Nateglinide

Summary

Nateglinide (CHEMBL783) is an approved small-molecule EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor (ATC A10BX03); indicated across 2 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A10BX03
• Indications: 2 conditions
• Clinical trials: 14
• Chemistry: 317.4 Da · C19H27NO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL783
Name	Nateglinide
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5311309
ChEBI	CHEBI:31897
ATC	A10BX03
Molecular formula	C19H27NO3
Molecular weight	317.4
InChIKey	OELFLUMRDSZNSF-OFLPRAFFSA-N

SMILES: CC(C)C1CCC(CC1)C(=O)N[C@H](CC2=CC=CC=C2)C(=O)O

IUPAC name: (2R)-3-phenyl-2-[(4-propan-2-ylcyclohexanecarbonyl)amino]propanoic acid

ChEBI definition: An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.

Pharmacological roles (ChEBI): EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor, hypoglycemic agent.

Also known as: A-4166, AY-4166, AY4166, D-nateglinide, DJN 608, DJN-608, Nateglinida, Nateglinide, NSC-758695, SDZ DJN 608, SDZ-DJN-608, Senaglinide

Patent coverage: 6,412 distinct patent families (25,810 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Fructose-bisphosphate aldolase, Prelamin-A/C, Solute carrier family 22 member 6, Solute carrier family 15 member 2, Cruzipain.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	6.1	Potency	794.3	nM	CHEMBL_ACT_3649221
O35956	5.04	Ki	9200	nM	CHEMBL_ACT_11003314
O35956	5.04	Ki	9200	nM	CHEMBL_ACT_6204585

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
diabetes mellitus	4	MONDO:0005015	EFO:0000400
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 14.

Phase distribution

Phase	Trials
PHASE4	9
PHASE1	3
PHASE2/PHASE3	1
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00212290	PHASE4	COMPLETED	Insulin Resistance and Central Nervous System (CNS) Function in Type 2 Diabetes
NCT00238472	PHASE4	COMPLETED	A Pilot Study to Evaluate the Effects of Nateglinide vs. Glibenclamide on Renal Hemodynamics and Albumin Excretion
NCT00259168	PHASE4	COMPLETED	Insulin Resistance and Vessel Function After Meals: Does Early Intervention Make a Difference?
NCT00319189	PHASE4	COMPLETED	Efficacy and Safety of Nateglinide Treatment in Renal Transplant Recipients
NCT00402909	PHASE4	COMPLETED	Safety and Efficacy of Nateglinide in Patients With Type 2 Diabetes Already Taking Insulin Glargine, Metformin and/or Pioglitazone or Rosiglitazone
NCT00437918	PHASE4	COMPLETED	The Effects of Nateglinide and Acarbose on the Post-Prandial Glucose Control in Type 2 Diabetic Patients
NCT00858013	PHASE4	COMPLETED	Study of the Durability of Glycemic Control With Nateglinide
NCT00928889	PHASE4	COMPLETED	Effects of Nateglinide vs Acarbose on Postprandial Glucose Fluctuation, Dyslipidemia, and Inflammatory Factors
NCT01030952	PHASE4	COMPLETED	Effects of Nateglinide on Postprandial Glucose Excursion by Restoring Early Phase Insulin Secretion
NCT00189774	PHASE2/PHASE3	COMPLETED	Nateglinide: a Double Blind Add-on Study With Pioglitazone for Type 2 Diabetic Patients
NCT01316107	PHASE3	COMPLETED	A Study to Assess Safety and Efficacy of ASP1941 in Combination With Nateglinide in Type 2 Diabetic Patients
NCT01159158	PHASE1	COMPLETED	Bioequivalence Study of Nateglinide Tablets 120 mg of Dr. Reddy’s Laboratories Limited Under Fasting Condition
NCT01160029	PHASE1	COMPLETED	Bioequivalence Study of Nateglinide Tablets 120 mg of Dr. Reddy’s Laboratories Limited Under Fed Condition
NCT02088918	PHASE1	COMPLETED	A Open-label, Single-dose, 2-Sequence, 2-Period, Crossover Study to Assess Safety and Pharmacokinetics of a Nateglinide/Metformin HCl Combined Tablet Compared With a Nateglinide 120 mg Tablet and Metformin HCl 500 mg Tablet Under Fasting Conditions in Healthy Male Subjects

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).