Identification
- Generic Name
- G4544
- DrugBank Accession Number
- DB05244
- Background
G4544 is an oral gallium compound that enables oral absorption of the active ingredient contained in Ganite™ (gallium nitrate injection). It targets bone tissue and is actively incorporated into bone mineral at sites where bone is metabolically active.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
For treatment of non-Hodgkin's lymphoma, bone metastases, Paget's disease, and osteoporosis
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G4544 is one of a class of gallium containing compounds that were originally developed by the U.S. National Cancer Institute. In investigational studies, high doses of gallium nitrate demonstrated consistent antitumor activity in patients with non Hodgkin's lymphoma. However, experimental work by Genta personnel and others established that lower doses of gallium directly inhibited calcium release from bone, principally by decreasing bone resorption and possibly by also stimulating bone formation.
- Mechanism of action
G4544 reduces bone loss by inhibiting calcium resorption from bone. Preclinical evidence suggests that the mechanism of G4544 action is multifactorial and different from other current therapies used to treat bone loss, such as estrogen or selective estrogen receptor modulators (SERMs), calcitonin, or bisphosphonates (e.g., Zometa or Fosamax). G4544 preferentially accumulates in metabolically active regions of bone, inhibits osteoclast-mediated bone resorption, and favorably alters bone mineral composition and properties.
- Absorption
Orally bioavailable.
- 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
- Humans and other mammals
Chemical Identifiers
- UNII
- Not Available
- 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
- 347910047
Clinical Trials
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
Drug created at October 21, 2007 22:24 / Updated at June 12, 2020 16:52