e-Drug3D

1571

APIXABAN


INN
APIXABAN

cas 503612-47-3
CLASS

BLOOD
ANTICOAGULANT
ACTIVE SITE INHIBITOR OF FXA

ROUTE (list)

ORAL

ATC code

B01AF02

PK parameters

F 50 PERCENT
Tmax 3.5 HOUR
VD 21 LITER
Cl 3.3 LITER / HOUR
PPB 87 PERCENT
t1/2 12 HOUR

Solubility

AQUEOUS SOLUBILITY ACROSS THE PHYSIOLOGICAL PH RANGE IS 0.04 MILLIGRAM / MILLILITER


Target

TARGET FACTOR XA

PDB
2P16 (FACTOR XA IN COMPLEX WITH THE INHIBITOR APIXABAN (BMS-562247) AKA 1-(4-METHOXYPHENYL)-7-OXO-6-(4-(2-OXO-1-PIPERIDINYL)PHENYL)-4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[3, 4-C]PYRIDINE-3-CARBOXAMIDE)

Ligand code = GG2 (link to the list of PDB complexes)

Download experimental 3D coordinates of GG2 with added hydrogens

DrugCentral

Coagulation factor X UNIPROT P00742 F10

Download SDF file 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4c]pyridine-3-carboxamide

Formula:
C25H25N5O4

Calculated chemical properties:

MW 459.50
NB_atoms 34
XLogP 2.70
PSA 102.756
NB_HD 2
NB_HA 9
fsp3 0.28
Lipinski(0=no;1=yes) 1

FDA
NDA 202155 (label) INN (APIXABAN) ELIQUIS (BRISTOL MYERS SQUIBB) APPROVAL= AP YEAR= 2012
NDA 209944 (pdf not found) INN (APIXABAN) APIXABAN (SUNSHINE LAKE) APPROVAL= TA YEAR= 2019
NDA 210013 (pdf not found) INN (APIXABAN) APIXABAN (MICRO LABS) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 210128 (pdf not found) INN (APIXABAN) APIXABAN (MYLAN) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 210171 (pdf not found) INN (APIXABAN) APIXABAN (SUN PHARM INDUSTRIES) APPROVAL= TA YEAR= 2019
NDA 210152 (pdf not found) INN (APIXABAN) APIXABAN (BIONPHARMA) APPROVAL= AP YEAR= 2020 DISCONTINUED
NDA 209898 (pdf not found) INN (APIXABAN) APIXABAN (INDOCO) APPROVAL= AP YEAR= 2020
NDA 210180 (pdf not found) INN (APIXABAN) APIXABAN (ACCORD HLTHCARE) APPROVAL= AP YEAR= 2020
NDA 210082 (pdf not found) INN (APIXABAN) APIXABAN (DR REDDYS LABS INC) APPROVAL= TA YEAR= 2020
NDA 210142 (pdf not found) INN (APIXABAN) APIXABAN (TEVA PHARMS USA INC) APPROVAL= TA YEAR= 2020
NDA 209845 (pdf not found) INN (APIXABAN) APIXABAN (BRECKENRIDGE) APPROVAL= AP YEAR= 2021 DISCONTINUED
NDA 210053 (pdf not found) INN (APIXABAN) APIXABAN (SIGMAPHARM LABS LLC) APPROVAL= TA YEAR= 2022
NDA 210133 (pdf not found) INN (APIXABAN) APIXABAN (PRINSTON PHARMA INC) APPROVAL= TA YEAR= 2022
NDA 213903 (pdf not found) INN (APIXABAN) APIXABAN (ZHEJIANG YONGNING PHARMACEUTICAL CO LTD) APPROVAL= TA YEAR= 2022
NDA 210026 (pdf not found) INN (APIXABAN) APIXABAN (AUROBINDO PHARMA LTD) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 210066 (pdf not found) INN (APIXABAN) APIXABAN (HETERO LABS LTD V) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 210185 (pdf not found) INN (APIXABAN) APIXABAN (ZYDUS PHARMS) APPROVAL= AP YEAR= 2023 DISCONTINUED
NDA 210156 (pdf not found) INN (APIXABAN) APIXABAN (TORRENT) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 210091 (pdf not found) INN (APIXABAN) APIXABAN (APOTEX) APPROVAL= AP YEAR= 2024 DISCONTINUED
NDA 209810 (pdf not found) INN (APIXABAN) APIXABAN (IMPAX) APPROVAL= AP YEAR= 2025 DISCONTINUED
NDA 210067 (pdf not found) INN (APIXABAN) APIXABAN (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2025 DISCONTINUED
NDA 218119 (pdf not found) INN (APIXABAN) APIXABAN (SCIEGEN PHARMACEUTICALS INC) APPROVAL= TA YEAR= 2025
NDA 220073 (label) INN (APIXABAN) ELIQUIS SPRINKLE (BRISTOL) APPROVAL= AP YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL