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BI-4122
- Development stage
- Preclinical
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
BI-4122 is an orally available, highly potent, and selective small molecule dual inhibitor of vanin-1 (VNN1) and vanin-2 (VNN2). Developed by Boehringer Ingelheim, BI-4122 reversibly and competitively blocks the enzymatic pantetheinase activity of vanin-1 and vanin-2, thereby preventing the conversion of pantetheine into pantothenic acid and cysteamine. This inhibition modulates cellular redox homeostasis and attenuates inflammatory and fibrotic signaling. BI-4122 has been investigated in preclinical models of chronic kidney disease, such as unilateral ureteral obstruction (UUO), where it significantly reduces tubulointerstitial fibrosis and suppresses proinflammatory mediators like IL-1β and IL-6.
02
Targets
VNN1 (Vanin-1)VNN2 (Vanin-2)
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