Drug intelligence / Profile preview

CTA018 + MT2832

Development stage
Unknown
Lead developer
Posner Lab
Modality
Small Molecules
Administration
Oral
01

Overview

**CTA018 + MT2832** is a combination of two compounds: CTA018, a vitamin D analogue that acts as a dual **vitamin D receptor (VDR) agonist** and **CYP24A1 antagonist**, and MT2832, an agent with limited publicly available mechanistic information. CTA018 selectively binds and activates the VDR, promoting its gene expression, while also potently inhibiting the vitamin D metabolizing enzyme CYP24A1, making it notably more effective than ketoconazole at reducing CYP24A1 activity. This dual action addresses vitamin D deficiency and resistance in chronic kidney disease (CKD) and related conditions. CTA018 exhibits distinct binding site interactions in the VDR (His393) and CYP24A1 (Met246, Glu329), facilitating VDR-mediated transcription and suppression of excessive vitamin D breakdown. The combination is being developed primarily for CKD-associated secondary hyperparathyroidism (sHPT) and disorders of vitamin D metabolism[1][3].

Brand names
CTA018 + MT2832
Other names
CTA-018 + MT-2832CTA-018/MT2832
02

Targets

CYP24A1 (Cytochrome P450 family 24 subfamily A member 1)VDR (Vitamin D receptor)

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