Safety and Tolerability of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Oncology

Mechanisms of acquired resistance to first- and second-generation EGFR tyrosine kinase inhibitors

(2018) D Westover et al.   ANNALS OF ONCOLOGY

Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045

(2018) Peng Zhao et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Investigating Novel Resistance Mechanisms to Third-Generation EGFR Tyrosine Kinase Inhibitor Osimertinib in Non–Small Cell Lung Cancer Patients

(2018) Zhe Yang et al.   CLINICAL CANCER RESEARCH

Dermatologic Toxicity Occurring During Anti-EGFR Monoclonal Inhibitor Therapy in Patients With Metastatic Colorectal Cancer: A Systematic Review

(2018) Mario E. Lacouture et al.   Clinical Colorectal Cancer

Resistance to EGFR inhibitors in non-small cell lung cancer: Clinical management and future perspectives

(2018) Chiara Tomasello et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Targeting non-small cell lung cancer with small-molecule EGFR tyrosine kinase inhibitors

(2018) Mahaveer Singh et al.   DRUG DISCOVERY TODAY

Systematic bioinformatic approaches reveal novel gene expression signatures associated with acquired resistance to EGFR targeted therapy in lung cancer

(2018) Marjan Mojtabavi Naeini et al.   GENE

Successful Osimertinib Rechallenge with Steroid Therapy after Osimertinib-induced Interstitial Lung Disease

(2018) Tatsunori Kiriu et al.   INTERNAL MEDICINE

Successful oral desensitization with osimertinib following osimertinib-induced fever and hepatotoxicity: a case report

(2018) Ryosuke Hirabayashi et al.   INVESTIGATIONAL NEW DRUGS

First-in-Human Phase I Study of AC0010, a Mutant-Selective EGFR Inhibitor in Non–Small Cell Lung Cancer: Safety, Efficacy, and Potential Mechanism of Resistance

(2018) Yuxiang Ma et al.   Journal of Thoracic Oncology

Acquired EGFR L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib

(2018) Yutao Liu et al.   LUNG CANCER

Management of acquired resistance to EGFR TKI–targeted therapy in advanced non-small cell lung cancer

(2018) Shang-Gin Wu et al.   Molecular Cancer

Third generation EGFR TKIs: current data and future directions

(2018) Chee-Seng Tan et al.   Molecular Cancer

Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer

(2018) Jean-Charles Soria et al.   NEW ENGLAND JOURNAL OF MEDICINE

EGFR-TKIs in non-small-cell lung cancer: focus on clinical pharmacology and mechanisms of resistance

(2018) Stefano Fogli et al.   PHARMACOGENOMICS

A case report of toxic epidermal necrolysis associated with AZD-9291

(2018) Jie Wang et al.   Drug Design Development and Therapy

Distribution of erlotinib in rash and normal skin in cancer patients receiving erlotinib visualized by matrix assisted laser desorption/ionization mass spectrometry imaging

(2018) Meiko Nishimura et al.   Oncotarget

Correlation of plasma erlotinib trough concentration with skin rash in Chinese NSCLC patients harboring exon 19 deletion mutation

(2018) Dehua Liao et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

NSAIDs may prevent EGFR-TKI-related skin rash in non-small cell lung cancer patients


(2018) Yohei Iimura et al.   INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS

Preliminary Phase II results of a multicenter, open-label study of nazartinib (EGF816) in adult patients with treatment-naïve EGFR-mutant non-small cell lung cancer (NSCLC).

(2018) Dong-Wan Kim et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

(2018) Xiaoyun Lu et al.   MEDICINAL RESEARCH REVIEWS

Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance

(2017) Harun Patel et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Dacomitinib-induced diarrhea: Targeting chloride secretion with crofelemer

(2017) Ysabella Z.A. Van Sebille et al.   INTERNATIONAL JOURNAL OF CANCER

Incidence, risk and prognostic role of anti-epidermal growth factor receptor-induced skin rash in biliary cancer: a meta-analysis

(2017) Fangqiang Wei et al.   International Journal of Clinical Oncology

Efficacy and safety of osimertinib in a Japanese compassionate use program

(2017) Yutaka Fujiwara et al.   JAPANESE JOURNAL OF CLINICAL ONCOLOGY

Phase I Study and Biomarker Analysis of Pyrotinib, a Novel Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor, in Patients With Human Epidermal Growth Factor Receptor 2–Positive Metastatic Breast Cancer

(2017) Fei Ma et al.   JOURNAL OF CLINICAL ONCOLOGY

Rapid onset of conjunctivitis associated with overdosing of erlotinib

(2017) P. Sun et al.   JOURNAL OF CLINICAL PHARMACY AND THERAPEUTICS

MA16.06 Phase I/II Study of AC0010, Mutant-Selective EGFR Inhibitor, in Non-Small Cell Lung Cancer (NSCLC) Patients with EGFR T790M Mutation

(2017) Yi Long Wu et al.   Journal of Thoracic Oncology

Successful Osimertinib Rechallenge after Severe Osimertinib-Induced Hepatotoxicity

(2017) Hironori Yoshida et al.   Journal of Thoracic Oncology

Successful Osimertinib Rechallenge in a Patient with T790M-Mutant Non–Small Cell Lung Cancer after Osimertinib-Induced Interstitial Lung Disease

(2017) Eisaku Miyauchi et al.   Journal of Thoracic Oncology

Placebo-controlled phase II study of vitamin K3 cream for the treatment of cetuximab-induced rash

(2017) Jesper Grau Eriksen et al.   SUPPORTIVE CARE IN CANCER

Predictive blood plasma biomarkers for EGFR inhibitor-induced skin rash

(2017) Vivien Hichert et al.   Oncotarget

A Phase II Study of Poziotinib in Patients with Epidermal Growth Factor Receptor (EGFR)-Mutant Lung Adenocarcinoma Who Have Acquired Resistance to EGFR–Tyrosine Kinase Inhibitors

(2017) Ji-Youn Han et al.   Cancer Research and Treatment

Third-Generation Tyrosine Kinase Inhibitors Targeting Epidermal Growth Factor Receptor Mutations in Non-Small Cell Lung Cancer

(2017) Tristan A. Barnes et al.   Frontiers in Oncology

Observation of hepatotoxicity during long-term gefitinib administration in patients with non-small-cell lung cancer

(2016) Jingjing Wang et al.   ANTI-CANCER DRUGS

Development of a skin rash within the first week and the therapeutic effect in afatinib monotherapy for EGFR-mutant non-small cell lung cancer (NSCLC): Okayama Lung Cancer Study Group experience

(2016) Kenichiro Kudo et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Clinical Pharmacokinetics and Pharmacodynamics of Afatinib

(2016) Sven Wind et al.   CLINICAL PHARMACOKINETICS

Impact of dermatologic adverse events induced by targeted therapies on quality of life

(2016) Cécile Charles et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Hyperglycaemia Induced by Novel Anticancer Agents: An Undesirable Complication or a Potential Therapeutic Opportunity?

(2016) Rashmi R. Shah   DRUG SAFETY

Tyrosine Kinase Inhibitor-Induced Interstitial Lung Disease: Clinical Features, Diagnostic Challenges, and Therapeutic Dilemmas

(2016) Rashmi R. Shah   DRUG SAFETY

Dosing to rash? – The role of erlotinib metabolic ratio from patient serum in the search of predictive biomarkers for EGFR inhibitor-mediated skin rash

(2016) Michael Steffens et al.   EUROPEAN JOURNAL OF CANCER

Influence of Renal Impairment on the Pharmacokinetics of Afatinib: An Open-Label, Single-Dose Study

(2016) Sabrina Wiebe et al.   EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS

Pharmacokinetic drug-drug interactions of tyrosine kinase inhibitors: A focus on cytochrome P450, transporters, and acid suppression therapy

(2016) Caroline Gay et al.   HEMATOLOGICAL ONCOLOGY

Practical recommendation for rash and diarrhea management in Indian patients treated with tyrosine kinase inhibitors for the treatment of non-small cell lung cancer

(2016) K Prabhash et al.   INDIAN JOURNAL OF CANCER

Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity

(2016) Hiroto Ueda et al.   INVESTIGATIONAL NEW DRUGS

Skin problems and EGFR-tyrosine kinase inhibitor

(2016) Toshiyuki Kozuki   JAPANESE JOURNAL OF CLINICAL ONCOLOGY

Current mechanism of acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitors and updated therapy strategies in human nonsmall cell lung cancer

(2016) Kaixian Zhang et al.   Journal of Cancer Research and Therapeutics

Rapidly progressive cataract formation associated with non-small-cell lung cancer therapy

(2016) Erica Liu et al.   JOURNAL OF CATARACT AND REFRACTIVE SURGERY

Pan Canadian Rash Trial: A Randomized Phase III Trial Evaluating the Impact of a Prophylactic Skin Treatment Regimen on Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitor–Induced Skin Toxicities in Patients With Metastatic Lung Cancer

(2016) Barbara Melosky et al.   JOURNAL OF CLINICAL ONCOLOGY

Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer

(2016) Shuhang Wang et al.   Journal of Hematology & Oncology

Acquired C797S Mutation upon Treatment with a T790M-Specific Third-Generation EGFR Inhibitor (HM61713) in Non–Small Cell Lung Cancer

(2016) Haa-Na Song et al.   Journal of Thoracic Oncology

Successful treatment with afatinib after grade 3 hepatotoxicity induced by both gefitinib and erlotinib in EGFR mutation-positive non-small cell lung cancer

(2016) Yoshitaka Zenke et al.   LUNG CANCER

Hyperglycemia Associated With Targeted Oncologic Treatment: Mechanisms and Management

(2016) Jonathan W. Goldman et al.   ONCOLOGIST

New developments in the management of non-small-cell lung cancer, focus on rociletinib: what went wrong?

(2016) Nele Van Der Steen et al.   OncoTargets and Therapy

Three generations of epidermal growth factor receptor tyrosine kinase inhibitors developed to revolutionize the therapy of lung cancer

(2016) Haijun Zhang   Drug Design Development and Therapy

EGFR kinase inhibitors and gastric acid suppressants in EGFR-mutant NSCLC: a retrospective database analysis of potential drug interaction

(2016) Nesaretnam Barr Kumarakulasinghe et al.   Oncotarget

Practical recommendation for rash and diarrhea management in Indian patients treated with tyrosine kinase inhibitors for the treatment of non-small cell lung cancer

(2016) K Prabhash et al.   INDIAN JOURNAL OF CANCER

Mechanisms of resistance to third-generation EGFR tyrosine kinase inhibitors

(2016) Shuhang Wang et al.   Frontiers of Medicine

Characteristics of and Risk Factors for Interstitial Lung Disease Induced by Chemotherapy for Lung Cancer

(2015) Takumi Sakurada et al.   ANNALS OF PHARMACOTHERAPY

Evaluation of drug-drug interactions for oncology therapies:in vitro-in vivoextrapolation model-based risk assessment

(2015) Nigel J. Waters   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

ErbB small molecule tyrosine kinase inhibitor (TKI) induced diarrhoea: Chloride secretion as a mechanistic hypothesis

(2015) Ysabella Z.A. Van Sebille et al.   CANCER TREATMENT REVIEWS

Use of the epidermal growth factor receptor inhibitors gefitinib, erlotinib, afatinib, dacomitinib, and icotinib in the treatment of non-small-cell lung cancer: a systematic review

(2015) P.M. Ellis et al.   Current Oncology

Update on Cardiovascular Safety of Tyrosine Kinase Inhibitors: With a Special Focus on QT Interval, Left Ventricular Dysfunction and Overall Risk/Benefit

(2015) Rashmi R. Shah et al.   DRUG SAFETY

Expert Consensus on the Management of Adverse Events from EGFR Tyrosine Kinase Inhibitors in the UK

(2015) R. Califano et al.   DRUGS

Canertinib induces ototoxicity in three preclinical models

(2015) Jian Tang et al.   HEARING RESEARCH

Clinical pharmacokinetics, safety, and preliminary efficacy evaluation of icotinib in patients with advanced non-small cell lung cancer

(2015) Dongyang Liu et al.   LUNG CANCER

Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer

(2015) Lecia V. Sequist et al.   NEW ENGLAND JOURNAL OF MEDICINE

Phase II trial of epidermal growth factor ointment for patients with Erlotinib-related skin effects

(2015) In Gyu Hwang et al.   SUPPORTIVE CARE IN CANCER

Tyrosine kinase inhibitors for epidermal growth factor receptor gene mutation–positive non-small cell lung cancers: an update for recent advances in therapeutics

(2015) Clement Chung   JOURNAL OF ONCOLOGY PHARMACY PRACTICE

Acquired Resistance ofEGFR-Mutant Lung Cancer to a T790M-Specific EGFR Inhibitor

(2015) Helena A. Yu et al.   JAMA Oncology

ERBB Receptors: From Oncogene Discovery to Basic Science to Mechanism-Based Cancer Therapeutics

(2014) Carlos L. Arteaga et al.   CANCER CELL

Oral epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small cell lung cancer: Comparative pharmacokinetics and drug–drug interactions

(2014) Solange Peters et al.   CANCER TREATMENT REVIEWS

Pharmacokinetic Drug Interactions of Afatinib with Rifampicin and Ritonavir

(2014) Sven Wind et al.   CLINICAL DRUG INVESTIGATION

pH-Dependent Drug–Drug Interactions for Weak Base Drugs: Potential Implications for New Drug Development

(2014) L Zhang et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Effect of Tyrosine Kinase Inhibitors on Wound Healing and Tissue Repair: Implications for Surgery in Cancer Patients

(2014) Devron R. Shah et al.   DRUG SAFETY

Drug interactions between tyrosine-kinase inhibitors and acid suppressive agents: more than meets the eye

(2014) Guo Yu et al.   LANCET ONCOLOGY

A single-arm, multicenter, safety-monitoring, phase IV study of icotinib in treating advanced non-small cell lung cancer (NSCLC)

(2014) Xingsheng Hu et al.   LUNG CANCER

Icotinib Is an Active Treatment of Non-Small-Cell Lung Cancer: A Retrospective Study

(2014) Xiaofeng Chen et al.   PLoS One

Emerging toxicities in the treatment of non-small cell lung cancer: Ocular disorders

(2013) Francesco Agustoni et al.   CANCER TREATMENT REVIEWS

Playing Russian Roulette With Tyrosine Kinase Inhibitors

(2013) R Z Szmulewitz et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Hepatotoxicity of Tyrosine Kinase Inhibitors: Clinical and Regulatory Perspectives

(2013) Rashmi R. Shah et al.   DRUG SAFETY

Tyrosine Kinase Inhibitors: Their On-Target Toxicities as Potential Indicators of Efficacy

(2013) Devron R. Shah et al.   DRUG SAFETY

Cardiovascular Safety of Tyrosine Kinase Inhibitors: With a Special Focus on Cardiac Repolarisation (QT Interval)

(2013) Rashmi R. Shah et al.   DRUG SAFETY

Dosing to rash: A phase II trial of the first-line erlotinib for patients with advanced non-small-cell lung cancer an Eastern Cooperative Oncology Group Study (E3503)

(2013) J.R. Brahmer et al.   EUROPEAN JOURNAL OF CANCER

Impact of EGFR Inhibitor in Non–Small Cell Lung Cancer on Progression-Free and Overall Survival: A Meta-Analysis

(2013) Chee Khoon Lee et al.   JNCI-Journal of the National Cancer Institute

Correlation between erlotinib pharmacokinetics, cutaneous toxicity and clinical outcomes in patients with advanced non-small cell lung cancer (NSCLC)

(2013) Marcello Tiseo et al.   LUNG CANCER

The ErbB/HER family of protein-tyrosine kinases and cancer

(2013) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Skin Rash could Predict the Response to EGFR Tyrosine Kinase Inhibitor and the Prognosis for Patients with Non-Small Cell Lung Cancer: A Systematic Review and Meta-Analysis

(2013) Hong-bing Liu et al.   PLoS One

A review of the treatment options for skin rash induced by EGFR-targeted therapies: Evidence from randomized clinical trials and a metaanalysis

(2013) Janja Ocvirk et al.   Radiology and Oncology

Reduced CYP2D6 function is associated with gefitinib-induced rash in patients with non-small cell lung cancer

(2012) Tomohiro Suzumura et al.   BMC CANCER

Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers

(2012) Can-Jun Ruan et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Relationship between skin rash and outcome in non-small-cell lung cancer patients treated with anti-EGFR tyrosine kinase inhibitors: A literature-based meta-analysis of 24 trials

(2012) Fausto Petrelli et al.   LUNG CANCER

Ocular Adverse Events of Systemic Inhibitors of the Epidermal Growth Factor Receptor: Report of 5 Cases

(2012) Alejandro Saint-Jean et al.   OPHTHALMOLOGY

The Association of Rash Severity With Overall Survival

(2012) Edward J. Stepanski et al.   PANCREAS

Phase II open-label study of erlotinib in combination with gemcitabine in unresectable and/or metastatic adenocarcinoma of the pancreas: relationship between skin rash and survival (Pantar study)

(2011) E. Aranda et al.   ANNALS OF ONCOLOGY

Erlotinib ‘dosing-to-rash’: a phase II intrapatient dose escalation and pharmacologic study of erlotinib in previously treated advanced non-small cell lung cancer

(2011) A C Mita et al.   BRITISH JOURNAL OF CANCER

Toxicity as a Biomarker of Efficacy of Molecular Targeted Therapies: Focus on EGFR and VEGF Inhibiting Anticancer Drugs

(2011) R. Dienstmann et al.   ONCOLOGIST

Inconsistent Labeling of Food Effect for Oral Agents across Therapeutic Areas: Differences between Oncology and Non-Oncology Products

(2010) S. P. Kang et al.   CLINICAL CANCER RESEARCH

A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer

(2009) Olivier Rixe et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Epidermal Growth Factor Receptor Expression in Human Fetal Cochlea With Turner Syndrome

(2009) Ilona Schwentner et al.   OTOLOGY & NEUROTOLOGY