Drug intelligence / Profile preview

TM5441

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

TM5441 is an orally bioavailable **small molecule inhibitor** of **plasminogen activator inhibitor-1 (PAI-1)**, a serine protease inhibitor involved in regulating fibrinolysis and associated with various pathological conditions[1][2][3]. By specifically inhibiting PAI-1, TM5441 increases activity of tissue plasminogen activator and urokinase, thus promoting the breakdown of blood clots[1]. TM5441 has demonstrated protective and therapeutic effects in preclinical models of **hepatic steatosis (NAFLD), obesity, metabolic syndrome, diabetic nephropathy, inflammatory kidney injury, lung fibrosis, and cancer**, primarily by preventing tissue fibrosis, inflammation, and promoting mitochondrial biogenesis[3][5]. Unlike some other PAI-1 inhibitors, TM5441 lacks significant bleeding risk and does not inhibit other serine proteases such as antithrombin III or α2-antiplasmin[3]. Although TM5441 shows promising activity in animal models and cellular assays, it has not been approved for medical use and is primarily used in scientific research[1][2].

02

Targets

PAI-1 (Plasminogen activator inhibitor type 1)

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