DGIdb - BEXAROTENE Drug Record

BEXAROTENE chembl:CHEMBL1023 ApprovedAntineoplasticImmunotherapy

Alternate Names:

LGD1069
LG100069
TARGRETINE
LGD-1069
BEXAROTENE
LG-100069
TARGRETIN
BEXAROTENUM
P-[1-(5,6,7,8,-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHYL)VINYL]BENZOIC ACID
BEXAROTÈNE
BEXAROTENO
4-[1-(5,6,7,8,-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTALENYL)ETHENYL]BENZOIC ACID
4-[1-(3,5,5,8,8-PENTAMETHYLTETRALIN-2-YL)ETHENYL]BENZOIC ACID
TARGRETYN
P-(1-(5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHYL)VINYL)BENZOIC ACID
TARGREXIN
TARGREXIN®
BEXAROTEN
pubchem.compound:82146
rxcui:233272
chembl:CHEMBL1023
drugbank:00307
chemidplus:153559-49-0

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent
Drug Class	antineoplastic agents
Year of Approval	1999

(6 More Sources)

Publications:

Yen et al., 2005, The selective retinoid X receptor agonist bexarotene (LGD1069, Targretin) prevents and overcomes multidrug resistance in advanced breast carcinoma., Mol. Cancer Ther.
Lalloyer et al., 2006, The RXR agonist bexarotene improves cholesterol homeostasis and inhibits atherosclerosis progression in a mouse model of mixed dyslipidemia., Arterioscler. Thromb. Vasc. Biol.
Yen et al., 2006, A selective retinoid X receptor agonist bexarotene (LGD1069, targretin) inhibits angiogenesis and metastasis in solid tumours., Br. J. Cancer
Rigas et al., 2005, Emerging role of rexinoids in non-small cell lung cancer: focus on bexarotene., Oncologist
Rizvi et al., 2001, Placebo-controlled trial of bexarotene, a retinoid x receptor agonist, as maintenance therapy for patients treated with chemotherapy for advanced non-small-cell lung cancer., Clin Lung Cancer
Farol et al., 2004, Bexarotene: a clinical review., Expert Rev Anticancer Ther
Tooker et al., 2007, Bexarotene (LGD1069, Targretin), a selective retinoid X receptor agonist, prevents and reverses gemcitabine resistance in NSCLC cells by modulating gene amplification., Cancer Res.
Lowe et al., Bexarotene., Am J Clin Dermatol
Tsai et al., 2008, A phase I study of bexarotene, a retinoic X receptor agonist, in non-M3 acute myeloid leukemia., Clin. Cancer Res.
Wagner CE et al., 2009, Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene)., J Med Chem
Ohsawa F et al., 2013, Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency., J Med Chem
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Fu et al., 2007, The retinoid X receptor-selective ligand, LGD1069, inhibits tumor-induced angiogenesis via suppression of VEGF in human non-small cell lung cancer., Cancer Lett.

BEXAROTENE RXRB

Interaction Score: 11.34

Interaction Types & Directionality:

activator (activating)

agonist (activating)

Interaction Info:

Mechanism of Interaction Retinoid X receptor agonist

Direct Interaction yes

Notes

PMIDs:
15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 17016423 17139284 18765556

Sources:
TALC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
BEXAROTENE RXRG

Interaction Score: 11.16

Interaction Types & Directionality:

activator (activating)

agonist (activating)

Interaction Info:

Mechanism of Interaction Retinoid X receptor agonist

Direct Interaction yes

Specific Action of the Ligand Agonist

PMIDs:
15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556

Sources:
TALC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
BEXAROTENE RXRA

Interaction Score: 1.57

Interaction Types & Directionality:

activator (activating)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19791803 23391145 15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556

Sources:
TALC DTC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD
BEXAROTENE NR1H3

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BEXAROTENE MAPK8

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17027148

Sources:
NCI
BEXAROTENE BLM

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BEXAROTENE NR1I2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
BEXAROTENE KAT2A

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BEXAROTENE PPARG

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measured using a TR-FRET competitive displacement assay.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
BEXAROTENE USP1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: BEXAROTENE
- Version: 01-August-2011
Alternate Names:

BEXAROTENE Primary Drug Name

Drug Info:

Year of Approval 1999

Drug Class antineoplastic agents

Publications:
TdgClinicalTrial: BEXAROTENE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:
NCI: LGD1069
- Version: 14-September-2017
Alternate Names:

C1635 NCI drug code

Drug Info:

Publications:

Fu et al., 2007, The retinoid X receptor-selective ligand, LGD1069, inhibits tumor-induced angiogenesis via suppression of VEGF in human non-small cell lung cancer., Cancer Lett.

DTC: BEXAROTENE

Version: 02-September-2020

Alternate Names:

CHEMBL1023 ChEMBL Drug ID

Drug Info:

Publications:

Wagner CE et al., 2009, Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene)., J Med Chem

Ohsawa F et al., 2013, Mechanism of retinoid X receptor partial agonistic action of 1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)-1H-benzotriazole-5-carboxylic acid and structural development to increase potency., J Med Chem

TALC: BEXAROTENE
- Version: 12-May-2016
Alternate Names:

BEXAROTENE Drug Generic Name

BEXAROTENE Primary Drug Name

LGD 1069 Drug Synonym

Drug Info:

Publications:
GuideToPharmacology: 135650520
- Version: 29-September-2020
Alternate Names:

BEXAROTENE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Bexarotene
- Version: 2020.06.01
Alternate Names:

D0N0RU TTD Drug ID

Drug Info:

Publications:
ChemblInteractions: CHEMBL1023
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1023
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
PharmGKB: bexarotene
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	Retinoid X receptor agonist
Direct Interaction	yes
Notes

Specific Action of the Ligand	Agonist
Endogenous Drug?	False
Direct Interaction?	True

Details of the Assay for Interaction	Measured using a TR-FRET competitive displacement assay.
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

BEXAROTENE	Drug Generic Name
BEXAROTENE	Primary Drug Name
LGD 1069	Drug Synonym

activator (activating)
agonist (activating)

activator (activating)
agonist (activating)

activator (activating)
agonist (activating)

BEXAROTENE Drug Record

BEXAROTENE chembl:CHEMBL1023 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: activator (activating) agonist (activating)

Interaction Info: Mechanism of Interaction Retinoid X receptor agonist Direct Interaction yes Notes

PMIDs: 15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 17016423 17139284 18765556

Sources: TALC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: activator (activating) agonist (activating)

Interaction Info: Mechanism of Interaction Retinoid X receptor agonist Direct Interaction yes Specific Action of the Ligand Agonist

PMIDs: 15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556

Sources: TALC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: activator (activating) agonist (activating)

Interaction Info: Specific Action of the Ligand Agonist Endogenous Drug? False Direct Interaction? True

PMIDs: 19791803 23391145 15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556

Sources: TALC DTC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17027148

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Details of the Assay for Interaction Measured using a TR-FRET competitive displacement assay. Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: BEXAROTENE

Alternate Names: BEXAROTENE Primary Drug Name

Drug Info: Year of Approval 1999 Drug Class antineoplastic agents

Publications:

TdgClinicalTrial: BEXAROTENE

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class Small Molecule FDA Approval approved

Publications:

NCI: LGD1069

Alternate Names: C1635 NCI drug code

Drug Info:

Publications: Fu et al., 2007, The retinoid X receptor-selective ligand, LGD1069, inhibits tumor-induced angiogenesis via suppression of VEGF in human non-small cell lung cancer., Cancer Lett.

DTC: BEXAROTENE

Alternate Names: CHEMBL1023 ChEMBL Drug ID

Drug Info:

TALC: BEXAROTENE

Alternate Names: BEXAROTENE Drug Generic Name BEXAROTENE Primary Drug Name LGD 1069 Drug Synonym

Drug Info:

Publications:

GuideToPharmacology: 135650520

Alternate Names: BEXAROTENE GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Bexarotene

Alternate Names: D0N0RU TTD Drug ID

Drug Info:

Publications:

ChemblInteractions: CHEMBL1023

Alternate Names:

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1023

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

activator (activating)

agonist (activating)

Interaction Info:

Mechanism of Interaction Retinoid X receptor agonist

Direct Interaction yes

Notes

PMIDs:
15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 17016423 17139284 18765556

Sources:
TALC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

activator (activating)

agonist (activating)

Interaction Info:

Mechanism of Interaction Retinoid X receptor agonist

Direct Interaction yes

Specific Action of the Ligand Agonist

PMIDs:
15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556

Sources:
TALC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

activator (activating)

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19791803 23391145 15897247 17008586 16495926 15632250 14700480 15056048 17483357 11702369 18765556

Sources:
TALC DTC TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
17027148

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measured using a TR-FRET competitive displacement assay.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

BEXAROTENE Primary Drug Name

Drug Info:

Year of Approval 1999

Drug Class antineoplastic agents

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

C1635 NCI drug code

Publications:

Fu et al., 2007, The retinoid X receptor-selective ligand, LGD1069, inhibits tumor-induced angiogenesis via suppression of VEGF in human non-small cell lung cancer., Cancer Lett.

Alternate Names:

CHEMBL1023 ChEMBL Drug ID

Alternate Names:

BEXAROTENE Drug Generic Name

BEXAROTENE Primary Drug Name

LGD 1069 Drug Synonym

Alternate Names:

BEXAROTENE GuideToPharmacology Ligand Name

Alternate Names:

D0N0RU TTD Drug ID