bempedoic-acid

Description: Bempedoic acid (ESP-55016; ETC-1002), a novel and potent ATP-citrate lyase (ACL) inhibitor, is an orally bioavailable, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid is a regulator of lipid and carbohydrate metabolism.

References:

1. PinkoskySL, et al. AMP-activated protein kinase and ATP-citrate lyase are twodistinct molecular targets for ETC-1002, a novel small moleculeregulator of lipid and carbohydrate metabolism. J Lipid Res. 2013Jan; 54(1):134-51.

2. FilippovS, et al. ETC-1002 regulates immune response, leukocyte homing, andadipose tissue inflammation via LKB1-dependent activation of macrophageAMPK. J Lipid Res. 2013 Aug; 54(8):2095-108.

3. Adenosine triphosphate citrate lyase: Emerging target in the treatment of dyslipidemia. J Clin Lipidol. 2015 May-Jun; 9(3):384-9.