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

Stem definition	Drug id	CAS RN
antihyperglycaemics	1886	105816-04-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nateglinide D-Nateglinide glinate glunate natelide senaglinide	A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES. Molecular weight: 317.43 Formula: C19H27NO3 CLOGP: 4.30 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 66.40 ALOGS: -4.57 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nateglinide
D-Nateglinide
glinate
glunate
natelide
senaglinide

A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.

Molecular weight: 317.43
Formula: C19H27NO3
CLOGP: 4.30
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 66.40
ALOGS: -4.57
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.36	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	73 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	16.20 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	13 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	1.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.50 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.32 mg/mL	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	0.15 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.03 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 22, 2000	FDA	NOVARTIS

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
Lactic acidosis	71.89	23.83	27	1166	38260	63449569
Blood glucose increased	43.18	23.83	24	1169	83732	63404097
Glycosylated haemoglobin increased	27.87	23.83	10	1183	12388	63475441
Hypoglycaemia	25.02	23.83	15	1178	60050	63427779

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FDA Adverse Event Reporting System (Male)

None

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
Hypoglycaemia	48.43	21.14	31	2024	101563	79640770
Lactic acidosis	47.89	21.14	27	2028	70332	79672001
Blood glucose increased	31.40	21.14	25	2030	114950	79627383

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A10BX03	ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Other blood glucose lowering drugs, excl. insulins
CHEBI has role	CHEBI:35526	antidiabetic
CHEBI has role	CHEBI:68612	dipeptidyl peptidase-4 inhibitors
FDA EPC	N0000175428	Glinide
FDA MoA	N0000175448	Potassium Channel Antagonists
MeSH PA	D007004	Hypoglycemic 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
Diabetes mellitus type 2	indication	44054006	DOID:9352
Infectious disease	contraindication	40733004
Hypopituitarism	contraindication	74728003	DOID:9406
Disease of liver	contraindication	235856003	DOID:409
Hypoglycemic disorder	contraindication	237630007
Primary adrenocortical insufficiency	contraindication	373662000
Fever	contraindication	386661006
Surgical procedure	contraindication	387713003
Traumatic injury	contraindication	417746004

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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	3.79	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
Sulfonylurea receptor 1, Kir6.2	Ion channel	Q09428 Q14654	ABCC8_HUMAN KCJ11_HUMAN	BLOCKER	Ki	6.46	WOMBAT-PK	CHEMBL
Sulfonylurea receptor 2, Kir6.2	Ion channel	O60706 Q14654	ABCC9_HUMAN KCJ11_HUMAN	BLOCKER	Ki	4.99	WOMBAT-PK
Solute carrier family 22 member 6	Transporter		S22A6_RAT		Ki	5.04	CHEMBL

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External reference:

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ID	Source
009028	NDDF
134604002	SNOMEDCT_US
15875	MMSL
167424	MMSL
274332	RXNORM
387070004	SNOMEDCT_US
4021252	VUID
4021252	VANDF
41X3PWK4O2	UNII
5311309	PUBCHEM_CID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Nateglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3354	TABLET	60 mg	ORAL	ANDA	26 sections
Nateglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3354	TABLET	60 mg	ORAL	ANDA	26 sections
Nateglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3355	TABLET	120 mg	ORAL	ANDA	26 sections
Nateglinide	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3355	TABLET	120 mg	ORAL	ANDA	26 sections
NATEGLINIDE	Human Prescription Drug Label	1	16571-758	TABLET	60 mg	ORAL	ANDA	26 sections
NATEGLINIDE	Human Prescription Drug Label	1	16571-758	TABLET	60 mg	ORAL	ANDA	26 sections
NATEGLINIDE	Human Prescription Drug Label	1	16571-759	TABLET	120 mg	ORAL	ANDA	26 sections
NATEGLINIDE	Human Prescription Drug Label	1	16571-759	TABLET	120 mg	ORAL	ANDA	26 sections
Nateglinide	HUMAN PRESCRIPTION DRUG LABEL	1	42291-636	TABLET, COATED	60 mg	ORAL	ANDA	24 sections
Nateglinide	HUMAN PRESCRIPTION DRUG LABEL	1	42291-637	TABLET, COATED	120 mg	ORAL	ANDA	24 sections

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