Kinase drug discovery 20 years after imatinib: progress and future directions
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …
Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021
Q Wu, W Qian, X Sun, S Jiang - Journal of hematology & oncology, 2022 - Springer
Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …
Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis
CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …
including cancer, has fostered incremental efforts on drug discovery programs over the past …
Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …
structures or functions that are difficult to interfere with using conventional drug design …
The ascension of targeted covalent inhibitors
J Singh - Journal of Medicinal Chemistry, 2022 - ACS Publications
Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …
Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label …
YL Wu, Y Cheng, X Zhou, KH Lee, K Nakagawa… - The Lancet …, 2017 - thelancet.com
Background Dacomitinib is a second-generation, irreversible EGFR tyrosine kinase inhibitor.
We compared its efficacy and safety with that of the reversible EGFR tyrosine kinase inhibitor …
We compared its efficacy and safety with that of the reversible EGFR tyrosine kinase inhibitor …
[HTML][HTML] Mechanisms of acquired resistance to first-and second-generation EGFR tyrosine kinase inhibitors
Patients with non-small-cell lung cancer (NSCLC) whose tumours harbour activating
mutations within the epidermal growth factor receptor (EGFR) frequently derive significant …
mutations within the epidermal growth factor receptor (EGFR) frequently derive significant …
Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers
R Roskoski Jr - Pharmacological research, 2019 - Elsevier
The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …
owing to its general role in signal transduction and in oncogenesis. This family consists of …
Improvement in overall survival in a randomized study that compared dacomitinib with gefitinib in patients with advanced non–small-cell lung cancer and EGFR …
TS Mok, Y Cheng, X Zhou, KH Lee… - Journal of Clinical …, 2018 - ascopubs.org
Purpose ARCHER 1050, a randomized, open-label, phase III study of dacomitinib versus
gefitinib in treatment-naïve patients with advanced non–small-cell lung cancer (NSCLC) and …
gefitinib in treatment-naïve patients with advanced non–small-cell lung cancer (NSCLC) and …
AZD9291 in EGFR inhibitor–resistant non–small-cell lung cancer
Background The EGFR T790M mutation is the most common mechanism of drug resistance
to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in patients who have …
to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in patients who have …