63481843
Virologic failure	119.22	30.98	25	2658	1837	63484502
Foetal exposure during pregnancy	118.01	30.98	46	2637	31916	63454423
Exposure during pregnancy	102.91	30.98	70	2613	155477	63330862
Drug interaction	99.55	30.98	80	2603	229051	63257288
Immune reconstitution inflammatory syndrome	99.05	30.98	27	2656	6057	63480282
Fanconi syndrome acquired	96.50	30.98	19	2664	1017	63485322
Viral mutation identified	91.48	30.98	20	2663	1790	63484549

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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
Psychiatric decompensation	371.98	22.23	88	5610	2849	34948384
Depression suicidal	311.67	22.23	74	5624	2431	34948802
Tearfulness	307.06	22.23	74	5624	2593	34948640
Depressive symptom	256.80	22.23	65	5633	2794	34948439
Immune reconstitution inflammatory syndrome	256.22	22.23	83	5615	8676	34942557
Psychomotor skills impaired	222.84	22.23	62	5636	3844	34947389
Paranoia	196.86	22.23	74	5624	11994	34939239
Lipodystrophy acquired	185.80	22.23	52	5646	3292	34947941
Mitochondrial toxicity	177.87	22.23	48	5650	2651	34948582
Drug interaction	174.18	22.23	198	5500	225748	34725485

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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
Immune reconstitution inflammatory syndrome	380.18	20.71	111	7695	13730	79722852
Psychiatric decompensation	379.37	20.71	86	7720	3877	79732705
Depression suicidal	312.31	20.71	73	7733	3769	79732813
Tearfulness	279.44	20.71	73	7733	5972	79730610
Drug interaction	245.82	20.71	249	7557	414934	79321648
Depressive symptom	242.05	20.71	66	7740	6357	79730225
Psychomotor skills impaired	231.27	20.71	61	7745	5176	79731406
Hepatitis B	216.29	20.71	64	7742	8268	79728314
Paranoia	195.49	20.71	73	7733	19359	79717223
Mitochondrial toxicity	190.24	20.71	47	7759	3067	79733515

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:53756	reverse transcriptase inhibitors
MeSH PA	D019380	Anti-HIV Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D044966	Anti-Retroviral Agents
MeSH PA	D000998	Antiviral Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D019384	Nucleic Acid Synthesis Inhibitors
MeSH PA	D018894	Reverse Transcriptase 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
Human immunodeficiency virus infection	indication	86406008	DOID:526
Coronavirus infection	off-label use	186747009
Prevention of HIV Infection after Exposure	off-label use
Osteomalacia	contraindication	4598005	DOID:10573
Hypophosphatemia	contraindication	4996001
Suicidal thoughts	contraindication	6471006
Hypercholesterolemia	contraindication	13644009
Torsades de pointes	contraindication	31722008
Depressive disorder	contraindication	35489007

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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	0.23	acidic
pKa2	4.92	acidic
pKa3	4.28	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	UniProt	Type	Activity value (-log[M])	Bioact source
Reverse transcriptase/RNaseH	Enzyme	Q72547_9HIV1	IC50	6.42	CHEMBL
Reverse transcriptase	Enzyme	Q9WKE8_9HIV1	IC50	6.42	CHEMBL
Capsid protein	Unclassified	Q03732_HBV	EC50	6.62	CHEMBL

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External reference:

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ID	Source
TFO	PDB_CHEM_ID
009357	NDDF
10948	IUPHAR_LIGAND_ID
117466	RXNORM
206184-49-8	SECONDARY_CAS_RN
395264002	SNOMEDCT_US
4021279	VUID
4021279	VANDF
422091007	SNOMEDCT_US
464205	PUBCHEM_CID

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Pharmaceutical products:

None