e-Drug3D

1809

TIPIRACIL

INN
TIPIRACIL

cas 183204-74-2

CLASS

ANTINEOPLASTIC
THYMIDINE PHOSPHORYLASE INHIBITOR
TREATMENT OF PATIENTS WITH METASTATIC COLORECTAL CANCER
TIPIRACIL INCREASES TRIFLURIDINE EXPOSURE BY INHIBITING ITS METABOLISM BY THYMIDINE PHOSPHORYLASE

ROUTE (list)

ORAL

ATC code

PK parameters

PPB 8 PERCENT
t1/2 2.1 HOUR

Solubility

SOLUBLE IN WATER

Target

TARGET THYMIDINE PHOSPHORYLASE

PDB
1UOU (CRYSTAL STRUCTURE OF HUMAN THYMIDINE PHOSPHORYLASE IN COMPLEX WITH A SMALL MOLECULE INHIBITOR)

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

Download experimental 3D coordinates of CMU with added hydrogens

DrugCentral

Thymidine phosphorylase UNIPROT P19971 TYMP

Download SDF file

2,4(1H,3H)-Pyrimidinedione, 5-chloro-6-[(2-imino-1-pyrrolidinyl)methyl]-

Formula:
C9H11ClN4O2

Calculated chemical properties:

MW 242.67
NB_atoms 16
XLogP 0.29
PSA 85.29
NB_HD 3
NB_HA 6
fsp3 0.44
Lipinski(0=no;1=yes) 1

FDA
NDA 207981 (label) INN (TIPIRACIL HYDROCHLORIDE ; TRIFLURIDINE) LONSURF (TAIHO ONCOLOGY) APPROVAL= AP YEAR= 2015
NDA 214036 (pdf not found) INN (TRIFLURIDINE ; TIPIRACIL) TRIFLURIDINE; TIPIRACIL (INTAS PHARMS LTD) APPROVAL= TA YEAR= 2022
NDA 214008 (pdf not found) INN (TIPIRACIL HYDROCHLORIDE ; TRIFLURIDINE) TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE (NATCO) APPROVAL= AP YEAR= 2023
NDA 214024 (pdf not found) INN (TIPIRACIL HYDROCHLORIDE ; TRIFLURIDINE) TIPIRACIL HYDROCHLORIDE AND TRIFLURIDINE (MSN) APPROVAL= AP YEAR= 2025