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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