The next generation of EGFR inhibitors: a patenting perspective of PROTACs based EGFR degraders

Discovery of novel exceptionally potent and orally active c-MET PROTACs for the treatment of tumors with MET alterations

(2023) Pengyun Li et al.   Acta Pharmaceutica Sinica B

Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities

(2023) Pritam Maity et al.   Journal of Medicinal Chemistry

Epidermal growth factor receptor PROTACs as an effective strategy for cancer therapy: A review

(2023) Chao Wang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Targeted Therapies for Lung Cancer Patients With Oncogenic Driver Molecular Alterations

(2022) Aaron C. Tan et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase 1/2 study of ARV-110, an androgen receptor (AR) PROTAC degrader, in metastatic castration-resistant prostate cancer (mCRPC).

(2022) Xin Gao et al.   JOURNAL OF CLINICAL ONCOLOGY

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

AENEAS: A Randomized Phase III Trial of Aumolertinib Versus Gefitinib as First-Line Therapy for Locally Advanced or MetastaticNon–Small-Cell Lung Cancer With EGFR Exon 19 Deletion or L858R Mutations

(2022) Shun Lu et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands

(2022) Hong-Yi Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

EGFR signaling pathway as therapeutic target in human cancers

(2022) Elena Levantini et al.   SEMINARS IN CANCER BIOLOGY

Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo

(2022) Wenjuan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Overcoming C797S mutation: The challenges and prospects of the fourth-generation EGFR-TKIs

(2022) Hong-Yi Zhao et al.   BIOORGANIC CHEMISTRY

Targeting androgen receptor degradation with PROTACs from bench to bedside

(2022) Xiaojuan Jia et al.   BIOMEDICINE & PHARMACOTHERAPY

Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma

(2021) Surya Kant Tripathi et al.   DRUG DISCOVERY TODAY

Effective degradation of EGFRL858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems

(2021) Xiaojuan Qu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research

(2021) Rui-Fang Dong et al.   PHARMACOLOGICAL RESEARCH

The rise and rise of protein degradation: Opportunities and challenges ahead

(2021) Scott J. Hughes et al.   DRUG DISCOVERY TODAY

Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP

(2021) Mengzhu Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Toward personalized treatment approaches for non-small-cell lung cancer

(2021) Meina Wang et al.   NATURE MEDICINE

Challenge and countermeasures for EGFR targeted therapy in non-small cell lung cancer

(2021) Xueli Tian et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Overview of PROTACs targeting the estrogen receptor: Achievements for biological and drug discovery

(2021) Hui Qin et al.   CURRENT MEDICINAL CHEMISTRY

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

(2020) George M. Burslem et al.   CELL

First-in-human phase I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide (ENZ) and/or abiraterone (ABI).

(2020) Daniel Peter Petrylak et al.   JOURNAL OF CLINICAL ONCOLOGY

Mutant‐Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug‐Resistant Mutations

(2020) Jaebong Jang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery and biological evaluation of proteolysis targeting chimeras (PROTACs) as an EGFR degraders based on osimertinib and lenalidomide

(2020) Kailun He et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

(2020) Andy Pike et al.   DRUG DISCOVERY TODAY

Lysosome-targeting chimaeras for degradation of extracellular proteins

(2020) Steven M. Banik et al.   NATURE

Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs

(2020) Michael J. Bond et al.   ACS Central Science

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

(2020) Katherine A. Donovan et al.   CELL

Proteolysis targeting chimera ( PROTAC ) for epidermal growth factor receptor enhances anti‐tumor immunity in non‐small cell lung cancer

(2020) Kai Wang et al.   DRUG DEVELOPMENT RESEARCH

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

(2020) Shenxin Zeng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Beyond osimertinib: The development of 3rd-generation EGFR Tyrosine Kinase Inhibitors

(2020) Misako Nagasaka et al.   Journal of Thoracic Oncology

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

(2019) Blake E. Smith et al.   Nature Communications

Comparing and contrasting predictive biomarkers for immunotherapy and targeted therapy of NSCLC

(2019) D. Ross Camidge et al.   Nature Reviews Clinical Oncology

Dacomitinib in the Management of Advanced Non-Small-Cell Lung Cancer

(2019) Sally C. M. Lau et al.   DRUGS

Single and dual targeting of mutant EGFR with an allosteric inhibitor

(2019) Ciric To et al.   Cancer Discovery

Non–Small Cell Lung Cancer: Epidemiology, Screening, Diagnosis, and Treatment

(2019) Narjust Duma et al.   MAYO CLINIC PROCEEDINGS

Role of the dynamic tumor microenvironment in controversies regarding immune checkpoint inhibitors for the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations

(2019) Anqi Lin et al.   Molecular Cancer

Degradation of proteins by PROTACs and other strategies

(2019) Yang Wang et al.   Acta Pharmaceutica Sinica B

Combination of EGFR-TKIs and chemotherapy in advanced EGFR mutated NSCLC: Review of the literature and future perspectives

(2019) Sara Elena Rebuzzi et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors

(2019) Harald Engelhardt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein

(2019) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Osimertinib and other third-generation EGFR TKI in EGFR-mutant NSCLC patients

(2018) J Remon et al.   ANNALS OF ONCOLOGY

Overview of current systemic management of EGFR-mutant NSCLC

(2018) W -H Hsu et al.   ANNALS OF ONCOLOGY

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

Combination Strategies Using EGFR-TKi in NSCLC Therapy: Learning from the Gap between Pre-Clinical Results and Clinical Outcomes

(2018) Zheng Yang et al.   International Journal of Biological Sciences

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

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

Dacomitinib: First Global Approval

(2018) Matt Shirley   DRUGS

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

(2018) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Discovery of JND3229 as a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy

(2018) Xiaoyun Lu et al.   ACS Medicinal Chemistry Letters

Osimertinib or Platinum–Pemetrexed in EGFR T790M–Positive Lung Cancer

(2017) Tony S. Mok et al.   NEW ENGLAND JOURNAL OF MEDICINE

Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer

(2017) Ken Uchibori et al.   Nature Communications

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

(2016) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

(2016) Yong Jia et al.   NATURE

Afatinib: First Global Approval

(2013) Rosselle T. Dungo et al.   DRUGS

Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma WithEGFRMutations

(2013) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies

(2011) Fenlai Tan et al.   LUNG CANCER

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA