DGIdb - ZILEUTON Drug Record

ZILEUTON chembl:CHEMBL93 Approved

Alternate Names:

ZYFLO CR
ABBOTT-64077
A-64077
ZILEUTON
ZYFLO
LEUTROL
ZILEUTONUM
N-[1-(BENZO[B]THIOPHEN-2-YL)ETHYL]-N-HYDROXYUREA
ZYFLO®
N-(1-BENZO(B)THIEN-2-YLETHYL)-N-HYDROXYUREA
(+-)-1-(1-BENZO[B]THIEN-2-YLETHYL)-1-HYDROXYUREA
chemidplus:111406-87-2
rxcui:40575
pubchem.compound:60490
chembl:CHEMBL93
drugbank:00744

Drug Info:

Drug Categories	cytochrome p-450 cyp1a2 inhibitors
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antiinflammatory agent
Year of Approval	1996
Drug Class	anti-asthmatic agents
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	decreased leukotriene production
Drug Categories	ugt1a9 substrates

(6 More Sources)

Publications:

Yamashita et al., 2000, Inhibition by troglitazone of the antigen-induced production of leukotrienes in immunoglobulin E-sensitized RBL-2H3 cells., Br. J. Pharmacol.
Wenzel, Leukotriene receptor antagonists and related compounds., Can. Respir. J.
Qian et al., 2001, Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor., Pharmacol. Res.
Coffey et al., 2001, Peroxynitrite-induced nitrotyrosination of proteins is blocked by direct 5-lipoxygenase inhibitor zileuton., J. Pharmacol. Exp. Ther.
Hardy et al., 1999, Prostaglandins and leukotriene B4 are potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 2 activity in human choriocarcinoma JEG-3 cells., Biol. Reprod.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Wenzel et al., Zileuton: the first 5-lipoxygenase inhibitor for the treatment of asthma., Ann Pharmacother
Guidot et al., 1994, Intrinsic 5-lipoxygenase activity is required for neutrophil responsivity., Proc. Natl. Acad. Sci. U.S.A.
Berger et al., 2007, Zileuton: clinical implications of 5-Lipoxygenase inhibition in severe airway disease., Int. J. Clin. Pract.
Zouboulis et al., 2010, Zileuton prevents the activation of the leukotriene pathway and reduces sebaceous lipogenesis., Exp. Dermatol.
Zouboulis, 2009, Zileuton, a new efficient and safe systemic anti-acne drug., Dermatoendocrinol
Vicente et al., 2001, Modulation of haem oxygenase-1 expression by nitric oxide and leukotrienes in zymosan-activated macrophages., Br. J. Pharmacol.
Pergola C et al., 2014, Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase., J Med Chem
Karg EM et al., 2009, Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase., J Med Chem
Schieferdecker S et al., 2015, Myxochelins target human 5-lipoxygenase., J Nat Prod
Tan EC et al., 2016, Common variants of catechol-O-methyltransferase influence patient-controlled analgesia usage and postoperative pain in patients undergoing total hysterectomy., Pharmacogenomics J
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Day JA et al., 2013, Investigating the selectivity of metalloenzyme inhibitors., J Med Chem

ZILEUTON KIAA0391

Interaction Score: 14.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25963335

Sources:
PharmGKB
ZILEUTON ALOX5

Interaction Score: 4.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zyflo

Novel drug target Established target

Mechanism of Interaction Arachidonate 5-lipoxygenase inhibitor

PMIDs:
10694244 10322101 11529688 11561080 10377029 11752352 8826571 8058773 17394438 19645854 20436887 11454666 24697244 19492852 25686392

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions NCI TEND GuideToPharmacology PharmGKB TTD
ZILEUTON MMP12

Interaction Score: 1.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24074025

Sources:
DTC
ZILEUTON MMP2

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24074025

Sources:
DTC
ZILEUTON CYP2C9

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
ZILEUTON CYP2C19

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
ZILEUTON CYP2D6

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
ZILEUTON CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC

DrugBank: DB00744

Version: 5.1.7

Alternate Names:

ZILEUTON DrugBank Drug Name

111406-87-2 CAS Number

Zileuton Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

Yamashita et al., 2000, Inhibition by troglitazone of the antigen-induced production of leukotrienes in immunoglobulin E-sensitized RBL-2H3 cells., Br. J. Pharmacol.

Guidot et al., 1994, Intrinsic 5-lipoxygenase activity is required for neutrophil responsivity., Proc. Natl. Acad. Sci. U.S.A.

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

ZILEUTON Primary Drug Name

Drug Info:

Drug Class anti-asthmatic agents

Year of Approval 1996

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

Drug Info:

Drug Indications antiinflammatory agent

Drug Class Small Molecule

FDA Approval approved

Publications:

DTC: ZILEUTON

Version: 02-September-2020

Alternate Names:

CHEMBL93 ChEMBL Drug ID

Drug Info:

Publications:

Day JA et al., 2013, Investigating the selectivity of metalloenzyme inhibitors., J Med Chem

Schieferdecker S et al., 2015, Myxochelins target human 5-lipoxygenase., J Nat Prod

Karg EM et al., 2009, Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase., J Med Chem

NCI: ZILEUTON
- Version: 14-September-2017
Alternate Names:

C26667 NCI drug code

Drug Info:

Publications:

Vicente et al., 2001, Modulation of haem oxygenase-1 expression by nitric oxide and leukotrienes in zymosan-activated macrophages., Br. J. Pharmacol.

PharmGKB: zileuton

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Tan EC et al., 2016, Common variants of catechol-O-methyltransferase influence patient-controlled analgesia usage and postoperative pain in patients undergoing total hysterectomy., Pharmacogenomics J

GuideToPharmacology: 178101979
- Version: 29-September-2020
Alternate Names:

ZILEUTON GuideToPharmacology Ligand Name

Drug Info:

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

D09JUG TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL93
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL93
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	Zyflo
Novel drug target	Established target
Mechanism of Interaction	Arachidonate 5-lipoxygenase inhibitor

ZILEUTON	DrugBank Drug Name
111406-87-2	CAS Number
Zileuton	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

ZILEUTON Drug Record

ZILEUTON chembl:CHEMBL93 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25963335

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Zyflo Novel drug target Established target Mechanism of Interaction Arachidonate 5-lipoxygenase inhibitor

PMIDs: 10694244 10322101 11529688 11561080 10377029 11752352 8826571 8058773 17394438 19645854 20436887 11454666 24697244 19492852 25686392

Sources: DTC DrugBank TdgClinicalTrial ChemblInteractions NCI TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24074025

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24074025

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22931300

Sources: DTC

DrugBank: DB00744

Alternate Names: ZILEUTON DrugBank Drug Name 111406-87-2 CAS Number Zileuton Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

TEND: ZILEUTON

Alternate Names: ZILEUTON Primary Drug Name

Drug Info: Drug Class anti-asthmatic agents Year of Approval 1996

Publications:

TdgClinicalTrial: ZILEUTON

Alternate Names:

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

Publications:

DTC: ZILEUTON

Alternate Names: CHEMBL93 ChEMBL Drug ID

Drug Info:

NCI: ZILEUTON

Alternate Names: C26667 NCI drug code

Drug Info:

Publications: Vicente et al., 2001, Modulation of haem oxygenase-1 expression by nitric oxide and leukotrienes in zymosan-activated macrophages., Br. J. Pharmacol.

PharmGKB: zileuton

Alternate Names:

Drug Info:

Publications: Tan EC et al., 2016, Common variants of catechol-O-methyltransferase influence patient-controlled analgesia usage and postoperative pain in patients undergoing total hysterectomy., Pharmacogenomics J

GuideToPharmacology: 178101979

Alternate Names: ZILEUTON GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Zileuton

Alternate Names: D09JUG TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL93

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL93

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
25963335

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Zyflo

Novel drug target Established target

Mechanism of Interaction Arachidonate 5-lipoxygenase inhibitor

PMIDs:
10694244 10322101 11529688 11561080 10377029 11752352 8826571 8058773 17394438 19645854 20436887 11454666 24697244 19492852 25686392

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions NCI TEND GuideToPharmacology PharmGKB TTD

Interaction Types & Directionality:

n/a

PMIDs:
24074025

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24074025

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22931300

Sources:
DTC

Alternate Names:

ZILEUTON DrugBank Drug Name

111406-87-2 CAS Number

Zileuton Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

ZILEUTON Primary Drug Name

Drug Info:

Drug Class anti-asthmatic agents

Year of Approval 1996

Drug Info:

Drug Indications antiinflammatory agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL93 ChEMBL Drug ID

Alternate Names:

C26667 NCI drug code

Publications:

Vicente et al., 2001, Modulation of haem oxygenase-1 expression by nitric oxide and leukotrienes in zymosan-activated macrophages., Br. J. Pharmacol.

Publications:

Tan EC et al., 2016, Common variants of catechol-O-methyltransferase influence patient-controlled analgesia usage and postoperative pain in patients undergoing total hysterectomy., Pharmacogenomics J

Alternate Names:

ZILEUTON GuideToPharmacology Ligand Name

Alternate Names:

D09JUG TTD Drug ID