Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- CTA018
- DrugBank Accession Number
- DB05024
- Background
CTA018 is a member of a new class of vitamin D analogues with a dual mechanism of action, called Vitamin D Signal Amplifiers. This proprietary new drug is both a potent inhibitor of CYP24 (the enzyme responsible for the breakdown of vitamin D) and a potent activator of vitamin D signaling pathways. CTA018 will be the first drug with this novel dual mechanism of action to enter clinical development. Preclinical studies have shown that CTA018 inhibits the proliferation of rapidly dividing cells such as human epidermal keratinocytes (skin cells) and is also effective in inhibiting pro-inflammatory cytokine secretion which may be involved in the etiology of psoriasis. Cytochroma anticipates that CTA018 will be more potent than currently marketed vitamin D analogues such as calcitriol and calcipotriol and it is expected to have a greater safety index.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Investigated for use/treatment in kidney disease and psoriasis and psoriatic disorders.
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Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Not Available
- Mechanism of action
CTA018 is a rationally designed Vitamin D hormone analog that acts as both a potent VDR agonist and CYP24 inhibitor. The Company believes this dual mechanism of action will provide efficacy and safety advantages over existing Vitamin D hormone replacement therapies for SHPT. CTA018 binds to the VDR located in parathyroid cells and triggers a genomic cascade of events resulting in suppression of PTH secretion. It also binds to the substrate binding pocket of CYP24, a cytochrome P450 enzyme that specifically and efficiently catabolizes Vitamin D hormones. By binding to CYP24 and blocking its activity, CTA018 levels in cells are more readily raised to therapeutic levels. Unlike common cytochrome P450 inhibitors (such as ketoconazole) which act non-specifically on all cytochromes, CTA018 specifically targets CYP24, making drug-drug interactions far less likely. The Company believes the novel dual activity of CTA018 will reduce the incidence of clinically-acquired resistance to Vitamin D hormone replacement therapy, allowing greatly improved efficacy at well tolerated dosages.
Target Actions Organism U1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial Not Available Humans UVitamin D3 receptor Not Available Humans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- XN4TL6M50Z
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Not Available
- External Links
- PubChem Substance
- 347909898
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data2 Completed Treatment Chronic Kidney Disease (CKD) / Renal Failure, Chronic Renal Failure / Renal Insufficiency,Chronic / Secondary Hyperparathyroidism (SHPT) 1 somestatus stop reason just information to hide 2 Completed Treatment Psoriasis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- A cytochrome P450 monooxygenase with a key role in vitamin D catabolism and calcium homeostasis. Via C24- and C23-oxidation pathways, catalyzes the inactivation of both the vitamin D precursor calcidiol (25-hydroxyvitamin D(3)) and the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:11012668, PubMed:15574355, PubMed:16617161, PubMed:24893882, PubMed:29461981, PubMed:8679605). With initial hydroxylation at C-24 (via C24-oxidation pathway), performs a sequential 6-step oxidation of calcitriol leading to the formation of the biliary metabolite calcitroic acid (PubMed:15574355, PubMed:24893882). With initial hydroxylation at C-23 (via C23-oxidation pathway), catalyzes sequential oxidation of calcidiol leading to the formation of 25(OH)D3-26,23-lactone as end product (PubMed:11012668, PubMed:8679605). Preferentially hydroxylates at C-25 other vitamin D active metabolites, such as CYP11A1-derived secosteroids 20S-hydroxycholecalciferol and 20S,23-dihydroxycholecalciferol (PubMed:25727742). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via FDXR/adrenodoxin reductase and FDX1/adrenodoxin (PubMed:8679605)
- Specific Function
- 1-alpha,25-dihydroxyvitamin d3 23-hydroxylase activity
- Gene Name
- CYP24A1
- Uniprot ID
- Q07973
- Uniprot Name
- 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
- Molecular Weight
- 58874.695 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells (PubMed:10678179, PubMed:15728261, PubMed:16913708, PubMed:28698609, PubMed:37478846). Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR (PubMed:28698609). The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes (PubMed:28698609). Plays a central role in calcium homeostasis (By similarity). Also functions as a receptor for the secondary bile acid lithocholic acid (LCA) and its metabolites (PubMed:12016314, PubMed:32354638)
- Specific Function
- Bile acid nuclear receptor activity
- Gene Name
- VDR
- Uniprot ID
- P11473
- Uniprot Name
- Vitamin D3 receptor
- Molecular Weight
- 48288.64 Da
Drug created at October 21, 2007 22:23 / Updated at June 12, 2020 16:52