NAV

OSI-7904L

Targets (1)

Identification

Name
OSI-7904L
Accession Number
DB05457
Description

OSI-7904L is a liposome encapsulated thymidylate synthase inhibitor, which is indicated for use in advanced gastric and/or gastroesophageal adenocarcinoma (A-G/GEJA). Current treatments also inhibit thymidylate synthase but the innovative lipid coating of OSI-7904L allows for more enduring results with administration of the TS inhibitor.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Pharmacology
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Indication

Investigated for use/treatment in gastric cancer.

Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

OSI-7904L is a liposome encapsulated thymidylate synthase inhibitor, which is indicated for use in advanced gastric and/or gastroesophageal adenocarcinoma (A-G/GEJA). Current treatments also inhibit thymidylate synthase but the innovative lipid coating of OSI-7904L allows for more enduring results with administration of the TS inhibitor.

Mechanism of action

Inhibits thymidylate synthase.

TargetActionsOrganism
UThymidylate synthaseNot 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
Medicalerrors
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Toxicity

Acceptable clinical safety profile

Affected organisms
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
Classification
Not classified

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
  1. Desjardins J, Emerson DL, Colagiovanni DB, Abbott E, Brown EN, Drolet DW: Pharmacokinetics, safety, and efficacy of a liposome encapsulated thymidylate synthase inhibitor, OSI-7904L [(S)-2-[5-[(1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl]amino-1-oxo- 2-isoindolynl]-glutaric acid] in mice. J Pharmacol Exp Ther. 2004 Jun;309(3):894-902. Epub 2004 Feb 24. [PubMed:14982966]
  2. Purcell WT, Ettinger DS: Novel antifolate drugs. Curr Oncol Rep. 2003 Mar;5(2):114-25. [PubMed:12583828]
PubChem Substance
347910150
Wikipedia
OSI-7904L

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentGastric Adenocarcinoma / Gastroesophageal Adenocarcinoma1
2CompletedTreatmentLocally Advanced or Metastatic Adenoca of the Biliary Tract1
1CompletedTreatmentAdvanced Solid Tumors1
1CompletedTreatmentColorectal Cancers1

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

Targets

Drugtargets
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Details1. Thymidylate synthase
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Thymidylate synthase activity
Specific Function
Contributes to the de novo mitochondrial thymidylate biosynthesis pathway.
Gene Name
TYMS
Uniprot ID
P04818
Uniprot Name
Thymidylate synthase
Molecular Weight
35715.65 Da

Drug created on November 18, 2007 18:25 / Updated on June 12, 2020 16:52