Tiplasinin

Tiplasinin

Clinical data
Other names	Tiplaxtinin; PAI-039
ATC code	None
Identifiers
IUPAC name (1-benzyl-5-(4-(trifluoromethoxy)phenyl)-1H-indol-3-yl)oxoacetic acid
CAS Number	393105-53-8
PubChem CID	6450819
ChemSpider	4953369
UNII	L396QIB983
KEGG	D06160
Chemical and physical data
Formula	C24H16F3NO4
Molar mass	439.390 g·mol−1
3D model (JSmol)	Interactive image
SMILES c2ccccc2Cn(cc1C(=O)C(O)=O)c4c1cc(cc4)-c(cc3)ccc3OC(F)(F)F

Tiplasinin (INN, USAN) or tiplaxtinin (PAI-039) is a drug which acts as an inhibitor of the serpin protein plasminogen activator inhibitor-1 (PAI-1), thereby increasing activity of the enzymes tissue plasminogen activator and urokinase, which are involved in the blood clotting cascade. Inhibition of PAI-1 can help to prevent damage to blood vessel walls that occurs as a consequence of chronic high blood pressure, as well as preventing the formation of blood clots that can lead to stroke and heart attack, and potentially also providing a novel treatment mechanism to slow the development of diabetes and obesity. Tiplasinin was unsuccessful in human clinical trials due to an unfavourable risk to benefit ratio and the need for tight dose control to avoid provoking bleeding disorders, however it is still widely used in scientific research and newer drugs sharing the same mechanism of action are likely to be developed for medical use in future.