Alogliptin

Summary

Alogliptin (CHEMBL376359) is an approved small-molecule EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor (ATC A10BH04) targeting DPP4; 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: A10BH04
• Targets: 1 (DPP4)
• Indications: 2 conditions
• Clinical trials: 56
• Chemistry: 339.4 Da · C18H21N5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL376359
Name	Alogliptin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11450633
ChEBI	CHEBI:72323
ATC	A10BH04
Molecular formula	C18H21N5O2
Molecular weight	339.4
InChIKey	ZSBOMTDTBDDKMP-OAHLLOKOSA-N

SMILES: CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCC[C@H](C3)N

IUPAC name: 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile

ChEBI definition: A piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of type 2 diabetes.

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

Also known as: Alogliptin, Alogliptina, Alogliptine, Vipidia, ALOGLIPTIN, Alogliptin benzoateÊ, Alogliptin benzoateÂ, alogliptin

Parent form; salt/anhydrous children: CHEMBL227529, CHEMBL459806, CHEMBL458537

Patent coverage: 1,469 distinct patent families (3,750 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,145 (84%) of the total. 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	8.5	0%	P27487

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Mu-type opioid receptor, Kappa-type opioid receptor, Dipeptidyl peptidase 4, Dipeptidyl peptidase 4.

Bioactivity

ChEMBL activities: 38 potent at pChembl ≥ 5 of 38 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DPP4	9	IC50	1	nM	CHEMBL_ACT_6335422
DPP4	8.82	IC50	1.5	nM	CHEMBL_ACT_13441713
DPP4	8.67	IC50	2.13	nM	CHEMBL_ACT_29093883
DPP4	8.62	Kd	2.4	nM	CHEMBL_ACT_19442631
DPP4	8.6	IC50	2.5	nM	CHEMBL_ACT_29093917
DPP4	8.59	IC50	2.56	nM	CHEMBL_ACT_25050576
DPP4	8.59	IC50	2.6	nM	CHEMBL_ACT_25050710
DPP4	8.57	IC50	2.7	nM	CHEMBL_ACT_19301472
DPP4	8.57	IC50	2.7	nM	CHEMBL_ACT_25050704
DPP4	8.51	IC50	3.1	nM	CHEMBL_ACT_23297211
DPP4	8.47	IC50	3.4	nM	CHEMBL_ACT_10869442
DPP4	8.47	IC50	3.4	nM	CHEMBL_ACT_5177081
DPP4	8.4	IC50	4	nM	CHEMBL_ACT_12044049
DPP4	8.4	IC50	4	nM	CHEMBL_ACT_18493702
DPP4	8.4	IC50	4	nM	CHEMBL_ACT_22800202
DPP4	8.4	IC50	4	nM	CHEMBL_ACT_25050565
DPP4	8.35	IC50	4.46	nM	CHEMBL_ACT_19099027
DPP4	8.28	IC50	5.3	nM	CHEMBL_ACT_18057405
DPP4	8.28	IC50	5.3	nM	CHEMBL_ACT_25636158
DPP4	8.24	IC50	5.71	nM	CHEMBL_ACT_29093912
DPP4	8.16	IC50	6.9	nM	CHEMBL_ACT_15714330
DPP4	8.16	IC50	6.85	nM	CHEMBL_ACT_25050689
DPP4	8.15	IC50	7	nM	CHEMBL_ACT_15065873
DPP4	8.15	IC50	7	nM	CHEMBL_ACT_19442621
DPP4	8.15	IC50	7	nM	CHEMBL_ACT_24995360
DPP4	8.15	IC50	7	nM	CHEMBL_ACT_25636110
DPP4	8.15	IC50	7	nM	CHEMBL_ACT_5192916
DPP4	8.12	IC50	7.6	nM	CHEMBL_ACT_16609233
DPP4	8.12	IC50	7.5	nM	CHEMBL_ACT_24967496
DPP4	8.12	IC50	7.5	nM	CHEMBL_ACT_25636155

Target pathways

Aggregated over 1 target gene(s): DPP4.

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
behavioral fear response	1
response to hypoxia	1
proteolysis	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
locomotory exploration behavior	1
psychomotor behavior	1
T cell activation	1
endothelial cell migration	1
symbiont entry into host cell	1

Indications & clinical

Indications

2 indications (0 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	3	MONDO:0005015	EFO:0000400
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 56.

Phase distribution

Phase	Trials
PHASE3	22
Not specified	10
PHASE4	8
PHASE2/PHASE3	7
PHASE1	5
PHASE2	4

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07289750	PHASE4	NOT_YET_RECRUITING	The Effect of Alogliptin Combined With Actoplus Met on Glucose and Lipid Metabolism and Pancreatic Function in Patients With T2DM Complicated With MAFLD
NCT02231021	PHASE4	COMPLETED	The Practical Evidence of Antidiabetic Combination Therapy in Korea
NCT02763007	PHASE4	TERMINATED	An Extension Study of PEAK Trial
NCT02771093	PHASE4	COMPLETED	An Exploratory Study of the Effects of Trelagliptin and Alogliptin on Glucose Variability in Patients With Type 2 Diabetes Mellitus
NCT03042325	PHASE4	WITHDRAWN	Safety and Efficacy of Alogliptin in Indian Participants With Type 2 Diabetes Mellitus
NCT03231709	PHASE4	COMPLETED	Treatment Preference for Weekly Dipeptidyl Peptidase-4 (DPP-4) Inhibitors Versus Daily DPP-4 Inhibitors in Participants With Type 2 Diabetes Mellitus
NCT03499704	PHASE4	COMPLETED	A Study to Evaluate the Effect of add-on Pioglitazone or Dapagliflozin in Participants With Type 2 Diabetes Mellitus Inadequately Controlled by DPP-4 Inhibitor and Metformin Therapy
NCT03794336	PHASE4	COMPLETED	Efficacy and Safety of Alogliptin vs. Acarbose in Chinese Type 2 Diabetes Mellitus (T2DM) Patients With High CV Risk or CHD Treated With Aspirin and Inadequately Controlled With Metformin Monotherapy or Drug Naive
NCT07093476	PHASE3	RECRUITING	Efficacy and Safety of Add-On Therapy With Empagliflozin in Patients With Type 2 Diabetes on a Background of Alogliptin and Metformin
NCT00286429	PHASE3	COMPLETED	Efficacy and Safety Study of Alogliptin and Insulin in the Treatment of Type 2 Diabetes.
NCT00286442	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Combined With Metformin in Participants With Type 2 Diabetes Mellitus
NCT00286455	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin in Subjects With Type 2 Diabetes
NCT00286468	PHASE3	COMPLETED	Study of Alogliptin Combined With Sulfonylurea in Subjects With Type 2 Diabetes Mellitus.
NCT00286494	PHASE3	COMPLETED	Study of Alogliptin Combined With Pioglitazone in Subjects With Type 2 Diabetes Mellitus
NCT00306384	PHASE3	COMPLETED	Long-term Safety of Alogliptin in Patients With Type 2 Diabetes Mellitus
NCT00328627	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Combined With Pioglitazone in Treating Subjects With Type 2 Diabetes Mellitus.
NCT00395512	PHASE3	COMPLETED	Efficacy of Alogliptin With Pioglitazone (Actos®) in Subjects With Type 2 Diabetes Mellitus
NCT00432276	PHASE3	COMPLETED	Efficacy of Alogliptin and Pioglitazone in Subjects With Type 2 Diabetes Mellitus
NCT00655863	PHASE3	COMPLETED	Efficacy of Alogliptin and With Pioglitazone in Patients With Type 2 Diabetes.
NCT00707993	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Compared to Glipizide in Elderly Diabetics
NCT00856284	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Plus Metformin Compared to Glipizide Plus Metformin in Patients With Type 2 Diabetes Mellitus
NCT00968708	PHASE3	COMPLETED	Cardiovascular Outcomes Study of Alogliptin in Patients With Type 2 Diabetes and Acute Coronary Syndrome
NCT01023581	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Plus Metformin in Patients With Type 2 Diabetes
NCT01263483	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Used in Combination With α-glucosidase Inhibitor in Participants With Type 2 Diabetes in Japan
NCT01263509	PHASE2/PHASE3	COMPLETED	Long-term Safety Study of Alogliptin Used in Combination With α-glucosidase Inhibitor in Participants With Type 2 Diabetes in Japan
NCT01289119	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin in Participants With Type 2 Diabetes
NCT01318070	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Used Combination With Thiazolidine in Participants With Type 2 Diabetes in Japan
NCT01318083	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Used in Combination With Sulfonylurea in Participants With Type 2 Diabetes in Japan
NCT01318109	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Alogliptin Used Combination With Metformin in Participants With Type 2 Diabetes in Japan
NCT01318122	PHASE2/PHASE3	COMPLETED	Long-term Safety Study of Alogliptin Used in Combination With Thiazolidine in Participants With Type 2 Diabetes in Japan
NCT01318135	PHASE2/PHASE3	COMPLETED	Long-term Safety Study of Alogliptin Used in Combination With Sulfonylurea or Metformin in Participants With Type 2 Diabetes in Japan
NCT01456130	PHASE3	COMPLETED	Long-term Study of Alogliptin as an Add-on to Rapid-Acting Insulin Secretagogues in Type 2 Diabetes
NCT01521962	PHASE3	COMPLETED	Study of Combination Therapy With SYR-322
NCT01632007	PHASE3	COMPLETED	Double-blind Comparative Study of SYR-472
NCT01890122	PHASE3	COMPLETED	Efficacy and Safety of Alogliptin and Metformin Fixed-Dose Combination in Participants With Type 2 Diabetes
NCT02068443	PHASE3	COMPLETED	Comparative Study to Evaluate Efficacy and Safety When Metformin Hydrochloride 500 mg Once Daily is Added on to SYR-322 25 mg in Type 2 Diabetic Patients With Inadequate Glycemic Control Despite Treatment With SYR-322 25 mg in Addition to Diet and Exercise Therapy
NCT05782192	PHASE3	COMPLETED	SAL067 Treatment in Patients With Type 2 Diabetes Who Are Not Controlled With Diet and Exercise
NCT00755846	PHASE2	COMPLETED	Safety and Efficacy Study of Alogliptin on Glycemic Control in Subjects With Type 2 Diabetes.
NCT00763347	PHASE2	TERMINATED	Efficacy and Safety Study of SYR-619 in Treating Subjects With Type 2 Diabetes Mellitus
NCT01263470	PHASE2	COMPLETED	Efficacy and Safety of Alogliptin in Participants With Type 2 Diabetes in Japan

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 3 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
LINAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4
SAXAGLIPTIN	ChEMBL + PubChem	Phase 4 (approved)	DPP4
ANAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
EVOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
GEMIFLOXACIN	ChEMBL	Phase 4 (approved)	DPP4
GOSOGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
METFORMIN	ChEMBL	Phase 4 (approved)	DPP4
OMARIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
SITAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
TENELIGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
TRELAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
VIDARABINE	ChEMBL	Phase 4 (approved)	DPP4
VILDAGLIPTIN	ChEMBL	Phase 4 (approved)	DPP4
CAFFEIC ACID	ChEMBL	Phase 3	DPP4
DBPR-108	ChEMBL	Phase 3	DPP4
DUTOGLIPTIN	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
TALABOSTAT	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