DGIdb - NATEGLINIDE Drug Record

NATEGLINIDE chembl:CHEMBL783 Approved

Alternate Names:

A-4166
DJN-608
SDZ DJN 608
AY-4166
STARSIS
STARLIX
SDZ-DJN-608
NATEGLINIDE
(-)-N-(TRANS-4-ISOPROPYLCYCLOHEXANECARBONYL)-D-PHENYLALANINE
AY 4166
A 4166
AY4166
DJN608
STARLIX®
TRANS-N-{[4-(1-METHYLETHYL)CYCLOHEXYL]CARBONYL}-D-PHENYLALANINE
chembl:CHEMBL783
drugbank:00731
pubchem.compound:60026
chemidplus:105816-04-4
rxcui:274332

Drug Info:

Year of Approval	2000
Drug Class	hypoglycemic agents
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antidiabetic
Drug Categories	cyclohexanes
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 cyp3a7 substrates
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	glinide
Drug Categories	oat1/slc22a6 inhibitors
Drug Categories	phenylalanine
Drug Categories	potassium channel antagonists
Drug Categories	ugt1a9 substrates

(4 More Sources)

Publications:

Kalliokoski A et al., 2008, Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide., J Clin Pharmacol
Sunaga et al., 2001, The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide., Eur. J. Pharmacol.
Hu et al., 2000, Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: A comparison with sulfonylureas and repaglinide., J. Pharmacol. Exp. Ther.
Chachin et al., 2003, Nateglinide, a D-phenylalanine derivative lacking either a sulfonylurea or benzamido moiety, specifically inhibits pancreatic beta-cell-type K(ATP) channels., J. Pharmacol. Exp. Ther.
Hansen et al., 2002, Differential interactions of nateglinide and repaglinide on the human beta-cell sulphonylurea receptor 1., Diabetes
Dornhorst, 2001, Insulinotropic meglitinide analogues., Lancet
Norman et al., 2001, Nateglinide: A structurally novel, short-acting, hypoglycemic agent., Drugs Today
Cheng Y et al., 2013, Effect of CYP2C9 and SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of nateglinide in healthy Chinese male volunteers., Eur J Clin Pharmacol
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Scarsi et al., 2007, Sulfonylureas and glinides exhibit peroxisome proliferator-activated receptor gamma activity: a combined virtual screening and biological assay approach., Mol. Pharmacol.

NATEGLINIDE ABCC8

Interaction Score: 2.45

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Trial Name Starlix

PMIDs:
11716850 10773014 12604678 12196472 11728565 12764427

Sources:
TdgClinicalTrial DrugBank ChemblInteractions
NATEGLINIDE KCNJ11

Interaction Score: 0.32

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Direct Interaction yes

PMIDs:
None found

Sources:
TEND ChemblInteractions
NATEGLINIDE KCNJ1

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
NATEGLINIDE CALCA

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
NATEGLINIDE SLCO1B1

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18187595

Sources:
PharmGKB
NATEGLINIDE PPARG

Interaction Score: 0.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
17082235

Sources:
DrugBank
NATEGLINIDE CYP2C9

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22842957 22931300

Sources:
DTC PharmGKB
NATEGLINIDE CYP2C19

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
NATEGLINIDE CYP1A2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
NATEGLINIDE CYP2D6

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
NATEGLINIDE CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC PharmGKB

DrugBank: DB00731

Version: 5.1.7

Alternate Names:

105816-04-4 CAS Number

Fastic Drug Brand

Starlix Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Sunaga et al., 2001, The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide., Eur. J. Pharmacol.

Hu et al., 2000, Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: A comparison with sulfonylureas and repaglinide., J. Pharmacol. Exp. Ther.

Chachin et al., 2003, Nateglinide, a D-phenylalanine derivative lacking either a sulfonylurea or benzamido moiety, specifically inhibits pancreatic beta-cell-type K(ATP) channels., J. Pharmacol. Exp. Ther.

TdgClinicalTrial: NATEGLINIDE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval approved

Publications:
TEND: NATEGLINIDE
- Version: 01-August-2011
Alternate Names:

Drug Info:

Drug Class hypoglycemic agents

Year of Approval 2000

Publications:
DTC: NATEGLINIDE
- Version: 02-September-2020
Alternate Names:

CHEMBL783 ChEMBL Drug ID

Drug Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

PharmGKB: nateglinide

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Cheng Y et al., 2013, Effect of CYP2C9 and SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of nateglinide in healthy Chinese male volunteers., Eur J Clin Pharmacol

Kalliokoski A et al., 2008, Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide., J Clin Pharmacol

TTD: Nateglinide
- Version: 2020.06.01
Alternate Names:

D06PSS TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL783
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL783
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Direct Interaction	yes
Mechanism of Interaction	Sulfonylurea receptor 1, Kir6.2 blocker
Trial Name	Starlix

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

blocker (inhibitory)
inhibitor (inhibitory)

NATEGLINIDE Drug Record

NATEGLINIDE chembl:CHEMBL783 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker Trial Name Starlix

PMIDs: 11716850 10773014 12604678 12196472 11728565 12764427

Sources: TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker Direct Interaction yes

PMIDs: None found

Sources: TEND ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18187595

Sources: PharmGKB

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 17082235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22842957 22931300

Sources: DTC PharmGKB

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 PharmGKB

DrugBank: DB00731

Alternate Names: 105816-04-4 CAS Number Fastic Drug Brand Starlix Drug Brand

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

TdgClinicalTrial: NATEGLINIDE

Alternate Names:

Drug Info: Drug Indications antidiabetic Drug Class Small Molecule FDA Approval approved

Publications:

TEND: NATEGLINIDE

Alternate Names:

Drug Info: Drug Class hypoglycemic agents Year of Approval 2000

Publications:

DTC: NATEGLINIDE

Alternate Names: CHEMBL783 ChEMBL Drug ID

Drug Info:

Publications: Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for &gt;200 compounds., Chem Res Toxicol

PharmGKB: nateglinide

Alternate Names:

Drug Info:

TTD: Nateglinide

Alternate Names: D06PSS TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL783

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL783

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Trial Name Starlix

PMIDs:
11716850 10773014 12604678 12196472 11728565 12764427

Sources:
TdgClinicalTrial DrugBank ChemblInteractions

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sulfonylurea receptor 1, Kir6.2 blocker

Direct Interaction yes

PMIDs:
None found

Sources:
TEND ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
18187595

Sources:
PharmGKB

Interaction Types & Directionality:

agonist (activating)

PMIDs:
17082235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
22842957 22931300

Sources:
DTC PharmGKB

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 PharmGKB

Alternate Names:

105816-04-4 CAS Number

Fastic Drug Brand

Starlix Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Drug Info:

Drug Indications antidiabetic

Drug Class Small Molecule

FDA Approval approved

Drug Info:

Drug Class hypoglycemic agents

Year of Approval 2000

Alternate Names:

CHEMBL783 ChEMBL Drug ID

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Alternate Names:

D06PSS TTD Drug ID