Identification

Generic Name
OSI-7904L
DrugBank Accession Number
DB05457
Background

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

Indication

Investigated for use/treatment in gastric cancer.

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
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
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
Toxicity

Acceptable clinical safety profile

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
Affected organisms
Not Available

Chemical Identifiers

UNII
ON177ZCE7M
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. [Article]
  2. Purcell WT, Ettinger DS: Novel antifolate drugs. Curr Oncol Rep. 2003 Mar;5(2):114-25. [Article]
PubChem Substance
347910150
Wikipedia
OSI-7904L

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAdenocarcinoma of the Stomach / Gastro-oesophageal Adenocarcinoma1
2CompletedTreatmentLocally Advanced or Metastatic Adenoca of the Biliary Tract1
1CompletedTreatmentColorectal Cancer1
1CompletedTreatmentSolid Tumors, Advanced Solid Tumors1

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

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
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 at November 18, 2007 18:25 / Updated at June 12, 2020 16:52