e-Drug3D

863

M TICAGRELOR


INN
TICAGRELOR

(is an active metabolite)

cas 220347-05-7
CLASS

BLOOD
P2Y12 PLATELET INHIBITOR
ANTITHROMBOTIC AGENTS

ROUTE (list)

-

ATC code

B01AC24

PK parameters

F 36 PERCENT
VD 88 LITER
Cl 6.7 LITER / HOUR (EQN)
PPB 99 PERCENT
t1/2 9 HOUR

Target

TARGET P2Y12 ADP-RECEPTOR

DrugCentral

P2Y purinoceptor 12 UNIPROT Q9H244 P2RY12

Download SDF file 1,2,3-Cyclopentanetriol, 4-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-, (1S,2R,3S,4R)-

Formula:
C21H24F2N6O3S

Calculated chemical properties:

MW 478.53
NB_atoms 33
XLogP 2.00
PSA 122.17
NB_HD 4
NB_HA 9
fsp3 0.52
Lipinski(0=no;1=yes) 1

FDA
-

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL

e-Drug3D

1524

TICAGRELOR


INN
TICAGRELOR

(has an active metabolite)

cas 274693-27-5
CLASS

BLOOD
P2Y12 PLATELET INHIBITOR
ANTITHROMBOTIC AGENTS

ROUTE (list)

ORAL

ATC code

B01AC24

PK parameters

F 36 PERCENT
VD 88 LITER
Cl 8.7 LITER / HOUR (EQN)
PPB 99 PERCENT
t1/2 7 HOUR

Solubility

AQUEOUS SOLUBILITY OF APPROXIMATELY 10 MICROGRAM / MILLILITER AT ROOM TEMPERATURE


Target

TARGET P2Y12 ADP-RECEPTOR

PDB
5ALC (TICAGRELOR ANTIDOTE CANDIDATE FAB 72 IN COMPLEX WITH TICAGRELOR)

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

Download experimental 3D coordinates of TIQ with added hydrogens

DrugCentral

P2Y purinoceptor 12 UNIPROT Q9H244 P2RY12

Download SDF file (1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5(propylthio)-3H-[1,2,3]-triazolo[4,5-d]pyrimidin-3-yl]-5-(2hydroxyethoxy)cyclopentane-1,2-diol

Formula:
C23H28F2N6O4S

Calculated chemical properties:

MW 522.58
NB_atoms 36
XLogP 2.01
PSA 132.065
NB_HD 4
NB_HA 10
fsp3 0.57
Lipinski(0=no;1=yes) 0

FDA
NDA 022433 (label) INN (TICAGRELOR) BRILINTA (ASTRAZENECA) APPROVAL= AP YEAR= 2011
NDA 208390 (pdf not found) INN (TICAGRELOR) TICAGRELOR (WATSON LABS INC) APPROVAL= AP YEAR= 2018
NDA 208531 (pdf not found) INN (TICAGRELOR) TICAGRELOR (AMNEAL) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 208575 (pdf not found) INN (TICAGRELOR) TICAGRELOR (HISUN PHARM HANGZHOU) APPROVAL= AP YEAR= 2019
NDA 208508 (pdf not found) INN (TICAGRELOR) TICAGRELOR (SUNSHINE) APPROVAL= AP YEAR= 2020
NDA 208596 (pdf not found) INN (TICAGRELOR) TICAGRELOR (MSN) APPROVAL= AP YEAR= 2020
NDA 208597 (pdf not found) INN (TICAGRELOR) TICAGRELOR (MYLAN) APPROVAL= AP YEAR= 2021
NDA 208567 (pdf not found) INN (TICAGRELOR) TICAGRELOR (ALKEM LABS LTD) APPROVAL= AP YEAR= 2023
NDA 208599 (pdf not found) INN (TICAGRELOR) TICAGRELOR (PRINSTON INC) APPROVAL= AP YEAR= 2024
NDA 208541 (pdf not found) INN (TICAGRELOR) TICAGRELOR (DR REDDYS) APPROVAL= AP YEAR= 2024
NDA 208537 (pdf not found) INN (TICAGRELOR) TICAGRELOR (INVAGEN PHARMS) APPROVAL= AP YEAR= 2025
NDA 208576 (pdf not found) INN (TICAGRELOR) TICAGRELOR (ALEMBIC) APPROVAL= AP YEAR= 2025
NDA 208584 (pdf not found) INN (TICAGRELOR) TICAGRELOR (APOTEX) APPROVAL= AP YEAR= 2025
NDA 218962 (pdf not found) INN (TICAGRELOR) TICAGRELOR (SCIEGEN PHARMS) APPROVAL= AP YEAR= 2025
NDA 210219 (pdf not found) INN (TICAGRELOR) TICAGRELOR (ALKEM LABS LTD) APPROVAL= AP YEAR= 2025
NDA 211498 (pdf not found) INN (TICAGRELOR) TICAGRELOR (TARO) APPROVAL= AP YEAR= 2025
NDA 212258 (pdf not found) INN (TICAGRELOR) TICAGRELOR (MACLEODS PHARMS LTD) APPROVAL= AP YEAR= 2025
NDA 216187 (pdf not found) INN (TICAGRELOR) TICAGRELOR (CHANGZHOU PHARM) APPROVAL= AP YEAR= 2025
NDA 208539 (pdf not found) INN (TICAGRELOR) TICAGRELOR (MICRO LABS) APPROVAL= AP YEAR= 2026
NDA 217679 (pdf not found) INN (TICAGRELOR) TICAGRELOR (MANKIND PHARMA) APPROVAL= AP YEAR= 2026
NDA 219006 (pdf not found) INN (TICAGRELOR) TICAGRELOR (ZHEJIANG JINGXIN) APPROVAL= AP YEAR= 2026

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL