Drug/Small Molecule:
erlotinib

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.



last updated 10/25/2013

FDA Label for erlotinib and EGFR

This label is on the FDA Biomarker List
Genetic testing required

Summary

TARCEVA (erlotinib) is a kinase inhibitor indicated for First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

Annotation

Excerpts from the erlotinib drug label:

TARCEVA is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.

Select patients for the first-line treatment of metastatic NSCLC with TARCEVA based on the presence of EGFR exon 19 deletions or exon 21 (L858R) substitution mutations in tumor specimens. Information on FDA-approved tests for the detection of EGFR mutations in NSCLC is available at: http://www.fda.gov/CompanionDiagnostics.

Epidermal growth factor receptor (EGFR) is expressed on the cell surface of both normal and cancer cells. In some tumor cells signaling through this receptor plays a role in tumor cell survival and proliferation irrespective of EGFR mutation status. Erlotinib reversibly inhibits the kinase activity of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor and thereby inhibiting further downstream signaling. Erlotinib binding affinity for EGFR exon 19 deletion or exon 21 L858R mutations is higher than its affinity for the wild type receptor. Erlotinib inhibition of other tyrosine kinase receptors has not been fully characterized.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Erlotinib drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Carcinoma, Non-Small-Cell Lung
    • Warnings section, Adverse reactions section
    • source: PHONT
  • Lung Neoplasms
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Neoplasms
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • Pancreatic Neoplasms
    • Indications & usage section, Warnings section, Adverse reactions section
    • source: PHONT
  • CYP1A2
    • Clinical pharmacology section, metabolism/PK
    • source: FDA Label
  • CYP3A4
    • Drug interactions section, Clinical pharmacology section, metabolism/PK
    • source: FDA Label
  • EGFR
    • Indications & usage section, Dosage & administration section, Clinical pharmacology section, efficacy
    • source: FDA Label

last updated 10/25/2013

European Medicines Agency (EMA) Label for erlotinib and EGFR, UGT1A1

Genetic testing required

Summary

The EMA European Public Assessment Report (EPAR) requires testing tumours for EGFR mutations in patients with non-small cell lung cancer prior to treatment with erlotinib and recommends using a well-validated method of testing. The drug should be used with caution in patients with low expression of UGT1A1 or Gilbert's disease (caused by genetic variants in UGT1A1 gene), due to the inhibitory effects of erlotinib on glucuronidation by UGT1A1 (UGT1A1 genetic testing is not required).

Annotation

Excerpts from the Erlotinib (Tarceva) EPAR:

EGFR mutations may lead to constitutive activation of anti-apoptotic and proliferation signaling pathways. The potent effectiveness of erlotinib in blocking EGFR-mediated signalling in these EGFR mutation positive tumours is attributed to the tight binding of erlotinib to the ATP-binding site in the mutated kinase domain of the EGFR. Due to the blocking of downstream-signaling, the proliferation of cells is stopped, and cell death is induced through the intrinsic apoptotic pathway. Tumour regression is observed in mouse models of enforced expression of these EGFR activating mutations.


Patients with Non-Small Cell Lung Cancer: EGFR mutation testing should be performed prior to initiation of Tarceva therapy in chemo-na¿¿ve patients with advanced or metastatic NSCLC.


No survival benefit or other clinically relevant effects of the treatment have been demonstrated in patients with Epidermal Growth Factor Receptor (EGFR)- IHC negative tumours (see section 5.1).

This information is highlighted in the following sections: therapeutic indications, posology and method of administration, pharmacodynamic properties, package leaflet: information for the user.

The label also includes information regarding inhibition of metabolism enzymes by erlotinib, and metabolism of erlotinib by CYP3A4, CYP1A1 and CYP1B1, and as a substrate of ABCB1 (P-glycoprotein). The drug should be used with caution in patients with low expression of UGT1A1 or Gilbert's disease (caused by genetic variants in UGT1A1 gene), due to the inhibitory effects of erlotinib on glucuronidation by UGT1A1.

Excerpts from the Erlotinib (Tarceva) EPAR:

Erlotinib is a potent inhibitor of CYP1A1, and a moderate inhibitor of CYP3A4 and CYP2C8, as well as a strong inhibitor of glucuronidation by UGT1A1 in vitro.

Concomitant use of CYP3A4 substrates and modulators may require dose adjustment

The inhibition of glucuronidation may cause interactions with medicinal products which are substrates of UGT1A1 and exclusively cleared by this pathway. Patients with low expression levels of UGT1A1 or genetic glucuronidation disorders (e.g. Gilbert's disease) may exhibit increased serum concentrations of bilirubin and must be treated with caution.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Erlotinib EMA drug label.

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.

Genes and/or phenotypes found in this label

  • CYP3A4
    • Dosage & administration section, Drug interactions section, Pharmacokinetics section, metabolism/PK
    • source: European Medicines Agency (EMA) Label

Clinical Variants that meet the highest level of criteria, manually curated by PharmGKB, are shown below.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
EGFR PCR Kit EGFR EGFR: 19 deletions in exon 19 , EGFR L858R , EGFR L861Q , EGFR G719X (detects the presence of G719S , EGFR G719A or G719C but does not distinguish between them) , EGFR S768I , EGFR 3 insertions in exon 20 (detects the presence of any of 3 insertions, but does not distinguish between them)

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA ABCB1 *2 (PMID: 11503014) N/A N/A N/A
No VIP available No VIP available VA CYP3A4 *1B N/A N/A N/A
No VIP available No Clinical Annotations available VA
rs1065634 *1022A>G, -507A>G, 115259768T>C, 4748A>G, 85231686T>C
T > C
5' Flanking
No VIP available No Clinical Annotations available VA
rs11710163 -27+9024T>C, 12636288A>G, 12696288A>G, 14391T>C
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs12118636 23048077G>A, 53076159G>A
G > A
Not Available
No VIP available CA VA
rs121434568 177791T>G, 2573T>G, 55181822T>G, 55191822T>G, Leu858Arg
T > G
Not Available
Leu858Arg
No VIP available CA VA
rs121434569 1193G>A, 167347C>T, 2369C>T, 55171378C>T, 55181378C>T, Thr790Met
C > T
Not Available
Thr790Met
No VIP available No Clinical Annotations available VA
rs16886403 33347T>C, 483-13181T>C, 56139246T>C, 6733605T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs17309872 *771A>T, *843T>A, 32814T>A, 33515788A>T, 3711880A>T, 58044A>T
A > T
3' Flanking
No VIP available No Clinical Annotations available VA
rs17661089 56105996A>G, 6700355A>G, 97A>G
A > G
Not Available
No VIP available CA No Variant Annotations available
rs2227983 147531G>A, 147531G>C, 147531G>T, 1562G>A, 1562G>C, 1562G>T, 4818624G>A, 4818624G>C, 4818624G>T, 55229255G>A, 55229255G>C, 55229255G>T, Arg521Lys, Arg521Met, Arg521Thr, EGFR: 497G/A, EGFR:1562G>A, EGFR:R497K, R497K, R521K
G > A
G > T
G > C
Missense
Arg521Thr
Arg521Lys
Arg521Met
No VIP available No Clinical Annotations available VA
rs2237717 116405387T>C, 2583+2065T>C, 2637+2065T>C, 54438230T>C, 97929T>C
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs2622604 -19-17758A>G, -20+614A>G, 13626645T>C, 6088A>G, 89078924T>C, ABCG2 SNP in intron 1, rs2622604 C>T
T > C
Intronic
No VIP available No Clinical Annotations available VA
rs451774 *606A>G, *851A>G, 24754A>G, 28442550A>G, 28502550A>G
A > G
3' UTR
No VIP available CA VA
rs712829 -216G>T, 216G>T, 4676124G>T, 5031G>T, 55086755G>T, EGFR:-216G>T
G > T
5' UTR
No VIP available CA VA
rs726501 21967G>A, 482+15984G>A, 56127866G>A, 6722225G>A
G > A
Intronic
No VIP available No Clinical Annotations available VA
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • OSI-774
Trade Names
  • Tarceva
Brand Mixture Names

PharmGKB Accession Id:
PA134687924

Description

Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer.

Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.

Source: Drug Bank

Indication

For the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells.

Source: Drug Bank

Pharmacology

Erlotinib is a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor.

Source: Drug Bank

Food Interaction

Take with a glass of water.|Take at least 1 hour before or 2 hours after any food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1.

Source: Drug Bank

Protein Binding

93% protein bound to albumin and alpha-1 acid glycoprotein (AAG)

Source: Drug Bank

Absorption

Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%.

Source: Drug Bank

Half-Life

Median half-life of 36.2 hours.

Source: Drug Bank

Toxicity

Symptoms of overdose include diarrhea, rash, and liver transaminase elevation.

Source: Drug Bank

Chemical Properties

Chemical Formula

C22H23N3O4

Source: Drug Bank

Isomeric SMILES

COCCOc1cc2c(cc1OCCOC)ncnc2Nc3cccc(c3)C#C

Source: OpenEye

Canonical SMILES

COCCOC1=C(OCCOC)C=C2C(NC3=CC=CC(=C3)C#C)=NC=NC2=C1

Source: Drug Bank

Average Molecular Weight

393.4357

Source: Drug Bank

Monoisotopic Molecular Weight

393.168856239

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. EGFR Inhibitor Pathway, Pharmacodynamics
    Model non-tissue specific cancer cell displaying genes that may be involved in the treatment using epidermal growth factor receptor specific tyrosine kinase inhibitors or monoclonal antibodies.
  1. Erlotinib Pathway, Pharmacokinetics
    Model human liver cell showing genes involved in the transportation and metabolism of Erlotinib.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
EGFR (source: Drug Bank)

Drug Interactions

Drug Description
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
atazanavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
atazanavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
clarithromycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
clarithromycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erythromycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erythromycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
indinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
indinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
itraconazole This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
itraconazole This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
ketoconazole This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
ketoconazole This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
nefazodone This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
nefazodone This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
nelfinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
nelfinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
rifabutin Decreased levels/effect of erlotinib (source: Drug Bank)
rifabutin Decreased levels/effect of erlotinib (source: Drug Bank)
rifampin Decreased levels/effect of erlotinib (source: Drug Bank)
rifampin Decreased levels/effect of erlotinib (source: Drug Bank)
rifapentine Decreased levels/effect of erlotinib (source: Drug Bank)
ritonavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
ritonavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
saquinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
saquinavir This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
telithromycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
telithromycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
troleandomycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
troleandomycin This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
voriconazole This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
voriconazole This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This potent CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This potent CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib Decreased levels/effect of erlotinib (source: Drug Bank)
erlotinib Decreased levels/effect of erlotinib (source: Drug Bank)
erlotinib Decreased levels/effect of erlotinib (source: Drug Bank)
erlotinib Decreased levels/effect of erlotinib (source: Drug Bank)
erlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinib (source: Drug Bank)
erlotinib Telithromycin may reduce clearance of Erlotinib. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Erlotinib if Telithromycin is initiated, discontinued or dose changed. (source: Drug Bank)
erlotinib Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. (source: Drug Bank)
erlotinib Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of erlotinib by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of erlotinib if voriconazole is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

Publications related to erlotinib: 78

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Clinical Implementation of Germline Cancer Pharmacogenetic Variants during the Next-Generation Sequencing Era. Clinical pharmacology and therapeutics. 2013. Gillis Nancy K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The integrated landscape of driver genomic alterations in glioblastoma. Nature genetics. 2013. Frattini Veronique, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Emerging landscape of oncogenic signatures across human cancers. Nature genetics. 2013. Ciriello Giovanni, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for the epidermal growth factor receptor. Pharmacogenetics and genomics. 2013. Hodoglugil Ugur, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Impact of Systematic EGFR and KRAS Mutation Evaluation on Progression-Free Survival and Overall Survival in Patients with Advanced Non-Small-Cell Lung Cancer Treated by Erlotinib in a French Prospective Cohort (ERMETIC Project-Part 2). Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2012. Cadranel Jacques, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Efficacy of EGFR tyrosine kinase inhibitors for non-adenocarcinoma NSCLC patients with EGFR mutation. Cancer chemotherapy and pharmacology. 2012. Cho Su-Hee, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics and pharmacogenomics: role of mutational analysis in anti-cancer targeted therapy. The pharmacogenomics journal. 2012. Savonarola A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Association of ABCB1 polymorphisms with erlotinib pharmacokinetics and toxicity in Japanese patients with non-small-cell lung cancer. Pharmacogenomics. 2012. Hamada Akinobu, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Plasma epidermal growth factor receptor mutation analysis and possible clinical applications in pulmonary adenocarcinoma patients treated with erlotinib. Oncology letters. 2012. Chen Yuh-Min, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial. The lancet oncology. 2012. Rosell Rafael, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pretreatment epidermal growth factor receptor (EGFR) T790M mutation predicts shorter EGFR tyrosine kinase inhibitor response duration in patients with non-small-cell lung cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2012. Su Kang-Yi, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Pharmacogenetic predictors for EGFR-inhibitor-associated skin toxicity. The pharmacogenomics journal. 2011. Parmar S, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Prospective molecular marker analyses of EGFR and KRAS from a randomized, placebo-controlled study of erlotinib maintenance therapy in advanced non-small-cell lung cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2011. Brugger Wolfram, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
A noninvasive system for monitoring resistance to epidermal growth factor receptor tyrosine kinase inhibitors with plasma DNA. Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer. 2011. Nakamura Tomomi, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study. The lancet oncology. 2011. Zhou Caicun, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Genetic effects and modifiers of radiotherapy and chemotherapy on survival in pancreatic cancer. Pancreas. 2011. Zeng Hongmei, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genetic variations in multiple drug action pathways and survival in advanced stage non-small cell lung cancer treated with chemotherapy. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Li Yafei, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
A phase 2 trial of erlotinib in patients with previously treated squamous cell and adenocarcinoma of the esophagus. Cancer. 2011. Ilson David H, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Pretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutations. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Rosell Rafael, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Rebiopsy of lung cancer patients with acquired resistance to EGFR inhibitors and enhanced detection of the T790M mutation using a locked nucleic acid-based assay. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Arcila Maria E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors. Science translational medicine. 2011. Sequist Lecia V, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Practical recommendations for pharmacogenomics-based prescription: 2010 ESF-UB Conference on Pharmacogenetics and Pharmacogenomics. Pharmacogenomics. 2011. Becquemont Laurent, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetic tests in cancer chemotherapy: what physicians should know for clinical application. The Journal of pathology. 2011. Lee Soo-Youn, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Use of epidermal growth factor receptor mutation analysis in patients with advanced non-small-cell lung cancer to determine erlotinib use as first-line therapy. PLoS currents. 2011. Ishibe Naoko, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Systematic review of pharmacoeconomic studies of pharmacogenomic tests. Pharmacogenomics. 2010. Beaulieu Mathieu, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The UGT1A1*28 polymorphism correlates with erlotinib's effect on SN-38 glucuronidation. European journal of cancer (Oxford, England : 1990). 2010. Liu Yong, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Targeted cancer therapies in the twenty-first century: lessons from imatinib. Clinical pharmacology and therapeutics. 2010. Stegmeier F, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Acquired resistance to gefitinib: the contribution of mechanisms other than the T790M, MET, and HGF status. Lung cancer (Amsterdam, Netherlands). 2010. Onitsuka Takamitsu, et al. PubMed
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Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer cell. 2010. Turke Alexa B, et al. PubMed
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Comparison of the drug-drug interactions potential of erlotinib and gefitinib via inhibition of UDP-glucuronosyltransferases. Drug metabolism and disposition: the biological fate of chemicals. 2010. Liu Yong, et al. PubMed
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Clinicopathologic and molecular features of epidermal growth factor receptor T790M mutation and c-MET amplification in tyrosine kinase inhibitor-resistant Chinese non-small cell lung cancer. Pathology oncology research : POR. 2009. Chen Hua-Jun, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Grb7 upregulation is a molecular adaptation to HER2 signaling inhibition due to removal of Akt-mediated gene repression. PloS one. 2010. Nencioni Alessio, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The increasing role of pharmacogenetics in the treatment of gastrointestinal cancers. Gastrointestinal cancer research : GCR. 2009. Yalçin Suayib. PubMed
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Screening for epidermal growth factor receptor mutations in lung cancer. The New England journal of medicine. 2009. Rosell Rafael, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Clinically available pharmacogenomics tests. Clinical pharmacology and therapeutics. 2009. Flockhart D A, et al. PubMed
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Histone deacetylase inhibitors induce a very broad, pleiotropic anticancer drug resistance phenotype in acute myeloid leukemia cells by modulation of multiple ABC transporter genes. Clinical cancer research : an official journal of the American Association for Cancer Research. 2009. Hauswald Stefanie, et al. PubMed
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Prospective phase II study of gefitinib in non-small cell lung cancer with epidermal growth factor receptor gene mutations. Lung cancer (Amsterdam, Netherlands). 2009. Sugio Kenji, et al. PubMed
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Genetic determinants of response to clopidogrel and cardiovascular events. The New England journal of medicine. 2009. Simon Tabassome, et al. PubMed
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Redox regulation of multidrug resistance in cancer chemotherapy: molecular mechanisms and therapeutic opportunities. Antioxidants & redox signaling. 2009. Kuo Macus Tien. PubMed
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Several major antiepileptic drugs are substrates for human P-glycoprotein. Neuropharmacology. 2008. Luna-Tortós Carlos, et al. PubMed
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Effects of erlotinib in EGFR mutated non-small cell lung cancers with resistance to gefitinib. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008. Costa Daniel B, et al. PubMed
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Detection of mutations in EGFR in circulating lung-cancer cells. The New England journal of medicine. 2008. Maheswaran Shyamala, et al. PubMed
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Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
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Molecular characteristics of bronchioloalveolar carcinoma and adenocarcinoma, bronchioloalveolar carcinoma subtype, predict response to erlotinib. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2008. Miller Vincent A, et al. PubMed
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Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2008. Rudin Charles M, et al. PubMed
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Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression. Neuron. 2008. Uhr Manfred, et al. PubMed
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Citalopram enantiomers in plasma and cerebrospinal fluid of ABCB1 genotyped depressive patients and clinical response: a pilot study. Pharmacological research : the official journal of the Italian Pharmacological Society. 2008. Nikisch Georg, et al. PubMed
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Impact of EGFR gene polymorphisms on anticancer drug cytotoxicity in vitro. Molecular diagnosis & therapy. 2008. Puyo Stéphane, et al. PubMed
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MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proceedings of the National Academy of Sciences of the United States of America. 2007. Bean James, et al. PubMed
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Relationship of EGFR mutations, expression, amplification, and polymorphisms to epidermal growth factor receptor inhibitors in the NCI60 cell lines. Clinical cancer research : an official journal of the American Association for Cancer Research. 2007. Liu Wanqing, et al. PubMed
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MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science (New York, N.Y.). 2007. Engelman Jeffrey A, et al. PubMed
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Association of variant ABCG2 and the pharmacokinetics of epidermal growth factor receptor tyrosine kinase inhibitors in cancer patients. Cancer biology & therapy. 2007. Li Jing, et al. PubMed
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Response to treatment and survival of patients with non-small cell lung cancer undergoing somatic EGFR mutation testing. The oncologist. 2007. Sequist Lecia V, et al. PubMed
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Cobalamin potentiates vinblastine cytotoxicity through downregulation of mdr-1 gene expression in HepG2 cells. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 2007. Marguerite Véronique, et al. PubMed
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Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Molecular pharmaceutics. 2007. Collnot Eva-Maria, et al. PubMed
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Novel D761Y and common secondary T790M mutations in epidermal growth factor receptor-mutant lung adenocarcinomas with acquired resistance to kinase inhibitors. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Balak Marissa N, et al. PubMed
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Analysis of epidermal growth factor receptor gene mutation in patients with non-small cell lung cancer and acquired resistance to gefitinib. Clinical cancer research : an official journal of the American Association for Cancer Research. 2006. Kosaka Takayuki, et al. PubMed
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Presence of epidermal growth factor receptor gene T790M mutation as a minor clone in non-small cell lung cancer. Cancer research. 2006. Inukai Michio, et al. PubMed
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Cyclin D1 and epidermal growth factor polymorphisms associated with survival in patients with advanced colorectal cancer treated with Cetuximab. Pharmacogenetics and genomics. 2006. Zhang Wu, et al. PubMed
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Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer research. 2006. Leggas Markos, et al. PubMed
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Impact of P-glycoprotein on clopidogrel absorption. Clinical pharmacology and therapeutics. 2006. Taubert Dirk, et al. PubMed
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Metabolism and excretion of erlotinib, a small molecule inhibitor of epidermal growth factor receptor tyrosine kinase, in healthy male volunteers. Drug metabolism and disposition: the biological fate of chemicals. 2006. Ling Jie, et al. PubMed
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Single nucleotide polymorphisms in human P-glycoprotein: its impact on drug delivery and disposition. Expert opinion on drug delivery. 2006. Dey Surajit. PubMed
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Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR. Nature genetics. 2005. Bell Daphne W, et al. PubMed
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Mutations in the epidermal growth factor receptor and in KRAS are predictive and prognostic indicators in patients with non-small-cell lung cancer treated with chemotherapy alone and in combination with erlotinib. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2005. Eberhard David A, et al. PubMed
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EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proceedings of the National Academy of Sciences of the United States of America. 2004. Pao William, et al. PubMed
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Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical pharmacology. 2004. Ehrhardt Manuela, et al. PubMed
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Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharmaceutical research. 2004. Hochman Jerome H, et al. PubMed
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Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clinical pharmacology and therapeutics. 2004. Marzolini Catia, et al. PubMed
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Specific method for determination of OSI-774 and its metabolite OSI-420 in human plasma by using liquid chromatography-tandem mass spectrometry. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2003. Zhao Ming, et al. PubMed
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Genetic polymorphisms of the human MDR1 drug transporter. Annual review of pharmacology and toxicology. 2003. Schwab Matthias, et al. PubMed
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Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein. Naunyn-Schmiedeberg's archives of pharmacology. 2001. Pauli-Magnus C, et al. PubMed
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The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. The Journal of clinical investigation. 1999. Greiner B, et al. PubMed
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Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual review of pharmacology and toxicology. 1999. Ambudkar S V, et al. PubMed
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Competitive, non-competitive and cooperative interactions between substrates of P-glycoprotein as measured by its ATPase activity. Biochimica et biophysica acta. 1997. Litman T, et al. PubMed
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P-glycoprotein structure and evolutionary homologies. Cytotechnology. 1993. Croop J M. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00530
PDB:
AQ4
ChEBI:
114785
PubChem Compound:
176870
PubChem Substance:
46508021
7885946
Drugs Product Database (DPD):
2269023
BindingDB:
5446
ChemSpider:
154044
HET:
AQ4
Therapeutic Targets Database:
DAP001010

Clinical Trials

These are trials that mention erlotinib and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.