Drug & Cancer & Variant
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Search content: Drug = AEE-788
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Gene Variant Type Tumor Drug Drug level Reference More
EGFR T790M MUT Lung Cancer AEE-788 RIII 1
Evidence region

CIVIC

Patient Criteria

-

Note

Lung cancers can accumulate activating mutations in oncogenes such as EGFR. The common L858R EGFR mutation has been shown previously to be sensitive to small molecular tyrosine kinase inhibitors (ie. erlotinib). In response, tumors may accumulate an additional 'gatekeeper' mutation in EGFR, T790M. Authors show that T790M retain low affinity for gefitinib and that introduction of T790M in the presence of L858R mutant increases the ATP affinity of L858R and activates wild-type EGFR, thus showing that increased ATP affinity is the primary mode of resistance in tumors with T790M, though irreversible ATP inhibitors (ie. HKI-272) are able to overcome this resistance via covalent bonding.

Gene name

EGFR

Full name

epidermal growth factor receptor

Gene type

protein-coding

Function

The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor, thus inducing receptor dimerization and tyrosine autophosphorylation leading to cell proliferation. Mutations in this gene are associated with lung cancer. EGFR is a component of the cytokine storm which contributes to a severe form of Coronavirus Disease 2019 (COVID-19) resulting from infection with severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). [provided by RefSeq, Jul 2020]

Drug name

AEE-788

DrugBank ID

DB12558

Synonyms

-

Brand

-

Description

AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

Target gene

-

EGFR L858R MUT All Tumor Types AEE-788 V 1
Evidence region

CIVIC

Patient Criteria

-

Note

EGFR L858R was expressed in Ba/F3 cells which do not contain endogenous EGFR, and conferred growth factor independance to the cells. Cells were plated and treated with 1st generation EGFR inhibitors Gefitinib, Erlotinib, or the the tool compound AEE788, and IC50 values were measured. L858R EGFR cells had very low IC50 nmol/L values for all three inhibitors in comparison to other constructs (Gefitinib=12, Erlotinib=6, AEE788=6), indicating sensitivity to all three constructs.

Gene name

EGFR

Full name

epidermal growth factor receptor

Gene type

protein-coding

Function

The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor, thus inducing receptor dimerization and tyrosine autophosphorylation leading to cell proliferation. Mutations in this gene are associated with lung cancer. EGFR is a component of the cytokine storm which contributes to a severe form of Coronavirus Disease 2019 (COVID-19) resulting from infection with severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). [provided by RefSeq, Jul 2020]

Drug name

AEE-788

DrugBank ID

DB12558

Synonyms

-

Brand

-

Description

AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

Target gene

-

EGFR T790M MUT All Tumor Types AEE-788 RIII 1
Evidence region

CIVIC

Patient Criteria

-

Note

Experimental - EGFR T790M mutation has been associated with resistance to first generation EGFR tyrosine kinase inhibitors, including erlotinib and gefitinib. In an in vitro study, Ba/F3 cells stably expressing EGFR T790M demonstrated resistance to gefitinib and erlotinib and the tool construct AEE788. These cells had very high IC50 nmol/L values for all three inhibitors in comparison to other constructs (Gefitinib>2000, Erlotinib>2000, AEE788>2000), indicating resitance to all three inhibitors.

Gene name

EGFR

Full name

epidermal growth factor receptor

Gene type

protein-coding

Function

The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor, thus inducing receptor dimerization and tyrosine autophosphorylation leading to cell proliferation. Mutations in this gene are associated with lung cancer. EGFR is a component of the cytokine storm which contributes to a severe form of Coronavirus Disease 2019 (COVID-19) resulting from infection with severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). [provided by RefSeq, Jul 2020]

Drug name

AEE-788

DrugBank ID

DB12558

Synonyms

-

Brand

-

Description

AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.

Target gene

-

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