e-Drug3D

1513

LINAGLIPTIN


INN
LINAGLIPTIN

cas 668270-12-0
CLASS

METABOLISM
BLOOD GLUCOSE LOWERING
DIPEPTIDYL PEPTIDASE-4 (DPP-4) INHIBITOR
TYPE 2 DIABETES MELLITUS

ROUTE (list)

ORAL

ATC code

A10BH05
A10BD19
A10BD11
A10BD27

PK parameters

F 30 PERCENT
Tmax 1.5 HOUR
VD 1110 LITER
Cl 76 LITER / HOUR (EQN)
PPB 84 PERCENT
t1/2 12 HOUR (5 MILLIGRAM)

Solubility

VERY SLIGHTLY SOLUBLE IN WATER 0.9 MILLIGRAM / MILLILITER


Target

TARGET DPP-4
DIPEPTIDYL PEPTIDASE-4

PDB
2RGU (CRYSTAL STRUCTURE OF COMPLEX OF HUMAN DPP4 AND INHIBITOR)

Ligand code = 356 (link to the list of PDB complexes)

Download experimental 3D coordinates of 356 with added hydrogens

DrugCentral

Dipeptidyl peptidase 4 UNIPROT P27487 DPP4

Download SDF file 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-

Formula:
C25H28N8O2

Calculated chemical properties:

MW 472.55
NB_atoms 35
XLogP 1.15
PSA 100.572
NB_HD 2
NB_HA 10
fsp3 0.40
Lipinski(0=no;1=yes) 1

FDA
NDA 201280 (pdf not found) INN (LINAGLIPTIN) TRADJENTA (BOEHRINGER INGELHEIM) APPROVAL= AP YEAR= 2011 NEWMOLECULARENTITY
NDA 201281 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) JENTADUETO (BOEHRINGER INGELHEIM) APPROVAL= AP YEAR= 2012
NDA 206073 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN) GLYXAMBI (BOEHRINGER INGELHEIM) APPROVAL= AP YEAR= 2015
NDA 208026 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) JENTADUETO XR (BOEHRINGER INGELHEIM) APPROVAL= AP YEAR= 2016
NDA 208415 (pdf not found) INN (LINAGLIPTIN) LINAGLIPTIN (AUROBINDO PHARMA LTD) APPROVAL= TA YEAR= 2017
NDA 208430 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) LINAGLIPTIN; METFORMIN HYDROCHLORIDE (MYLAN PHARMS INC) APPROVAL= TA YEAR= 2018
NDA 208454 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) LINAGLIPTIN AND METFORMIN HYDROCHLORIDE (SUN PHARM INDS LTD) APPROVAL= TA YEAR= 2020
NDA 212359 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN) EMPAGLIFLOZIN AND LINAGLIPTIN (MSN LABS PVT LTD) APPROVAL= TA YEAR= 2020
NDA 212614 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) TRIJARDY XR (BOEHRINGER INGELHEIM) APPROVAL= AP YEAR= 2020
NDA 212354 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN) EMPAGLIFLOZIN; LINAGLIPTIN (KINAPSE LIMITED) APPROVAL= TA YEAR= 2020
NDA 208427 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) LINAGLIPTIN AND METFORMIN HYDROCHLORIDE (DR REDDYS LABS LTD) APPROVAL= TA YEAR= 2021
NDA 212364 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN) EMPAGLIFLOZIN; LINAGLIPTIN (ANNORA PHARMA) APPROVAL= TA YEAR= 2021
NDA 208335 (pdf not found) INN (LINAGLIPTIN) LINAGLIPTIN (SUNSHINE) APPROVAL= AP YEAR= 2021
NDA 208336 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) LINAGLIPTIN AND METFORMIN HYDROCHLORIDE (SUNSHINE) APPROVAL= AP YEAR= 2021
NDA 208473 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) LINAGLIPTIN AND METFORMIN HYDROCHLORIDE (PRINSTON PHARMA INC) APPROVAL= TA YEAR= 2022
NDA 212264 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN) EMPAGLIFLOZIN AND LINAGLIPTIN (PRINSTON PHARMA INC) APPROVAL= TA YEAR= 2022
NDA 212366 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN) EMPAGLIFLOZIN; LINAGLIPTIN (ALKEM LABS LTD) APPROVAL= TA YEAR= 2022
NDA 208448 (pdf not found) INN (LINAGLIPTIN) LINAGLIPTIN (ZYDUS PHARMS) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 208449 (pdf not found) INN (LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) LINAGLIPTIN AND METFORMIN HYDROCHLORIDE (ZYDUS PHARMS) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 217049 (pdf not found) INN (EMPAGLIFLOZIN ; LINAGLIPTIN ; METFORMIN HYDROCHLORIDE) EMPAGLIFLOZIN; LINAGLIPTIN; METFORMIN HYDROCHLORIDE (ZYDUS PHARMS USA INC) APPROVAL= TA YEAR= 2024
NDA 208423 (pdf not found) INN (LINAGLIPTIN) LINAGLIPTIN (INVAGEN PHARMS) APPROVAL= AP YEAR= 2024
NDA 208428 (pdf not found) INN (LINAGLIPTIN) LINAGLIPTIN (DR REDDYS LABS LTD) APPROVAL= TA YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL