4.6 Review

The Development of Positron Emission Tomography Tracers for In Vivo Targeting the Kinase Domain of the Epidermal Growth Factor Receptor

Related references

Note: Only part of the references are listed.
Article Chemistry, Medicinal

Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of Osimertinib

Kenji Mishiro et al.

Summary: Researchers attempted to develop nuclear imaging probes for detecting EGFR mutations. They designed and synthesized radioactive or nonradioactive osimertinib derivatives and evaluated their activity. The results showed that these derivatives accumulated significantly higher in tumors with mutations compared to normal tissues, but they also showed high accumulation in the lungs. Therefore, further structural modifications of the probes are needed.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Oncology

Preclinical Comparison of the Blood-brain barrier Permeability of Osimertinib with Other EGFR TKIs

Nicola Colclough et al.

Summary: The study investigates the potential of osimertinib in treating EGFR-mutant brain metastases, demonstrating its significant brain penetrance and impact on brain tumor growth rate.

CLINICAL CANCER RESEARCH (2021)

Article Endocrinology & Metabolism

Complete inhibition of ABCB1 and ABCG2 at the blood-brain barrier by co-infusion of erlotinib and tariquidar to improve brain delivery of the model ABCB1/ABCG2 substrate [11C]erlotinib

Nicolas Tournier et al.

Summary: This study investigated the feasibility of simultaneous inhibition of ABCB1 and ABCG2 at the blood-brain barrier by co-infusion of erlotinib and tariquidar. The combination led to increased brain distribution of the model substrate in mice and macaques, potentially enhancing brain delivery of molecularly targeted anticancer drugs for the treatment of brain tumors. Additionally, tolerability and induction of apoptosis were assessed in human cerebral organoids, showing promising results for future applications.

JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM (2021)

Article Chemistry, Medicinal

A Radiobrominated Tyrosine Kinase Inhibitor for EGFR with L858R/T790M Mutations in Lung Carcinoma

Muammar Fawwaz et al.

Summary: The study aimed to develop a PET imaging probe for detecting EGFR L858R/T790M mutations, and [Br-77]BrCO1686 showed high cytotoxicity and significant accumulation in tumor cells, indicating potential as a molecular probe for targeted imaging.

PHARMACEUTICALS (2021)

Review Biotechnology & Applied Microbiology

Trends in kinase drug discovery: targets, indications and inhibitor design

Misty M. Attwood et al.

Summary: The article analyzes the landscape of approved and investigational therapies that target kinases, highlighting the increasing importance of kinase inhibitors in oncology and beyond. It discusses trends in kinase inhibitor design and points out that there are still substantial unexplored opportunities for this drug class.

NATURE REVIEWS DRUG DISCOVERY (2021)

Article Radiology, Nuclear Medicine & Medical Imaging

Quantification of [18F]afatinib using PET/CT in NSCLC patients: a feasibility study

E. A. van de Stadt et al.

EJNMMI RESEARCH (2020)

Article Radiology, Nuclear Medicine & Medical Imaging

A Proof-of-Concept Study to Inhibit ABCG2-and ABCB1-Mediated Efflux Transport at the Human Blood-Brain Barrier

Martin Bauer et al.

JOURNAL OF NUCLEAR MEDICINE (2019)

Article Biochemistry & Molecular Biology

Synthesis and preliminary evaluation of 18F-icotinib for EGFR-targeted PET imaging of lung cancer

Xinmiao Lu et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

Review Oncology

Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer

Alessandro Leonetti et al.

BRITISH JOURNAL OF CANCER (2019)

Article Radiology, Nuclear Medicine & Medical Imaging

Development of a Fluorinated Analogue of Erlotinib for PET Imaging of EGFR Mutation-Positive NSCLC

Ofer Shamni et al.

MOLECULAR IMAGING AND BIOLOGY (2019)

Review Oncology

EGFR first- and second-generation TKIs-there is still place for them in EGFR-mutant NSCLC patients

Niki Karachaliou et al.

TRANSLATIONAL CANCER RESEARCH (2019)

Article Radiology, Nuclear Medicine & Medical Imaging

Molecular Imaging of ABCB1 and ABCG2 Inhibition at the Human Blood-Brain Barrier Using Elacridar and 11C-Erlotinib PET

Remy B. Verheijen et al.

JOURNAL OF NUCLEAR MEDICINE (2018)

Article Medicine, Research & Experimental

Effect of Rifampicin on the Distribution of [11C]Erlotinib to the Liver, a Translational PET Study in Humans and in Mice

Martin Bauer et al.

MOLECULAR PHARMACEUTICS (2018)

Article Multidisciplinary Sciences

Mechanisms of acquired resistance to afatinib clarified with liquid biopsy

Tomomi Nakamura et al.

PLOS ONE (2018)

Article Radiology, Nuclear Medicine & Medical Imaging

Strategies to Inhibit ABCB1-and ABCG2-Mediated Efflux Transport of Erlotinib at the Blood-Brain Barrier: A PET Study on Nonhuman Primates

Nicolas Tournier et al.

JOURNAL OF NUCLEAR MEDICINE (2017)

Article Radiology, Nuclear Medicine & Medical Imaging

A multi species evaluation of the radiation dosimetry of [11C]erlotinib, the radiolabeled analog of a clinically utilized tyrosine kinase inhibitor

J. Ryan Petrulli et al.

NUCLEAR MEDICINE AND BIOLOGY (2017)

Article Radiology, Nuclear Medicine & Medical Imaging

[11C]Erlotinib PET cannot detect acquired erlotinib resistance in NSCLC tumor xenografts in mice

Alexander Traxl et al.

NUCLEAR MEDICINE AND BIOLOGY (2017)

Article Chemistry, Medicinal

18F-Labeled Pyrido[3,4-d]pyrimidine as an Effective Probe for Imaging of L858R Mutant Epidermal Growth Factor Receptor

Hiroyuki Kimura et al.

ACS MEDICINAL CHEMISTRY LETTERS (2017)

Article Multidisciplinary Sciences

Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC

Yan Song et al.

SCIENTIFIC REPORTS (2017)

Article Chemistry, Analytical

Evaluation of 18F-labeled icotinib derivatives as potential PET agents for tumor imaging

Hongyu Ren et al.

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY (2016)

Article Radiology, Nuclear Medicine & Medical Imaging

Effects of erlotinib therapy on [11C]erlotinib uptake in EGFR mutated, advanced NSCLC

Idris Bahce et al.

EJNMMI RESEARCH (2016)

Article Radiology, Nuclear Medicine & Medical Imaging

Breast Cancer Resistance Protein and P-Glycoprotein Influence In Vivo Disposition of 11C-Erlotinib

Alexander Traxl et al.

JOURNAL OF NUCLEAR MEDICINE (2015)

Article Radiology, Nuclear Medicine & Medical Imaging

Identifying erlotinib-sensitive non-small cell lung carcinoma tumors in mice using [11C]erlotinib PET

Galith Abourbeh et al.

EJNMMI RESEARCH (2015)

Article Radiology, Nuclear Medicine & Medical Imaging

Development of [18F]afatinib as new TKI-PET tracer for EGFR positive tumors

Paul Slobbe et al.

NUCLEAR MEDICINE AND BIOLOGY (2014)

Article Radiology, Nuclear Medicine & Medical Imaging

A Pilot Study on EGFR-Targeted Molecular Imaging of PET/CT With 11C-PD153035 in Human Gliomas

Jikui Sun et al.

CLINICAL NUCLEAR MEDICINE (2013)

Review Biochemistry & Molecular Biology

The epidermal growth factor receptor variant III (EGFRvIII): where wild things are altered

Hui K. Gan et al.

FEBS JOURNAL (2013)

Article Radiology, Nuclear Medicine & Medical Imaging

Metabolism of Epidermal Growth Factor Receptor Targeting Probe [11C]PD153035: Impact on Biodistribution and Tumor Uptake in Rats

Erik Samen et al.

JOURNAL OF NUCLEAR MEDICINE (2013)

Article Oncology

Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Lung Cancers

Helena A. Yu et al.

JOURNAL OF THE NATIONAL COMPREHENSIVE CANCER NETWORK (2013)

Article Biotechnology & Applied Microbiology

Molecular Imaging of Nonsmall Cell Lung Carcinomas Expressing Active Mutant EGFR Kinase Using PET with [124I]-Morpholino-IPQA

Skye Hsin-Hsien Yeh et al.

BIOMED RESEARCH INTERNATIONAL (2013)

Article Pharmacology & Pharmacy

Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker

Flavio Solca et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2012)

Article Radiology, Nuclear Medicine & Medical Imaging

Molecular Imaging with 11C-PD153035 PET/CT Predicts Survival in Non-Small Cell Lung Cancer Treated with EGFR-TKI: A Pilot Study

Xue Meng et al.

JOURNAL OF NUCLEAR MEDICINE (2011)

Article Radiology, Nuclear Medicine & Medical Imaging

Radiosynthesis and Initial In Vitro Evaluation of [18F]F-PEG6-IPQA-A Novel PET Radiotracer for Imaging EGFR Expression-Activity in Lung Carcinomas

Ashutosh Pal et al.

MOLECULAR IMAGING AND BIOLOGY (2011)

Article Multidisciplinary Sciences

Molecular imaging of active mutant L858R EGF receptor (EGFR) kinase-expressing nonsmall cell lung carcinomas using PET/CT

Hsin Hsien Yeh et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2011)

Review Biochemistry & Molecular Biology

Epidermal growth factor receptor in relation to tumor development: EGFR gene and cancer

Tetsuya Mitsudomi et al.

FEBS JOURNAL (2010)

Article Radiology, Nuclear Medicine & Medical Imaging

[C-11]Gefitinib ([C-11]Iressa): Radiosynthesis, In Vitro Uptake, and In Vivo Imaging of Intact Murine Fibrosarcoma

Ming-Rong Zhang et al.

MOLECULAR IMAGING AND BIOLOGY (2010)

Article Radiology, Nuclear Medicine & Medical Imaging

Evaluation of Modified PEG-Anilinoquinazoline Derivatives as Potential Agents for EGFR Imaging in Cancer by Small Animal PET

Maria A. Pantaleo et al.

MOLECULAR IMAGING AND BIOLOGY (2010)

Article Biochemical Research Methods

Modified PEG-anilinoquinazoline derivatives as potential EGFR PET agents

Samar Dissoki et al.

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS (2009)

Article Radiology, Nuclear Medicine & Medical Imaging

PET-Based Biodistribution and Radiation Dosimetry of Epidermal Growth Factor Receptor-Selective Tracer 11C-PD153035 in Humans

Ningbo Liu et al.

JOURNAL OF NUCLEAR MEDICINE (2009)

Review Pharmacology & Pharmacy

Sex Differences in the Expression of Hepatic Drug Metabolizing Enzymes

David J. Waxman et al.

MOLECULAR PHARMACOLOGY (2009)

Article Radiology, Nuclear Medicine & Medical Imaging

In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [11C]gefitinib

Kazunori Kawamura et al.

NUCLEAR MEDICINE AND BIOLOGY (2009)

Article Radiology, Nuclear Medicine & Medical Imaging

Evaluation of [F-18]gefitinib as a molecular imaging probe for the assessment of the epidermal growth factor receptor status in malignant tumors

Helen Su et al.

EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2008)

Article Veterinary Sciences

Anesthesia and other considerations for in vivo imaging of small animals

Isabel J. Hildebrandt et al.

ILAR JOURNAL (2008)

Article Medicine, General & Internal

Further characterization of the epidermal growth factor receptor ligand 11C-PD153035

Wang Hui et al.

CHINESE MEDICAL JOURNAL (2007)

Article Cell Biology

TheEGF receptor family: spearheading a merger of signaling and therapeutics

Erez M. Bublil et al.

CURRENT OPINION IN CELL BIOLOGY (2007)

Article Radiology, Nuclear Medicine & Medical Imaging

The tyrosine kinase inhibitor PD153035:: implication of labeling position on radiometabolites formed in vitro

Erik Samen et al.

NUCLEAR MEDICINE AND BIOLOGY (2006)

Article Radiology, Nuclear Medicine & Medical Imaging

Molecular imaging of EGFR kinase activity in tumors with 124I-labeled small molecular tracer and positron emission tomography

A. Pal et al.

MOLECULAR IMAGING AND BIOLOGY (2006)

Article Oncology

FDA drug approval summary:: Erlotinib (Tarceva®) tablets

MH Cohen et al.

ONCOLOGIST (2005)

Article Medicine, General & Internal

EGFR mutation and resistance of non-small-cell lung cancer to gefitinib

S Kobayashi et al.

NEW ENGLAND JOURNAL OF MEDICINE (2005)

Article Multidisciplinary Sciences

EGF receptor gene mutations are common in lung cancers from never smokers and are associated with sensitivity of tumors to gefitinib and erlotinib

W Pao et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2004)

Review Oncology

EGF receptor ligands

RC Harris et al.

EXPERIMENTAL CELL RESEARCH (2003)

Article Oncology

EGFR and cancer prognosis

RI Nicholson et al.

EUROPEAN JOURNAL OF CANCER (2001)

Article Radiology, Nuclear Medicine & Medical Imaging

Potential 18F-labeled biomarkers for epidermal growth factor receptor tyrosine kinase

TA Bonasera et al.

NUCLEAR MEDICINE AND BIOLOGY (2001)

Article Oncology

The epidermal growth factor receptor as a target for cancer therapy

J Mendelsohn

ENDOCRINE-RELATED CANCER (2001)