Gemigliptin

Summary

Gemigliptin (CHEMBL3707235) is a phase-3 clinical-stage small molecule (ATC A10BH06); indicated across 5 conditions including diabetes mellitus and kidney disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: A10BH06
• Indications: 5 conditions
• Clinical trials: 32
• Chemistry: 489.4 Da · C18H19F8N5O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3707235
Name	Gemigliptin
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11953153
ATC	A10BH06
Molecular formula	C18H19F8N5O2
Molecular weight	489.4
InChIKey	ZWPRRQZNBDYKLH-VIFPVBQESA-N

SMILES: C1CC(CN(C1=O)C[C@H](CC(=O)N2CCC3=C(C2)N=C(N=C3C(F)(F)F)C(F)(F)F)N)(F)F

IUPAC name: 1-[(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one

Also known as: Gemigliptin, Gemigliptina, Gemigliptine, LC-150444, GEMIGLIPTIN

Parent form; salt/anhydrous children: CHEMBL5598215

Patent coverage: 523 distinct patent families (1,360 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,324 (97%) 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

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

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

Indications & clinical

Indications

5 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
kidney disorder	3	MONDO:0005240	EFO:0003086
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
neoplasm	2	MONDO:0005070	MONDO:0004992
liver disorder	1	MONDO:0005154	EFO:0001421

Clinical trials

Total trials: 32.

Phase distribution

Phase	Trials
PHASE1	15
PHASE3	8
PHASE4	4
Not specified	4
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02500329	PHASE4	UNKNOWN	Effect of Gemigliptin or Acarbose on Endothelial Function in Type 2 DM Patients
NCT03202563	PHASE4	COMPLETED	Trial to Evaluate the Efficacy on Glycemic Variability and Safety of Gemigliptin Compared With Dapagliflozin Added on Metformin Alone or Diabetes Medication Naïve Patient in Type 2 Diabetes Mellitus (Stable II Study)
NCT05194592	PHASE4	UNKNOWN	Comparison of the Effects of Dapagliflozin and Gemigliptin on Ketone Metabolism and Cardiac Remodeling in Type 2 Diabetes
NCT05663736	PHASE4	UNKNOWN	Effect of Gemigliptin Versus Glimepiride on Cardiac Diastolic Function in Patients With Type 2 Diabetes
NCT01787396	PHASE3	COMPLETED	Phase III Trial to Evaluate the Efficacy and Safety of Initial Combination Therapy With Gemigliptin 50mg q.d and Metformin q.d
NCT01968044	PHASE3	COMPLETED	A Phase IIIb Study to Evaluate the Safety and Efficacy of Gemigliptin in Type 2 Diabetes Mellitus Patients With Moderate or Severe Renal Impairment(GUARD Study)
NCT01990469	PHASE3	COMPLETED	Efficacy and Safety of Gemigliptin 50mg qd Added in Patients With Type 2 Diabetes Inadequately Controlled on Glimepiride and Metformin
NCT02089126	PHASE3	UNKNOWN	Phase III Trial to Evaluate the Efficacy and Safety of Gemigliptin 50mg qd Added to Ongoing Glimepiride as Fix-dose Combination in Patients With Type 2 Diabetes
NCT02250872	PHASE2/PHASE3	UNKNOWN	Effects of DPP4 Inhibitor on Cisplatin Induced Acute Kidney Injury
NCT02343926	PHASE3	COMPLETED	Phase 3 Study to Compare the Efficacy and Safety of Gemigliptin and Vildagliptin as Add-on Therapy to Metformin in People With Type 2 Diabetes Inadequately Controlled With Metformin
NCT02831361	PHASE3	COMPLETED	Trial to Evaluate the Efficacy and Safety of Gemigliptin Compared With Placebo Added on Insulin Alone or on Insulin in Combination With Metformin in Type 2 DM (ZEUS II Study)
NCT03842267	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of Gemigliptin in Type 2 Diabetes Who Have Inadequate GlycemIc Control With Dapagliflozin and Metformin (SOLUTION Study)
NCT04255238	PHASE3	UNKNOWN	A Study to Evaluate the Efficacy and Safety of Dual add-on Therapy With Gemigliptin 50 mg and Dapagliflozin 10 mg Added to Metformin Who Have Inadequate Glycemic Control on Metformin Alone
NCT01001013	PHASE1	COMPLETED	Pharmacokinetic Drug Interaction Between LC15-0444 and Pioglitazone After Oral Administration in Healthy Male Subjects
NCT01426399	PHASE1	COMPLETED	Pharmacokinetic/Pharmacodynamic Drug-drug Interaction of LC15-0444 and Metformin After Oral Administration in Healthy Male Subjects
NCT01595880	PHASE1	COMPLETED	BE Study of the Combinations of Gemigliptin 50mg and Metformin HCl Extended Release 500mg in Comparison to Each Component Administered Alone
NCT01662674	PHASE1	COMPLETED	BE Study of the Combinations of Gemigliptin 50mg and Metformin HCl Extended Release 1000mg in Comparison to Each Component Administered Alone
NCT01768455	PHASE1	COMPLETED	Pharmacokinetic Drug Interaction Study Between Gemigliptin and Glimepiride in Healthy Male Subjects
NCT01823133	PHASE1	COMPLETED	Study for Investigate the Pharmacokinetic Drug Interactions Between Gemigliptin and Rosuvastatin
NCT01825850	PHASE1	COMPLETED	Pharmacokinetic Drug Interaction Study Between Gemigliptin and Irbesartan After Oral Administration in Healthy Male Subjects
NCT02004587	PHASE1	COMPLETED	Influence of Hepatic Impairment on Pharmacokinetic (PK) and Pharmacodynamic (PD) of Gemigliptin PK and PD After Multiple Oral Doses in Healthy White Volunteers
NCT02056600	PHASE1	COMPLETED	BE Study of the Combinations of Gemigliptin 50mg and Metformin HCl Extended Release 1000mg in Comparison to Each Component Administered Alone.
NCT02670018	PHASE1	UNKNOWN	BE Study of the Combinations of Gemigliptin 50mg and Metformin HCl Extended Release 2000mg in Comparison to Each Component Administered Alone
NCT02670070	PHASE1	UNKNOWN	BE Study of the Combinations of Gemigliptin 50mg and Rosuvastatin 20mg in Comparison to Each Component Administered Alone
NCT03310749	PHASE1	COMPLETED	An Assessment of Pharmacokinetic Gemigliptin and Metformin Interactions in Healthy Mexican Volunteers
NCT03565458	PHASE1	UNKNOWN	Gemigliptin, Dapagliflozin, Empagliflozin DDI Study
NCT03864432	PHASE1	COMPLETED	An Ascending Dose, Single/Multiple Dosing, Food Effect Clinical Trial to Evaluate Pharmacokinetics, Safety and Tolerability in Healthy Subjects After Oral Administration of Gemigliptin (Phase I)
NCT04070794	PHASE1	UNKNOWN	Food-effect Bioavailability of Fixed Dose Combination Zemimet® SR Tab. 50/1000 mg Under Fed and Fasting Conditions
NCT02186080	Not specified	COMPLETED	Effect of Gemigliptin on Metabolic Endotoxemia and Lipemia
NCT02290301	Not specified	COMPLETED	An Observational Study to Evaluate Cardiovascular Outcomes of T2DM PatientsTreated With Gemigliptin
NCT02609815	Not specified	COMPLETED	Initial Combination of Gemigliptin and Metformin on Microbiota Change
NCT04705506	Not specified	COMPLETED	Gemigliptin and Biomarkers of Kidney Injury and Vascular Calcification

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 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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