Drug intelligence / Profile preview

TM5614

Development stage
Phase 2
Lead developer
Renascience
Modality
Drug Delivery Systems
Administration
Oral
01

Overview

TM5614 is a novel, orally active plasminogen activator inhibitor-1 (PAI-1) inhibitor. It works by inhibiting PAI-1 activity, which consequently leads to the downregulation of hepatic PCSK9 transcription, resulting in decreased plasma levels of PCSK9. This reduction in PCSK9 levels lowers the catabolism of LDL receptors, allowing more LDL-C to be cleared from circulation. PAI-1 is a marker associated with obesity, type 2 diabetes, and metabolic syndrome, making its inhibition a target for treating these conditions. TM5614 has shown promising results and a favorable safety profile in various clinical trials for indications including advanced melanoma, chronic myeloid leukemia (CML), and cutaneous angiosarcoma.

Other names
PAI-1 inhibitor RS5614PAI1 inhibitor RS5614PAI 1 inhibitor RS5614
02

Targets

PAI-1 (Plasminogen activator inhibitor type 1)PCSK9 (Proprotein convertase subtilisin/kexin type 9)

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