Overview

Vitamin D Basics

Therapeutic Focus

 

CTA018 Injection

CTA018 Injection is a novel vitamin D analog with a dual mechanism of action that combines vitamin D hormone functions with CYP24 enzyme inhibition.  CTA018 Injection is under development for the treatment of secondary hyperparathyroidism (SHPT) in Stage 5 CKD patients.  SHPT remains poorly treated by existing therapies as the vast majority of patients are unable to simultaneously attain targets for serum intact parathyroid hormone (iPTH), serum calcium and serum phosphorus, as set forth in the National Kidney Foundation (NKF) Kidney/Disease Outcomes Quality Initiative (K/DOQI) guidelines for SHPT.  As a result of the inadequacy of current treatments, physicians must constantly adjust the prescribed dose and often interrupt dosing in an attempt to balance effectiveness with the avoidance of treatment-related side effects.  Cytochroma, in collaboration with the research group of Prof. Gary H. Posner at The Johns Hopkins University, has developed CTA018 and a portfolio of additional candidates that address these weaknesses. CTA018 Injection is expected to provide superior control of serum iPTH without having an adverse impact on serum calcium and serum phosphorus levels.

Mechanism of Action

Treatment of SHPT is most often accomplished with traditional vitamin D hormone therapies such as paricalcitol or doxercalciferol. CTA018 Injection represents the first product in a new generation of vitamin D hormone therapies that have been rationally designed to increase safety and efficacy through a unique dual mechanism of action. Like traditional therapies, CTA018 activates the vitamin D signaling pathway by binding to intracellular vitamin D receptors (VDR). Unlike traditional therapies, CTA018 also reduces the catabolism of vitamin D hormones by binding to and thereby blocking CYP24. CYP24 rapidly catabolizes vitamin D hormones with high specificity and has the function of protecting cells from excessive intracellular levels of vitamin D hormones. CTA018’s novel dual mechanism of action elicits the desired therapeutic response while reducing clinically acquired resistance to vitamin D hormone therapy caused by CYP24. The Company believes that CTA018 Injection will provide nephrologists with a safer and more effective therapeutic option for managing more advanced SHPT. 

Dual mechanism of action: CTA018 activates VDR-mediated gene regulation and inhibits CYP24.

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