Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC DOI Creative Commons
Misako Nagasaka, Viola W. Zhu, Sun Min Lim

et al.

Journal of Thoracic Oncology, Journal Year: 2020, Volume and Issue: 16(5), P. 740 - 763

Published: Dec. 17, 2020

Single-agent osimertinib is the standard of care for first-line treatment advancedEGFR+ NSCLC and remained only marketed third-generation EGFR tyrosine kinase inhibitor (TKI) until March 2020 when almonertinib (HS-10296) was approved in People's Republic China advanced T790M+ based on a phase 2 expansion study 1/2 trial. In this review, we profiled many TKIs late-stage clinical development (e.g., almonertinib, lazertinib, alflutinib1, rezivertinib, ASK120069, SH-1028, D-0316, abivertinib) their interim results from 1 trials, included designs 3 trials chemical structures publicly available. We also listed other pipeline search trial registration websites. addition, summarized that previously reported (rociletinib, olmutinib, nazartinib, mavelertinib), including rociletinib naquotinib. further combination design FLAURA2 (NCT04035486), MARIPOSA (NCT04487080), ACROSS1 (NCT04500704), ACROSS2 (NCT04500717) if positive can potentially usher next EGFR+ NSCLC.

Language: Английский

ctDNA as a cancer biomarker: A broad overview DOI

Luciana Santos Pessoa,

Manoela Heringer,

Valéria Pereira Ferrer

et al.

Critical Reviews in Oncology/Hematology, Journal Year: 2020, Volume and Issue: 155, P. 103109 - 103109

Published: Sept. 25, 2020

Language: Английский

Citations

200
Optimizing the sequencing of tyrosine kinase inhibitors (TKIs) in epidermal growth factor receptor (EGFR) mutation-positive non-small cell lung cancer (NSCLC) DOI Creative Commons

A. Gelatti,

Alexander Drilon, Fernando C. Santini

et al.

Lung Cancer, Journal Year: 2019, Volume and Issue: 137, P. 113 - 122

Published: Sept. 23, 2019

Non-small cell lung cancer (NSCLC) is the most common type of cancer, accounting for 80–85% cases. Epidermal growth factor receptor (EGFR) mutations are observed in approximately 40% and 20% patients with NSCLC Asian non-Asian populations, respectively.First-generation (gefitinib, erlotinib) second-generation (afatinib, dacomitinib) EGFR-tyrosine kinase inhibitors (TKIs) have been standard-of-care (SoC) first-line treatment sensitizing EGFR mutation positive advanced following Phase III trials versus platinum-based doublet chemotherapy. However, treated first- or EGFR-TKIs develop resistance. Osimertinib, a third-generation, central nervous system active EGFR-TKI which potently selectively inhibits both (EGFRm) T790 M resistance mutations, has shown superior efficacy first-generation (gefitinib / erlotinib). Osimertinib now option harboring EGFRm setting, choice disease progression on EGFR-TKIs. The dacomitinib also recently approved metastatic NSCLC.There remains need to determine appropriate sequencing this including as monotherapy combination other TKIs signaling pathway inhibitors. This review considers evolving role treatments maximize benefits NSCLC.

Language: Английский

Citations

189
Therapeutic strategies for EGFR-mutated non-small cell lung cancer patients with osimertinib resistance DOI Creative Commons
Kai Fu,

Fachao Xie,

Fang Wang

et al.

Journal of Hematology & Oncology, Journal Year: 2022, Volume and Issue: 15(1)

Published: Dec. 8, 2022

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are the preferential options for advanced non-small cell lung cancer (NSCLC) patients harboring EGFR mutations. Osimertinib is a potent irreversible third-generation EGFR-TKI targeting mutations but has little effect on wild-type EGFR. In view of its remarkable efficacy and manageable safety, osimertinib was recommended as standard first-line treatment or metastatic NSCLC with However, other EGFR-TKIs, will inevitably develop acquired resistance, which limits EGFR-mutated patients. The etiology triggering resistance complex including EGFR-dependent EGFR-independent pathways, different therapeutic strategies have been developed. Herein, we comprehensively summarized mechanisms discuss in detail potential suffering sake improvement survival further achievement precise medicine.

Language: Английский

Citations

184
EGFR signaling pathway as therapeutic target in human cancers DOI Creative Commons
Elena Levantini, Giorgia Maroni, Marzia Del Re

et al.

Seminars in Cancer Biology, Journal Year: 2022, Volume and Issue: 85, P. 253 - 275

Published: April 12, 2022

Language: Английский

Citations

174
Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC DOI Creative Commons
Misako Nagasaka, Viola W. Zhu, Sun Min Lim

et al.

Journal of Thoracic Oncology, Journal Year: 2020, Volume and Issue: 16(5), P. 740 - 763

Published: Dec. 17, 2020

Single-agent osimertinib is the standard of care for first-line treatment advancedEGFR+ NSCLC and remained only marketed third-generation EGFR tyrosine kinase inhibitor (TKI) until March 2020 when almonertinib (HS-10296) was approved in People's Republic China advanced T790M+ based on a phase 2 expansion study 1/2 trial. In this review, we profiled many TKIs late-stage clinical development (e.g., almonertinib, lazertinib, alflutinib1, rezivertinib, ASK120069, SH-1028, D-0316, abivertinib) their interim results from 1 trials, included designs 3 trials chemical structures publicly available. We also listed other pipeline search trial registration websites. addition, summarized that previously reported (rociletinib, olmutinib, nazartinib, mavelertinib), including rociletinib naquotinib. further combination design FLAURA2 (NCT04035486), MARIPOSA (NCT04487080), ACROSS1 (NCT04500704), ACROSS2 (NCT04500717) if positive can potentially usher next EGFR+ NSCLC.

Language: Английский

Citations

169