Gallium maltolate

Identification

Generic Name
Gallium maltolate
DrugBank Accession Number
DB05420
Background

Gallium maltolate is Titan’s novel oral agent in development for the potential treatment of chronic bacterial infections, bone disease and cancer.

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 445.032
Monoisotopic: 443.997181
Chemical Formula
C18H15GaO9
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in bladder cancer, lymphoma (unspecified), multiple myeloma, paget's disease, and prostate cancer.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action

Gallium maltolate is a novel orally active formulation of gallium, a semi-metallic element that is a potent inhibitor of ribonucleotide reductase, an enzyme that promotes tumor growth.Gallium is also known to concentrate in malignant tumors and sites of infection, and appears to favorably impact calcium deposition, making bones more resistant to degradation caused by cancer metastasis. Titan's novel product, gallium maltolate, may significantly expand the therapeutic potential of gallium by providing the advantages of enhanced bioavailablity, a potentially improved therapeutic profile and ease of administration.

TargetActionsOrganism
URibonucleoside-diphosphate reductase large subunitNot AvailableHumans
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
Adverseeffects
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Toxicity

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
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pyranones and derivatives. These are compounds containing a pyran ring which bears a ketone.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyrans
Sub Class
Pyranones and derivatives
Direct Parent
Pyranones and derivatives
Alternative Parents
Heteroaromatic compounds / Cyclic ketones / Oxacyclic compounds / Organic zwitterions / Organic salts / Organic oxides / Hydrocarbon derivatives
Substituents
Aromatic heteromonocyclic compound / Cyclic ketone / Heteroaromatic compound / Hydrocarbon derivative / Organic oxide / Organic oxygen compound / Organic salt / Organic zwitterion / Organooxygen compound / Oxacycle
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
17LEI49C2G
CAS number
108560-70-9
InChI Key
ASYYOZSDALANRF-UHFFFAOYSA-K
InChI
InChI=1S/3C6H6O3.Ga/c3*1-4-6(8)5(7)2-3-9-4;/h3*2-3,8H,1H3;/q;;;+3/p-3
IUPAC Name
gallium(3+) ion tris(2-methyl-4-oxo-4H-pyran-3-olate)
SMILES
[Ga+3].CC1=C([O-])C(=O)C=CO1.CC1=C([O-])C(=O)C=CO1.CC1=C([O-])C(=O)C=CO1

References

General References
  1. Martens RJ, Mealey K, Cohen ND, Harrington JR, Chaffin MK, Taylor RJ, Bernstein LR: Pharmacokinetics of gallium maltolate after intragastric administration in neonatal foals. Am J Vet Res. 2007 Oct;68(10):1041-4. [Article]
  2. Chitambar CR, Purpi DP, Woodliff J, Yang M, Wereley JP: Development of gallium compounds for treatment of lymphoma: gallium maltolate, a novel hydroxypyrone gallium compound, induces apoptosis and circumvents lymphoma cell resistance to gallium nitrate. J Pharmacol Exp Ther. 2007 Sep;322(3):1228-36. Epub 2007 Jun 28. [Article]
  3. Chua MS, Bernstein LR, Li R, So SK: Gallium maltolate is a promising chemotherapeutic agent for the treatment of hepatocellular carcinoma. Anticancer Res. 2006 May-Jun;26(3A):1739-43. [Article]
PubChem Compound
9846339
PubChem Substance
347827728
ChemSpider
8022053
Wikipedia
Gallium_maltolate

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Not Yet RecruitingTreatmentGlioblastoma Multiforme (GBM)1
1, 2TerminatedTreatmentMalignant Lymphomas / Multiple Myeloma (MM) / Neoplasms, Bladder / Prostatic Neoplasms1

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
PropertyValueSource
Water Solubility0.0149 mg/mLALOGPS
logP2.56ALOGPS
logP0.55ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)9.45ChemAxon
pKa (Strongest Basic)-3.6ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area49.36 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity44.27 m3·mol-1ChemAxon
Polarizability11.26 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ribonucleoside-diphosphate reductase activity, thioredoxin disulfide as acceptor
Specific Function
Provides the precursors necessary for DNA synthesis. Catalyzes the biosynthesis of deoxyribonucleotides from the corresponding ribonucleotides.
Gene Name
RRM1
Uniprot ID
P23921
Uniprot Name
Ribonucleoside-diphosphate reductase large subunit
Molecular Weight
90069.375 Da

Drug created on November 18, 2007 18:24 / Updated on June 12, 2020 16:52