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

Stem definition	Drug id	CAS RN
antivirals Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI)	1115	269055-15-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: etravirine intelence etravirin R-165335 TMC-125	HIV-1 reverse transriptase inhibitor; an anti-HIV agent Molecular weight: 435.29 Formula: C20H15BrN6O CLOGP: 5.17 LIPINSKI: 1 HAC: 7 HDO: 2 TPSA: 120.64 ALOGS: -4.41 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

etravirine
intelence
etravirin
R-165335
TMC-125

HIV-1 reverse transriptase inhibitor; an anti-HIV agent

Molecular weight: 435.29
Formula: C20H15BrN6O
CLOGP: 5.17
LIPINSKI: 1
HAC: 7
HDO: 2
TPSA: 120.64
ALOGS: -4.41
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.40	g	O

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.56 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 28, 2008	EMA
Jan. 18, 2008	FDA	JANSSEN R AND D

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
Enlarged clitoris	208.51	43.20	28	2401	130	63486463
Hyperandrogenism	191.70	43.20	25	2404	88	63486505
Viral mutation identified	170.79	43.20	33	2396	1777	63484816
Foetal exposure during pregnancy	167.73	43.20	58	2371	31904	63454689
Exposure during pregnancy	167.41	43.20	92	2337	155455	63331138
Virologic failure	145.51	43.20	29	2400	1833	63484760
Lipodystrophy acquired	127.92	43.20	25	2404	1427	63485166
Cloacal exstrophy	109.37	43.20	16	2413	150	63486443
Congenital genital malformation	102.49	43.20	15	2414	141	63486452
Bladder agenesis	102.21	43.20	15	2414	144	63486449

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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
Lipodystrophy acquired	470.08	24.40	106	4802	3238	34948785
Mitochondrial toxicity	414.52	24.40	92	4816	2607	34949416
Progressive external ophthalmoplegia	387.61	24.40	78	4830	1357	34950666
Eyelid ptosis	349.86	24.40	93	4815	5673	34946350
Diplopia	233.38	24.40	88	4820	16755	34935268
Virologic failure	219.87	24.40	58	4850	3422	34948601
Drug interaction	155.97	24.40	174	4734	225772	34726251
Viral mutation identified	120.78	24.40	35	4873	2919	34949104
Ophthalmoplegia	103.54	24.40	28	4880	1812	34950211
Drug resistance	100.99	24.40	56	4852	25871	34926152

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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
Lipodystrophy acquired	554.03	26.20	112	5357	4213	79734706
Mitochondrial toxicity	460.95	26.20	91	5378	3023	79735896
Progressive external ophthalmoplegia	449.48	26.20	79	5390	1366	79737553
Eyelid ptosis	341.48	26.20	90	5379	10954	79727965
Virologic failure	282.62	26.20	64	5405	4127	79734792
Viral mutation identified	255.19	26.20	58	5411	3800	79735119
Diplopia	235.87	26.20	88	5381	33378	79705541
Drug interaction	176.93	26.20	177	5292	415006	79323913
Drug resistance	125.08	26.20	60	5409	42153	79696766
Ophthalmoplegia	105.75	26.20	27	5442	2885	79736034

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AG04	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Non-nucleoside reverse transcriptase inhibitors
CHEBI has role	CHEBI:22587	antiviral agents
CHEBI has role	CHEBI:53756	reverse transcriptase inhibitors
FDA EPC	N0000175463	Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor
FDA EXT	N0000175460	Non-Nucleoside Analog
FDA MoA	N0000009948	Non-Nucleoside Reverse Transcriptase Inhibitors
FDA MoA	N0000182140	Cytochrome P450 2C19 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000185504	Cytochrome P450 2C9 Inhibitors
FDA MoA	N0000190118	Cytochrome P450 3A Inducers

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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
Human immunodeficiency virus infection	indication	86406008	DOID:526
Chronic type B viral hepatitis	contraindication	61977001
Chronic hepatitis C	contraindication	128302006
Liver function tests abnormal	contraindication	166603001
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	3.78	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	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Canalicular multispecific organic anion transporter 1	Transporter	Q92887	MRP2_HUMAN		IC50	5.11	CHEMBL
Multidrug resistance-associated protein 1	Transporter	P33527	MRP1_HUMAN		IC50	5.07	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.22	CHEMBL
Canalicular multispecific organic anion transporter 2	Transporter	O15438	MRP3_HUMAN		IC50	5.29	CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.12	CHEMBL
Reverse transcriptase/RNaseH	Enzyme		Q72547_9HIV1	INHIBITOR	IC50	9.22	CHEMBL	CHEMBL
Gag-Pol polyprotein	Polyprotein		POL_HV1A2		IC50	9	WOMBAT-PK
Cruzipain	Enzyme		CYSP_TRYCR		IC50	5.40	CHEMBL
Reverse transcriptase	Enzyme		Q9WKE8_9HIV1		IC50	8	CHEMBL
Reverse transcriptase protein	Unclassified		Q9WJQ2_9HIV1		IC50	8.89	CHEMBL

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External reference:

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ID	Source
65B	PDB_CHEM_ID
012527	NDDF
0C50HW4FO1	UNII
12675	IUPHAR_LIGAND_ID
130981	MMSL
193962	PUBCHEM_CID
24971	MMSL
348481	MMSL
4027244	VUID
4027244	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-473	TABLET	100 mg	ORAL	ANDA	25 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	42291-474	TABLET	200 mg	ORAL	ANDA	25 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1720	TABLET	25 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1720	TABLET	25 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1721	TABLET	100 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1721	TABLET	100 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1722	TABLET	200 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	60219-1722	TABLET	200 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1720	TABLET	25 mg	ORAL	ANDA	26 sections
etravirine	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1721	TABLET	100 mg	ORAL	ANDA	26 sections

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