Trelagliptin

Summary

Trelagliptin (CHEMBL1650443) is an approved small molecule; indicated across 1 condition including type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 1 condition
• Clinical trials: 19
• Chemistry: 357.4 Da · C18H20FN5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1650443
Name	Trelagliptin
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	15983988
Molecular formula	C18H20FN5O2
Molecular weight	357.4
InChIKey	IWYJYHUNXVAVAA-OAHLLOKOSA-N

SMILES: CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCC[C@H](C3)N

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

Also known as: SYR-472, Trelagliptin, Trelagliptina, Trelagliptine, TRELAGLIPTIN, trelagliptin, TRELAGLIPTIN SUCCINATE

Parent form; salt/anhydrous children: CHEMBL1650456, CHEMBL1650457, CHEMBL2105754

Patent coverage: 493 distinct patent families (1,367 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,023 (75%) 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

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Dipeptidyl peptidase 4.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
DPP4	8.89	IC50	1.3	nM	CHEMBL_ACT_18057404
DPP4	8.89	IC50	1.3	nM	CHEMBL_ACT_25636159
DPP4	8.85	IC50	1.43	nM	CHEMBL_ACT_18357664
DPP4	8.82	Ki	1.5	nM	CHEMBL_ACT_25636194
DPP4	8.4	IC50	4	nM	CHEMBL_ACT_5192908
DPP4	8.29	Ki	5.1	nM	CHEMBL_ACT_18357686
DPP4	8.27	IC50	5.4	nM	CHEMBL_ACT_25636168

Target pathways

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

Indications & clinical

Indications

1 disease in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 19.

Phase distribution

Phase	Trials
PHASE3	7
Not specified	5
PHASE4	4
PHASE2	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02771093	PHASE4	COMPLETED	An Exploratory Study of the Effects of Trelagliptin and Alogliptin on Glucose Variability in Patients With Type 2 Diabetes Mellitus
NCT03014479	PHASE4	COMPLETED	Study of the QOL Evaluation of Trelagliptin in Patients 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
NCT04374864	PHASE4	UNKNOWN	Dose Modification Requirement for Trelagliptin in Egyptian Population
NCT07073768	PHASE3	ENROLLING_BY_INVITATION	Comparison Between Efficacy of Trelagliptin and Sitagliptin in Type II Diabetic Patients
NCT01431807	PHASE3	COMPLETED	Long-term Study of SYR-472
NCT01632007	PHASE3	COMPLETED	Double-blind Comparative Study of SYR-472
NCT01751360	PHASE3	COMPLETED	SYR-472 Open-label Study
NCT02324569	PHASE3	COMPLETED	A Phase 4, Randomized, Double-blind, Parallel-group, Comparative Study and a Phase 4, Open-label, Long-term Study of SYR-472 (100 mg) in Combination With Insulin in Patients With Type 2 Diabetes
NCT02512068	PHASE3	COMPLETED	A Phase 3, Randomized, Double-blind, Parallel-group, Comparative Study and a Phase 3, Multicenter, Open-label, Long-term Study of SYR-472 (25 mg) in Patients With Type 2 Diabetes Mellitus Complicated by Severe Renal Impairment or End-stage Renal Disease
NCT03940183	PHASE3	COMPLETED	Clinical Trial of Trelagliptin Succinate Tablets in the Treatment of Type 2 Diabetes
NCT00653185	PHASE2	COMPLETED	Efficacy of SYR-472 in Subjects With Type 2 Diabetes Mellitus
NCT00760344	PHASE2	COMPLETED	Efficacy and Safety of SYR-472 in Subjects With Type 2 Diabetes Mellitus
NCT02372097	PHASE1	COMPLETED	A Phase 1, Bioequivalence Study of SYR-472 25mg and 50mg Tablets
NCT06889909	Not specified	ACTIVE_NOT_RECRUITING	Comparison of Once-Weekly Trelagliptin Vs. Once-Daily Vildagliptin for HbA1c Reduction in Type 2 Diabetes
NCT06913101	Not specified	ACTIVE_NOT_RECRUITING	Comparison of Once-Weekly Trelagliptin vs. Once-Daily Vildagliptin for HbA1c Reduction in Type 2 Diabetes
NCT03362398	Not specified	COMPLETED	Omarigliptin & Trelagliptin in Twelve Healthy Egyptian Volunteers
NCT03555591	Not specified	COMPLETED	Specified Drug-Use Survey of Trelagliptin Tablets Survey on Long-term Use in Patients With Type 2 Diabetes Mellitus
NCT04285983	Not specified	COMPLETED	Specified Drug-Use Survey of Trelagliptin Tablets Survey on Long-term Use in Type 2 Diabetes Mellitus Patients With Severe Renal Impairment or End-stage Renal Disease

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).