Teneligliptin

Summary

Teneligliptin (CHEMBL2147777) is an approved small molecule (ATC A10BH08) targeting DPP4, DPP8, and DPP9; 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: A10BH08
• Targets: 3 (DPP4, DPP8, DPP9)
• Indications: 2 conditions
• Clinical trials: 25
• Chemistry: 426.6 Da · C22H30N6OS

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2147777
Name	Teneligliptin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	11949652
ATC	A10BH08
Molecular formula	C22H30N6OS
Molecular weight	426.6
InChIKey	WGRQANOPCQRCME-PMACEKPBSA-N

SMILES: CC1=NN(C(=C1)N2CCN(CC2)[C@H]3C[C@H](NC3)C(=O)N4CCSC4)C5=CC=CC=C5

IUPAC name: [(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone

Also known as: MP-513, Teneligliptin, Teneligliptina, Teneligliptine, TENELIGLIPTIN, TENELIGLIPTIN HYDROBROMIDE HYDRATE, teneligliptin

Parent form; salt/anhydrous children: CHEMBL2147708, CHEMBL5596356

Patent coverage: 515 distinct patent families (1,406 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
DPP4	dipeptidyl peptidase 4	Inhibition	9.43	0%	P27487
DPP8	dipeptidyl peptidase 8	Inhibition	6.59	0.1%	Q6V1X1
DPP9	dipeptidyl peptidase 9	Inhibition	6.27	0.2%	Q86TI2

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Prostaglandin G/H synthase 2, Histamine H1 receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Dipeptidyl peptidase 4, Dipeptidyl peptidase 4, Dipeptidyl peptidase 8, Dipeptidyl peptidase 9.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 9 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P14740	9.54	IC50	0.29	nM	CHEMBL_ACT_12034801
DPP4	9.43	IC50	0.37	nM	CHEMBL_ACT_12035240
DPP4	9.39	Kd	0.41	nM	CHEMBL_ACT_19442628
DPP4	7.92	Kd	11.9	nM	CHEMBL_ACT_19442664
DPP8	6.58	IC50	260	nM	CHEMBL_ACT_12034869
DPP9	6.27	IC50	540	nM	CHEMBL_ACT_12034883
HRH1	5.28	AC50	5200	nM	CHEMBL_ACT_25212291

Target pathways

Aggregated over 3 target gene(s): DPP4, DPP8, DPP9.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
Synthesis, secretion, and inactivation of Glucagon-like Peptide-1 (GLP-1)	1	DPP4
Synthesis, secretion, and inactivation of Glucose-dependent Insulinotropic Polypeptide (GIP)	1	DPP4

Dominant GO biological processes

GO term	Targets
proteolysis	3
negative regulation of programmed cell death	2
protein maturation	2
CARD8 inflammasome complex assembly	2
pyroptotic cell death	2
NLRP1 inflammasome complex assembly	2
behavioral fear response	1
response to hypoxia	1
cell adhesion	1
positive regulation of cell population proliferation	1
negative regulation of extracellular matrix disassembly	1
peptide hormone processing	1
receptor-mediated endocytosis of virus by host cell	1
T cell costimulation	1
regulation of cell-cell adhesion mediated by integrin	1

Indications & clinical

Indications

2 indications (1 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	3	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 25.

Phase distribution

Phase	Trials
PHASE3	11
PHASE1	7
PHASE4	5
PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02449330	PHASE4	UNKNOWN	Teneligliptin on the Progressive Left Ventricular Diastolic Dysfunction With Type 2 Diabetes Mellitus Study
NCT02512523	PHASE4	COMPLETED	Exploratory Study to Compare the Effects of Tenelia® or Januvia® on Glucose Variability in add-on to Metformin (CGMS Study)
NCT03011177	PHASE4	COMPLETED	Teneligliptin Versus Linagliptin in Diabetes Mellitus Type Two Patients
NCT03508323	PHASE4	COMPLETED	Tenelia Elderly CGMS Study(TEDDY)
NCT04446026	PHASE4	COMPLETED	A Randomized, Placebo-controlled Clinical Trial of Teneligliptin as Quadruple Oral Combination Therapy for Type 2 DM After Failure of an Oral Triple Anti-diabetic Regimen
NCT00998881	PHASE3	COMPLETED	Monotherapy Study of MP-513 in Patients With Type 2 Diabetes
NCT01072331	PHASE3	COMPLETED	Pharmacokinetic/Pharmacodynamic Study of MP-513 With Type 2 Diabetes Mellitus
NCT01301833	PHASE3	COMPLETED	Long-term Safety Study of MP-513 in Patients With Type 2 Diabetes
NCT01798238	PHASE3	COMPLETED	Teneligliptin(MP-513) Versus Placebo in Type 2 Diabetes Mellitus
NCT02220907	PHASE3	COMPLETED	Long-Term Safety Study of MT-2412 in Japanese Patients With Type 2 Diabetes
NCT02314637	PHASE3	COMPLETED	Long-term Safety Study of MP-513 as Monotherapy or in Combination With Sulfonylurea in Japanese Type 2 Diabetic Patients
NCT02354222	PHASE3	COMPLETED	Confirmatory Study of MT-2412 in Japanese Patients With Type 2 Diabetes (Add-on Study of Teneligliptin)
NCT02354235	PHASE3	COMPLETED	Confirmatory Study of MT-2412 in Japanese Patients With Type 2 Diabetes (Add-on Study of Canagliflozin)
NCT02567994	PHASE3	COMPLETED	Tenelia Triple Combination Study
NCT02916706	PHASE3	COMPLETED	Efficacy and Safety of Teneligliptin in Chinese Patients With Type 2 Diabetes Mellitus
NCT02924064	PHASE3	COMPLETED	Efficacy and Safety of Teneligliptin in Combination With Metformin in Chinese Patients With Type 2 Diabetes Mellitus
NCT00628212	PHASE2	COMPLETED	Efficacy and Safety Study of MP-513 in Patients With Type 2 Diabetes
NCT03009513	PHASE1	COMPLETED	Teneligliptin-Glimepiride DDI Study
NCT03769870	PHASE1	COMPLETED	Teneligliptin and Atorvastatin DDI Study
NCT03787017	PHASE1	COMPLETED	A Study to Compare MP-513 20mg & Metformin XR 1000mg FDC With Coadministration of the Two Separate Drugs
NCT04431141	PHASE1	COMPLETED	Pharmacokinetic Drug Interaction Between Teneligliptin and Empagliflozin
NCT06339788	PHASE1	COMPLETED	Pharmacokinetics of HD-P023 and Co-administration of Teneligliptin and Empagliflozin High in Healthy Volunteers
NCT06889350	PHASE1	COMPLETED	Pharmacokinetics and Safety of HD-P023 and Co-administration of Teneligliptin and Empagliflozin High in Healthy Volunteers
NCT07102719	PHASE1	COMPLETED	Pharmacokinetics and Safety of HD-P023 and Co-administration of Teneligliptin and Empagliflozin High in Healthy Volunteers
NCT03793023	Not specified	COMPLETED	Observational Study to Evaluate the Efficacy and Safety of Teneligliptin

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 6 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

28 molecules share ≥1 primary target. Top 28 by shared-target count:

Molecule	Source	Status	Shared targets
ALOGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4, DPP8, DPP9
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4, DPP8, DPP9
SAXAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4, DPP8, DPP9
GOSOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
SITAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
VILDAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4, DPP8, DPP9
DUTOGLIPTIN	ChEMBL	Phase 3	DPP4, DPP8, DPP9
TALABOSTAT	ChEMBL	Phase 3	DPP4, DPP8, DPP9
ANAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
EVOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
GEMIFLOXACIN	ChEMBL	Phase 4 (approved)	DPP4
METFORMIN	ChEMBL	Phase 4 (approved)	DPP4
OMARIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
TRELAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
VIDARABINE	ChEMBL	Phase 4 (approved)	DPP4
CAFFEIC ACID	ChEMBL	Phase 3	DPP4
DBPR-108	ChEMBL	Phase 3	DPP4
EPIGALOCATECHIN GALLATE	ChEMBL	Phase 3	DPP4
QUERCETIN	ChEMBL	Phase 3	DPP4
RESVERATROL	ChEMBL	Phase 3	DPP4
RETAGLIPTIN	ChEMBL	Phase 3	DPP4
CARMEGLIPTIN	ChEMBL	Phase 2	DPP4
COFROGLIPTIN	ChEMBL	Phase 2	DPP4
FLAVONE	ChEMBL	Phase 2	DPP4
GALLIC ACID	ChEMBL	Phase 2	DPP4
GENISTEIN	ChEMBL	Phase 2	DPP4
LUTEOLIN	ChEMBL	Phase 2	DPP4
Carfilzomib	PubChem	Approved	DPP4