Tetrathiomolybdate
Identification
- Generic Name
- Tetrathiomolybdate
- DrugBank Accession Number
- DB05088
- Background
Tetrathiomolybdate is an oral, small-molecule, anticopper agent that is highly specific for lowering the levels of free copper in serum. COPREXA has completed pivotal clinical trials for the treatment of neurologic Wilson's disease. It is also developed for fibrotic disorders based upon the rationale that the fibrotic disease process is dependent upon the availability of free copper in the body.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
- Weight
- Average: 224.19
Monoisotopic: 225.794787 - Chemical Formula
- MoS4
- Synonyms
- Thiomolybdate
- Tiomolibdate ion
- External IDs
- ATN-224
Pharmacology
- Indication
Investigated for use/treatment in liver disease and pulmonary fibrosis.
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- Pharmacodynamics
Tetrathiomolybdate demonstrated the ability to reduce toxic free copper levels and substantially improve clinical neurologic outcomes in Wilson’s patients. Studies also showed it is capable of specifically inhibiting chronic fibrotic disease processes in the lung.
- Mechanism of action
Tetrathiomolybdate has demonstrated the ability to inhibit fibrosis in a number of well established animal models through the sequestration of available copper and inhibition of key fibrotric cytokines, including secreted protein acid rich in cysteine (SPARC), NFkappaB, TGF-beta, FGF-2, IL-1, IL-6, IL-8, and connective tissue growth factor (CTGF).
Target Actions Organism UAmyloid beta A4 protein 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAmbroxol The risk or severity of methemoglobinemia can be increased when Tetrathiomolybdate is combined with Ambroxol. Articaine The risk or severity of methemoglobinemia can be increased when Tetrathiomolybdate is combined with Articaine. Benzocaine The risk or severity of methemoglobinemia can be increased when Tetrathiomolybdate is combined with Benzocaine. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Tetrathiomolybdate is combined with Benzyl alcohol. Bupivacaine The risk or severity of methemoglobinemia can be increased when Tetrathiomolybdate is combined with Bupivacaine. - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Choline tetrathiomolybdate FD57A79R4P 649749-10-0 NEYVHGQOGHJAAD-UHFFFAOYSA-N - International/Other Brands
- Copexa / Coprexa
Categories
- Drug Categories
- Adenosine Triphosphatases, antagonists & inhibitors
- Angiogenesis Modulating Agents
- Antineoplastic Agents
- Chelating Agents
- Compounds used in a research, industrial, or household setting
- Elements
- Enzyme Inhibitors
- Growth Inhibitors
- Growth Substances
- Metals
- Metals, Heavy
- Sequestering Agents
- Transition Elements
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 91U3TGV99T
- CAS number
- 16330-92-0
- InChI Key
- CXVCSRUYMINUSF-UHFFFAOYSA-N
- InChI
- InChI=1S/Mo.4S/q;;;2*-1
- IUPAC Name
- (sulfanidyldisulfanylidenemolybdenio)sulfanide
- SMILES
- [S-][Mo]([S-])(=S)=S
References
- General References
- Not Available
- External Links
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Completed Treatment Primary Biliary Cholangitis 1 3 Completed Treatment Wilson's Disease 1 3 Terminated Treatment Wilson's Disease 1 2 Active Not Recruiting Treatment Breast Cancer 1 2 Completed Treatment Colorectal Carcinoma (CRC) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 300 °C with decomposition Not Available - Predicted Properties
Property Value Source logP 1.57 Chemaxon pKa (Strongest Acidic) 9.2 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 0 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 0 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 37.74 m3·mol-1 Chemaxon Polarizability 14.29 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.8526 Blood Brain Barrier + 0.9565 Caco-2 permeable + 0.5325 P-glycoprotein substrate Non-substrate 0.8815 P-glycoprotein inhibitor I Non-inhibitor 0.9718 P-glycoprotein inhibitor II Non-inhibitor 0.9958 Renal organic cation transporter Non-inhibitor 0.9404 CYP450 2C9 substrate Non-substrate 0.8471 CYP450 2D6 substrate Non-substrate 0.8348 CYP450 3A4 substrate Non-substrate 0.7961 CYP450 1A2 substrate Non-inhibitor 0.7649 CYP450 2C9 inhibitor Non-inhibitor 0.7287 CYP450 2D6 inhibitor Non-inhibitor 0.9226 CYP450 2C19 inhibitor Non-inhibitor 0.8342 CYP450 3A4 inhibitor Non-inhibitor 0.9357 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7635 Ames test Non AMES toxic 0.7926 Carcinogenicity Carcinogens 0.6589 Biodegradation Not ready biodegradable 0.9497 Rat acute toxicity 2.4587 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9173 hERG inhibition (predictor II) Non-inhibitor 0.9494
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Transition metal ion binding
- Specific Function
- Functions as a cell surface receptor and performs physiological functions on the surface of neurons relevant to neurite growth, neuronal adhesion and axonogenesis. Involved in cell mobility and tra...
- Gene Name
- APP
- Uniprot ID
- P05067
- Uniprot Name
- Amyloid beta A4 protein
- Molecular Weight
- 86942.715 Da
References
- Venti A, Giordano T, Eder P, Bush AI, Lahiri DK, Greig NH, Rogers JT: The integrated role of desferrioxamine and phenserine targeted to an iron-responsive element in the APP-mRNA 5'-untranslated region. Ann N Y Acad Sci. 2004 Dec;1035:34-48. [Article]
Drug created at October 21, 2007 22:23 / Updated at September 28, 2023 05:47