The synthesis review of the approved tyrosine kinase inhibitors for anticancer therapy in 2015–2020

Zanubrutinib: First Approval

(2020) Yahiya Y. Syed   DRUGS

Avapritinib: First Approval

(2020) Sohita Dhillon   DRUGS

Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance

(2020) Ning Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Anaplastic lymphoma kinase inhibitors: an updated patent review (2014-2018)

(2020) Yi-Min Liu et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Advances in Targeting RET-Dependent Cancers

(2020) Vivek Subbiah et al.   Cancer Discovery

Pemigatinib: First Approval

(2020) Sheridan M. Hoy   DRUGS

Entrectinib for the treatment of metastatic NSCLC: safety and efficacy

(2020) Andrea Sartore-Bianchi et al.   Expert Review of Anticancer Therapy

The European Medicines Agency Review of Gilteritinib (Xospata) for the Treatment of Adult Patients with Relapsed or Refractory Acute Myeloid Leukemia with an FLT3 Mutation

(2020) Kyriaki Tzogani et al.   ONCOLOGIST

Brigatinib and Alectinib for ALK Rearrangement-Positive Advanced Non-Small Cell Lung Cancer with or without Central Nervous System Metastasis: A Systematic Review and Network Meta-Analysis

(2020) Koichi Ando et al.   Cancers

Selpercatinib: First Approval

(2020) Anthony Markham   DRUGS

Fedratinib, a newly approved treatment for patients with myeloproliferative neoplasm-associated myelofibrosis

(2020) Moshe Talpaz et al.   LEUKEMIA

Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations

(2020) V. Subbiah et al.   ANNALS OF ONCOLOGY

Brigatinib: Novel ALK Inhibitor for Non–Small-Cell Lung Cancer

(2019) Sara A. Spencer et al.   ANNALS OF PHARMACOTHERAPY

Fibroblast Growth Factor Receptor 4 Targeting in Cancer: New Insights into Mechanisms and Therapeutic Strategies

(2019) Liwei Lang et al.   Cells

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

(2019) Shuang Qin et al.   Journal of Hematology & Oncology

Gilteritinib: First Global Approval

(2019) Sohita Dhillon   DRUGS

Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants

(2019) Bryan D. Smith et al.   CANCER CELL

Exploratory Process Development of Pexidartinib through the Tandem Tsuji–Trost Reaction and Heck Coupling

(2019) Dongsheng Chen et al.   SYNTHESIS-STUTTGART

Quizartinib (AC220): a promising option for acute myeloid leukemia

(2019) Fang Zhou et al.   Drug Design Development and Therapy

Phase 1 study of selective BTK inhibitor zanubrutinib in B-cell malignancies and safety and efficacy evaluation in CLL

(2019) Constantine Si Lun Tam et al.   BLOOD

Entrectinib: First Global Approval

(2019) Zaina T. Al-Salama et al.   DRUGS

Pexidartinib versus placebo for advanced tenosynovial giant cell tumour (ENLIVEN): a randomised phase 3 trial

(2019) William D Tap et al.   LANCET

Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors

(2019) Shuyan Dai et al.   Cells

Fibroblast Growth Factor Receptor Functions in Glioblastoma

(2019) Ana Jimenez-Pascual et al.   Cells

Pexidartinib: First Approval

(2019) Yvette N. Lamb   DRUGS

Midostaurin In Acute Myeloid Leukemia: An Evidence-Based Review And Patient Selection

(2019) Hussein A. Abbas et al.   Cancer Management and Research

The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review

(2018) Chengyuan Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Advances in studies of tyrosine kinase inhibitors and their acquired resistance

(2018) Qinlian Jiao et al.   Molecular Cancer

Role of Bruton’s tyrosine kinase in B cells and malignancies

(2018) Simar Pal Singh et al.   Molecular Cancer

Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2018) Freddie Bray et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Anlotinib: a novel multi-targeting tyrosine kinase inhibitor in clinical development

(2018) Guoshuang Shen et al.   Journal of Hematology & Oncology

Exploratory Process Development of Lorlatinib

(2018) Bryan Li et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Dacomitinib: First Global Approval

(2018) Matt Shirley   DRUGS

Pyrotinib: First Global Approval

(2018) Hannah A. Blair   DRUGS

Fruquintinib: First Global Approval

(2018) Matt Shirley   DRUGS

Fibroblast growth factor receptors as treatment targets in clinical oncology

(2018) Masaru Katoh   Nature Reviews Clinical Oncology

First macrocyclic 3 rd -generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib

(2017) Sulman Basit et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Midostaurin for the treatment of acute myeloid leukemia

(2017) Mrinal M Patnaik   Future Oncology

Anticancer therapy-induced vascular toxicity: VEGF inhibition and beyond

(2017) Daniela Di Lisi et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

Molecular-Targeted Therapies for Epidermal Growth Factor Receptor and Its Resistance Mechanisms

(2017) Toshimitsu Yamaoka et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The efficacy of larotrectinib (LOXO-101), a selective tropomyosin receptor kinase (TRK) inhibitor, in adult and pediatric TRK fusion cancers.

(2017) David Michael Hyman et al.   JOURNAL OF CLINICAL ONCOLOGY

Dacomitinib versus gefitinib as first-line treatment for patients with EGFR -mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial

(2017) Yi-Long Wu et al.   LANCET ONCOLOGY

Osimertinib: A Review in T790M-Positive Advanced Non-Small Cell Lung Cancer

(2017) Yvette N. Lamb et al.   Targeted Oncology

Genetic basis and molecular pathophysiology of classical myeloproliferative neoplasms

(2016) William Vainchenker et al.   BLOOD

Antitumor activity of alectinib, a selective ALK inhibitor, in an ALK-positive NSCLC cell line harboring G1269A mutation

(2016) Yasushi Yoshimura et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Neratinib, A Novel HER2-Targeted Tyrosine Kinase Inhibitor

(2016) Shruti Rakesh Tiwari et al.   Clinical Breast Cancer

Osimertinib: First Global Approval

(2016) Sarah L. Greig   DRUGS

Olmutinib: First Global Approval

(2016) Esther S. Kim   DRUGS

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

Renal toxicity of anticancer agents targeting vascular endothelial growth factor (VEGF) and its receptors (VEGFRs)

(2016) Laura Cosmai et al.   JOURNAL OF NEPHROLOGY

Lenvatinib: A Review in Refractory Thyroid Cancer

(2016) James E. Frampton   Targeted Oncology

Platelet-derived growth factor receptor/platelet-derived growth factor (PDGFR/PDGF) system is a prognostic and treatment response biomarker with multifarious therapeutic targets in cancers

(2016) Kwaku Appiah-Kubi et al.   TUMOR BIOLOGY

Tivozanib: Status of Development

(2015) Muhammad Omer Jamil et al.   Current Oncology Reports

Alectinib: a selective, next-generation ALK inhibitor for treatment of ALK-rearranged non-small-cell lung cancer

(2015) Mariacarmela Santarpia et al.   Expert Review of Respiratory Medicine

Alectinib: A Review of Its Use in Advanced ALK-Rearranged Non-Small Cell Lung Cancer

(2014) Kate McKeage   DRUGS

Investigational FMS-like tyrosine kinase 3 inhibitors in treatment of acute myeloid leukemia

(2014) Naveen Pemmaraju et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Anaplastic lymphoma kinase inhibitors as anticancer therapeutics: a patent review

(2014) Eugen F Mesaros et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor

(2014) M. Raymond V. Finlay et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations

(2014) Ted W. Johnson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Clinical Targeting of Mutated and Wild-Type Protein Tyrosine Kinases in Cancer

(2014) J. M. Drake et al.   MOLECULAR AND CELLULAR BIOLOGY

Tyrosinkinasen in Weichgewebstumoren

(2014) T. Knösel et al.   PATHOLOGE

Epidermal growth factor receptor targeting in cancer: A review of trends and strategies

(2013) Chetan Yewale et al.   BIOMATERIALS

Cell survival and metastasis regulation by Akt signaling in colorectal cancer

(2013) Ekta Agarwal et al.   CELLULAR SIGNALLING

The emerging issue of cardiac dysfunction induced by antineoplastic angiogenesis inhibitors

(2013) Carlo G. Tocchetti et al.   EUROPEAN JOURNAL OF HEART FAILURE

Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT isoforms

(2013) Kerstin Maria Kampa-Schittenhelm et al.   Molecular Cancer

Bruton’s Tyrosine Kinase (BTK) Inhibitors in Clinical Trials

(2013) Jan A. Burger   Current Hematologic Malignancy Reports

Overcoming acquired resistance to kinase inhibition: The cases of EGFR, ALK and BRAF

(2012) Simon Giroux   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): A better mousetrap? A review of the clinical evidence

(2012) Sai-Hong Ignatius Ou   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Targeting the FMS-like tyrosine kinase 3 in acute myeloid leukemia

(2012) R Swords et al.   LEUKEMIA

FMS-like tyrosine kinase 3 inhibitors: a patent review

(2011) Jongkook Lee et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

9-Substituted 6,6-Dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as Highly Selective and Potent Anaplastic Lymphoma Kinase Inhibitors

(2011) Kazutomo Kinoshita et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting Oncogenic ALK: A Promising Strategy for Cancer Treatment

(2011) E. Grande et al.   MOLECULAR CANCER THERAPEUTICS

Novel Therapeutic Options in Anaplastic Large Cell Lymphoma: Molecular Targets and Immunological Tools

(2011) O. Merkel et al.   MOLECULAR CANCER THERAPEUTICS

Platelet-derived growth factor receptor tyrosine kinase inhibitors: a review of the recent patent literature

(2010) Yujia Dai   EXPERT OPINION ON THERAPEUTIC PATENTS

Inhibitors of anaplastic lymphoma kinase: a patent review

(2010) Karen L Milkiewicz et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action?

(2009) Kristy J. Gotink et al.   ANGIOGENESIS

Identification ofN-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor

(2009) Qi Chao et al.   JOURNAL OF MEDICINAL CHEMISTRY