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

Stem definition	Drug id	CAS RN
arotinoid derivatives	361	153559-49-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: LGD 1069 bexarotene targretin targretyn targrexin	A tetrahydronaphthalene derivative and RETINOID X RECEPTOR antagonist that is used in the treatment of CUTANEOUS T-CELL LYMPHOMA. Molecular weight: 348.49 Formula: C24H28O2 CLOGP: 8.19 LIPINSKI: 1 HAC: 2 HDO: 1 TPSA: 37.30 ALOGS: -6.37 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

LGD 1069
bexarotene
targretin
targretyn
targrexin

A tetrahydronaphthalene derivative and RETINOID X RECEPTOR antagonist that is used in the treatment of CUTANEOUS T-CELL LYMPHOMA.

Molecular weight: 348.49
Formula: C24H28O2
CLOGP: 8.19
LIPINSKI: 1
HAC: 2
HDO: 1
TPSA: 37.30
ALOGS: -6.37
ROTB: 3

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	28.70 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)	0.01 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 29, 1999	FDA	VALEANT LUXEMBOURG
March 29, 2001	EMA

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
Hypertriglyceridaemia	101.57	35.78	20	456	6239	63482307
Cutaneous T-cell lymphoma	58.85	35.78	10	466	1370	63487176
Hypothyroidism	51.17	35.78	17	459	42615	63445931
Diffuse large B-cell lymphoma	37.81	35.78	9	467	6703	63481843
Blood triglycerides increased	36.91	35.78	10	466	12478	63476068

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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
Hypothyroidism	151.87	29.75	45	937	20857	34935092
Hypertriglyceridaemia	115.88	29.75	30	952	8418	34947531
Cutaneous T-cell lymphoma	78.80	29.75	16	966	1522	34954427
Thyroid stimulating hormone deficiency	39.57	29.75	5	977	19	34955930
Dyslipidaemia	36.81	29.75	12	970	7476	34948473

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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
Hypertriglyceridaemia	187.91	29.20	44	1401	12696	79730247
Hypothyroidism	178.47	29.20	57	1388	52335	79690608
Cutaneous T-cell lymphoma	131.15	29.20	25	1420	2678	79740265
Blood triglycerides increased	48.04	29.20	17	1428	21023	79721920
Dyslipidaemia	45.02	29.20	14	1431	11619	79731324
Diffuse large B-cell lymphoma	44.42	29.20	14	1431	12135	79730808
Thyroid stimulating hormone deficiency	40.02	29.20	5	1440	29	79742914
Skin exfoliation	29.46	29.20	16	1429	55084	79687859

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XF03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Retinoids for cancer treatment
CHEBI has role	CHEBI:35610	antineoplastic agents
FDA CS	M0018962	Retinoids
FDA EPC	N0000175607	Retinoid
MeSH PA	D000970	Antineoplastic Agents

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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
Primary cutaneous T-cell lymphoma	indication	400122007
Alcoholism	contraindication	7200002
Hypothyroidism	contraindication	40930008	DOID:1459
Hepatic failure	contraindication	59927004
Diabetes mellitus	contraindication	73211009	DOID:9351
Leukopenia	contraindication	84828003	DOID:615
Bilateral cataracts	contraindication	95722004
Disorder of biliary tract	contraindication	105997008	DOID:9741
Acute pancreatitis	contraindication	197456007	DOID:2913
Chronic pancreatitis	contraindication	235494005

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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	4.23	acidic

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
Retinoic acid receptor RXR-beta	Nuclear hormone receptor	P28702	RXRB_HUMAN	AGONIST	Ki	8.23	CHEMBL	CHEMBL
Retinoic acid receptor RXR-gamma	Nuclear hormone receptor	P48443	RXRG_HUMAN	AGONIST	Ki	8.08	CHEMBL	CHEMBL
Retinoic acid receptor RXR-alpha	Nuclear hormone receptor	P19793	RXRA_HUMAN	AGONIST	Kd	7.85	CHEMBL	CHEMBL
Retinoic acid receptor gamma	Nuclear hormone receptor	P13631	RARG_HUMAN		Ki	6.89	CHEMBL
Cytochrome P450 26A1	Enzyme	O43174	CP26A_HUMAN		IC50	4.87	CHEMBL
Cytochrome P450 26B1	Enzyme	Q9NR63	CP26B_HUMAN		IC50	5.23	CHEMBL
Oxysterols receptor LXR-beta	Nuclear other	P55055	NR1H2_HUMAN		EC50	6.36	CHEMBL
Retinoic acid receptor alpha	Nuclear hormone receptor	P10276	RARA_HUMAN		Ki	6.74	CHEMBL
Oxysterols receptor LXR-alpha	Nuclear other	Q13133	NR1H3_HUMAN		EC50	6.71	CHEMBL
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN	ANTAGONIST	IC50	5.52	IUPHAR

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External reference:

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ID	Source
008004	NDDF
116346006	SNOMEDCT_US
233272	RXNORM
234760	MMSL
2807	IUPHAR_LIGAND_ID
31640	MMSL
387023000	SNOMEDCT_US
4021197	VUID
4021197	VANDF
7782	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0399	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	25 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0399	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	25 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0378-6955	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	28 sections
bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2832	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	27 sections
bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0591-2832	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	27 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0832-0285	CAPSULE	75 mg	ORAL	ANDA	28 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	0832-0285	CAPSULE	75 mg	ORAL	ANDA	28 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	42291-072	CAPSULE	75 mg	ORAL	ANDA	27 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	43975-315	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	27 sections
Bexarotene	HUMAN PRESCRIPTION DRUG LABEL	1	43975-315	CAPSULE, LIQUID FILLED	75 mg	ORAL	ANDA	27 sections

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