治疗糖尿病肾病的新选择-非奈利酮

Diabetes is one of the major health problems in global society. Diabetic kidney disease (DKD) is a complication of systemic microvascular disease in diabetes. DKD is often combined with microvascular disease in other organs or systems, such as diabetic retinopathy, peripheral neuropathy, etc. Diabetes is also a major cause of chronic kidney disease and cardiovascular disease. On July 9, 2021, the FDA approved the launch of film-coated tablets for the treatment of chronic kidney disease patients with type 2 diabetes. The trade name is Kerendia. This is the first approved indication for fenelidone. Today, I will tell you about this new drug fenelidone for the treatment of diabetic nephropathy.

Finelidone is a highly selective nonsteroidal mineralocorticoid receptor antagonist (MRA) that does not show L-type calcium channel activity and has no significant effect on 65 different enzymes and ion channels, suggesting that Finelidone is highly specific. This specificity is primarily mediated through hydrogen bond donor interactions with mineralocorticoid receptor (MR)-specific residues Ala773 and Ser810. There is evidence that compared with steroidal MRA, fenelinone has significantly different binding adaptability to the MR ligand-binding domain, which leads to the protrusion of MR helix 12, which in turn renders MR activation ineffective and ultimately leads to its rapid degradation. It can be seen that fenelidone has a novel and special mechanism of inactivating MR signaling.

In the phase II clinical trial (ARTS), fenelidone had little effect on serum potassium and renal function in patients with heart failure combined with CKD/type 2 diabetes, and could effectively reduce NT-proBNP and proteinuria. In the recently announced phase III clinical study (FIDELIO-DKD), in patients with type 2 diabetes and CKD, based on the maximum tolerated dose of renin-angiotensin-aldosterone system (RAAS) blocker (ACEI/ARB) treatment, fenelidone significantly reduced the risk of renal composite endpoint events by 18% and the risk of cardiovascular composite key events by 14%.

Note: The above information comes from the Internet and is compiled and edited by Medical Companion Travel (please correct me if there are any errors or omissions). It is only to provide information on the latest drugs on the market in the world and help Chinese patients understand the latest international new drug trends. It is only for internal discussion among medical staff and does not serve as any basis for medication. For specific medication guidelines, please consult the attending physician.