Results of the Non-Steroidal Mineralocorticoid Receptor Antagonist KBP-5074 Compared with Eplerenone in a Rat Model of Mineralocorticoid-Induced Renal Injury Published in Frontiers in Pharmacology
Aug 06, 2021

PRINCETON, N.J., 6 August, 2021 -- KBP Biosciences Co., Ltd. (“KBP Biosciences” or the “Company”), a clinical-stage biotechnology company dedicated to research, development, and commercialization of innovative medicines for the global market, today announced publication of “The Non-Steroidal Mineralocorticoid Receptor Antagonist KBP 5074 Limits Albuminuria and has Improved Therapeutic Index Compared With Eplerenone in a Rat Model With Mineralocorticoid-Induced Renal Injury” in the peer-reviewed journal, Frontiers in Pharmacology. The paper was published in the June 2021 issue (DOI: 10.3389/fphar.2021.604928) with Professor Frederic Jaisser, as the lead author.

A uninephrectomized Sprague Dawley rat model of aldosterone-mediated renal disease was used to evaluate the therapeutic indices (TIs) and efficacy of the non-steroidal mineralocorticoid receptor antagonist (MRA) KBP-5074 and steroidal MRA eplerenone. The TI was calculated for each drug as the ratio of the concentration of drug producing 50% of maximum effect (EC50) for serum K+ to the EC50 for UACR. The TIs were 24.5 for KBP-5074 and 0.620 for eplerenone, resulting in a 39-fold improved TI for KBP-5074 compared with eplerenone. Additionally, the urinary Na+ and Na+/K+ ratio significantly increased at the middle and high doses of KBP-5074, but only at the highest dose of eplerenone. These results showed an increased TI and efficacy of KBP-5074 compared with eplerenone over a wider therapeutic window.

“The steroidal MRAs have been shown to be effective in reducing CV mortality and hospitalizations for heart failure in patients with heart failure and a reduced left ventricular ejection fraction as well as reducing blood pressure and albuminuria in patients with hypertension and / or chronic kidney disease (CKD). The study by Jaisser et al. shows that the new non-steroidal MRA KBP-5074 has an increased therapeutic index and efficacy over a wide dose range as compared to the steroidal MRA eplerenone in a renal impairment model. These results suggest that KBP-5074 has the potential to provide an even greater benefit to patients with advanced CKD than the steroidal MRAs,” said Dr. Bertram Pitt, M.D., Professor Emeritus, University of Michigan Medical School.

“This study demonstrates that the novel non-steroidal MRA KBP-5074 is more efficacious in reducing UACR than steroidal MRA eplerenone and increases therapeutic index in a chronic kidney disease rat model. These findings are consistent with the clinical results from the BLOCK-CKD study which showed KBP-5074 is an efficacious and safe treatment for CKD patients,” said Jay Zhang, Ph.D., Vice President of Discovery for KBP Biosciences and co-author of the manuscript.
Link to the publication in Frontiers in Pharmacology:

About KBP Biosciences

KBP Biosciences is a global, clinical-stage biotechnology company focused on discovering, developing, and commercializing innovative small-molecule therapeutics for the treatment of serious cardiorenal and infectious diseases with large unmet needs. Headquartered in Princeton, NJ, KBP Biosciences principally devotes its resources to major organ protection and anti-infectives therapeutic areas.

KBP Biosciences’ lead product candidate, KBP-5074, is a potentially best-in-class, next-generation, non-steroidal Mineralocorticoid Receptor Antagonist (MRA) discovered and developed by KBP’s scientists, and is being developed globally to initially treat Stage 3b/4, or moderate-to-severe, Chronic Kidney Disease (CKD) patients with uncontrolled hypertension. KBP Biosciences’ second product candidate, KBP-7072, a potentially best-in-class, potent, broad spectrum aminomethylcycline, is being developed as an anti-infective for Gram-positive, Gram-negative and anaerobic bacteria, including multi-drug resistant pathogens.

KBP Biosciences has built a proprietary small-molecule drug discovery platform to advance its pipeline of product candidates. The platform includes state-of-the-art processes for novel drug compound identification, high-volume screening and optimization, along with its substantial library of diverse chemical entities and select potential compounds. With its discovery platform, KBP Biosciences is able to generate a multitude of drug compounds and quickly identify the most promising differentiated and potent product candidates.

About KBP-5074

KBP-5074 is a non-steroidal MRA discovered and developed by KBP Biosciences. KBP-5074 selectively binds to recombinant human MRs with much higher affinity than to recombinant human glucocorticoid, progesterone, and androgen receptors, suggesting that KBP-5074 should be effective in blocking the hypertensive and renal tissue damaging effects of aldosterone with reduced risk of pro-diabetic and adverse endocrine effects. KBP-5074 has been investigated in eight phase 1 studies and the BLOCK-CKD phase 2b study. Phase 3 study preparations has been  closely consulted with the FDA’s Division of Cardiology and Nephrology.

For more information about KBP Biosciences, please visit the company website at


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