INCB7839

Identification

Name
INCB7839
Accession Number
DB05033
Description

INCB7839 is a novel, orally available ADAM metalloprotease inhibitor that is designed to block activation of the epidermal growth factor (EGFR) pathways. It represents a potentially important new class of targeted breast cancer therapy. It has shown promising clinical activity in heavily pretreated, refractory breast cancer patients.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Pharmacology
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Indication

Investigated for use/treatment in breast cancer.

Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics
Not Available
Mechanism of action

INCB7839 is a novel, orally available ADAM metalloprotease inhibitor that is designed to block activation of the epidermal growth factor (EGFR) pathways. Currently approved therapies that target the EGFR pathways have shown promising efficacy in metastatic disease, validating these pathways as targets; however, efficacy may be limited due to the fact that these drugs inhibit only one or two of the four HER receptor pathways. In contrast, the sheddase inhibitor, INCB7839, has the potential to inhibit activation through all four of the HER receptors, resulting in more complete inhibition of these pathways.

TargetActionsOrganism
UDisintegrin and metalloproteinase domain-containing protein 9Not 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
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Toxicity
Not Available
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
Not Available
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
Not Available
PubChem Substance
347909903

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentAnaplastic Astrocytoma (AA) / Anaplastic Oligodendroglioma (AO) / CNS Primary Tumor, NOS (Malignant Glioma) / DIPG / Glioblastoma Multiforme (GBM) / High-grade Astrocytoma NOS1
1, 2CompletedTreatmentDiffuse Large B Cell Non-Hodgkin Lymphoma1

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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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Probable zinc protease. May mediate cell-cell or cell-matrix interactions. Isoform 2 displays alpha-secretase activity for APP.
Gene Name
ADAM9
Uniprot ID
Q13443
Uniprot Name
Disintegrin and metalloproteinase domain-containing protein 9
Molecular Weight
90555.29 Da

Drug created on October 21, 2007 22:23 / Updated on June 12, 2020 16:52