erlotinib

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Associated Genetic Biomarkers

Associated Diseases

Overview

Generic Name(s):

erlotinib

Trade Name(s):

Tarceva

NCI Definition [1]:

A quinazoline derivative with antineoplastic properties. Competing with adenosine triphosphate, erlotinib reversibly binds to the intracellular catalytic domain of epidermal growth factor receptor (EGFR) tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation.

Biomarker-Directed Therapies

Erlotinib can be used in the treatment of non-small cell lung carcinoma. EGFR, EGFR A763_Y764insFQEA, and EGFR Exon 19 Deletion are the most frequent biomarker inclusion criteria for use of erlotinib [2].

Non-Small Cell Lung Carcinoma +

Disease is predicted to be sensitive to erlotinib: -

Biomarker Criteria:

Sample must match one or more of the following:

EGFR Exon 19 Deletion, EGFR L858R

Clinical Setting(s): Metastatic (FDA, NCCN, ASCO)

Note: Single agent or in combination with ramucirumab (FDA, NCCN), or in combination with bevacizumab (NCCN, non-squamous only).

Biomarker Criteria: Sample must match one or more of the following: EGFR Exon 19 Deletion, EGFR L858R	Clinical Setting(s): Metastatic (FDA, NCCN, ASCO)
	Note: Single agent or in combination with ramucirumab (FDA, NCCN), or in combination with bevacizumab (NCCN, non-squamous only).

Biomarker Criteria:

Sample must match one or more of the following:

EGFR G719A, EGFR G719C, EGFR G719S, EGFR L861Q, EGFR S768I

Sensitizing EGFR Mutations in Lung Cancer

Clinical Setting(s): Metastatic (NCCN)

Note: Single agent, or in combination with bevacizumab (non-squamous only) or ramucirumab.

Biomarker Criteria: Sample must match one or more of the following: EGFR G719A, EGFR G719C, EGFR G719S, EGFR L861Q, EGFR S768I Sensitizing EGFR Mutations in Lung Cancer	Clinical Setting(s): Metastatic (NCCN)
	Note: Single agent, or in combination with bevacizumab (non-squamous only) or ramucirumab.

Biomarker Criteria:

Sample must match all of the following:

Sensitizing EGFR Mutations in Lung Cancer

Clinical Setting(s): First Line of Therapy (NICE, SMC), Metastatic (NICE, BNF, SMC)

Biomarker Criteria:

Sample must match all of the following:

Sensitizing EGFR Mutations in Lung Cancer

Clinical Setting(s): First Line of Therapy (NICE, SMC), Metastatic (NICE, BNF, SMC)

Biomarker Criteria:

Sample must match one or more of the following:

Sensitizing EGFR Mutations (NCCN)

Clinical Setting(s): First Line of Therapy (NICE, SMC), Metastatic (NICE, SMC)

Biomarker Criteria:

Sample must match one or more of the following:

Sensitizing EGFR Mutations (NCCN)

Clinical Setting(s): First Line of Therapy (NICE, SMC), Metastatic (NICE, SMC)

Disease is predicted to be resistant to erlotinib: -

Biomarker Criteria:

Sample must match all of the following:

EGFR T790M

Sample must match one or more of the following:

EGFR Sensitizing Mutations

Clinical Setting(s): Metastatic (NCCN)

Note: EGFR T790M confers resistance to EGFR TKI therapy.

Biomarker Criteria: Sample must match all of the following: Sample must match all of the following: EGFR T790M Sample must match one or more of the following: EGFR Sensitizing Mutations	Clinical Setting(s): Metastatic (NCCN)
	Note: EGFR T790M confers resistance to EGFR TKI therapy.

Biomarker Criteria:

Sample must match all of the following:

EGFR T790M

Clinical Setting(s): Metastatic (NCCN)

Note: EGFR T790M confers resistance to EGFR TKI therapy.

Biomarker Criteria: Sample must match all of the following: EGFR T790M	Clinical Setting(s): Metastatic (NCCN)
	Note: EGFR T790M confers resistance to EGFR TKI therapy.

Biomarker Criteria:

Sample must match all of the following:

EGFR Exon 20 Insertion

Sample must not match any of the following:

EGFR A763_Y764insFQEA

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

EGFR Exon 20 Insertion

Sample must not match any of the following:

EGFR A763_Y764insFQEA

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

MET Amplification

Clinical Setting(s): Metastatic (NCCN)

Note: MET amplification renders the EGFR kinase resistant to EGFR TKIs, leading to primary or acquired resistance.

Biomarker Criteria: Sample must match all of the following: MET Amplification	Clinical Setting(s): Metastatic (NCCN)
	Note: MET amplification renders the EGFR kinase resistant to EGFR TKIs, leading to primary or acquired resistance.

Biomarker Criteria:

Sample must match all of the following:

ROS1 Fusion

Clinical Setting(s): Metastatic (NCCN)

Note: Not recommend by NCCN in subsequent lines of therapy, in patients with ROS1 rearrangements who relapsed on crizotinib

Biomarker Criteria: Sample must match all of the following: ROS1 Fusion	Clinical Setting(s): Metastatic (NCCN)
	Note: Not recommend by NCCN in subsequent lines of therapy, in patients with ROS1 rearrangements who relapsed on crizotinib

Biomarker Criteria:

Sample must match one or more of the following:

KRAS Resistance Mutations

Clinical Setting(s): Metastatic (NCCN)

Note: According to NCCN, mutations in KRAS have been associated with reduced responsiveness to EGFR TKI therapy.

Biomarker Criteria: Sample must match one or more of the following: KRAS Resistance Mutations	Clinical Setting(s): Metastatic (NCCN)
	Note: According to NCCN, mutations in KRAS have been associated with reduced responsiveness to EGFR TKI therapy.

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

EGFR Sensitizing Mutations

Sample must match one or more of the following:

KRAS Resistance Mutations

Clinical Setting(s): Metastatic (NCCN)

Note: According to NCCN, mutations in KRAS have been associated with reduced responsiveness to EGFR TKI therapy.

Biomarker Criteria: Sample must match all of the following: Sample must match one or more of the following: EGFR Sensitizing Mutations Sample must match one or more of the following: KRAS Resistance Mutations	Clinical Setting(s): Metastatic (NCCN)
	Note: According to NCCN, mutations in KRAS have been associated with reduced responsiveness to EGFR TKI therapy.

Biomarker Criteria:

Sample must match all of the following:

ALK Fusion

Clinical Setting(s): Relapse (NCCN)

Note: Not recommend by NCCN in subsequent lines of therapy, in patients with ALK rearrangements who relapsed on crizotinib.

Biomarker Criteria: Sample must match all of the following: ALK Fusion	Clinical Setting(s): Relapse (NCCN)
	Note: Not recommend by NCCN in subsequent lines of therapy, in patients with ALK rearrangements who relapsed on crizotinib.

Clinical Trials

View Clinical Trials for erlotinib

Erlotinib has been investigated in 42 clinical trials, of which 27 are open and 15 are closed. Of the trials investigating erlotinib, 10 are phase 1 (6 open), 5 are phase 1/phase 2 (2 open), 20 are phase 2 (13 open), 1 is phase 2/phase 3 (1 open), 4 are phase 3 (4 open), 1 is phase 4 (0 open), and 1 is no phase specified (1 open).

EGFR L858R, EGFR Exon 19 Deletion, and EGFR L861Q are the most frequent biomarker inclusion criteria for erlotinib clinical trials.

Non-small cell lung carcinoma, malignant solid tumor, and pancreatic adenocarcinoma are the most common diseases being investigated in erlotinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Erlotinib

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Erlotinib

This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating erlotinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:

osi-774, cp-258,774, Tarceva, n-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, erlotinib (substance), [6,7-bis-(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)-amine, erlotinib (product), erlotinib, erlotinib

Drug Categories [2]:

Tyrosine kinase inhibitors

Drug Target(s) [2]:

EGFR

NCIT ID [1]:

C65530

SNOMED ID [1]:

C-C781B

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.

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Associated Genetic Biomarkers

Associated Diseases

Overview

Biomarker-Directed Therapies

Clinical Trials

Drug Details

References

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