First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.04.032
Abstract: Non-small cell lung cancers (NSCLC) harboring anaplastic lymphoma kinase (ALK) gene rearrangements invariably develop resistance to 2nd-generation ALK inhibitors. Lorlatinib (PF-06463922) (6) is a 3rd-generation macrocyclic ALK-TKI that demonstrates many advantages over 2nd-generation ALK inhibitors.… read more here.
Keywords: inhibitor; alk; alk ros1; generation ... See more keywords
Evolution in the treatment landscape of non-small cell lung cancer with ALK gene alterations: from the first- to third-generation of ALK inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Expert Opinion on Emerging Drugs"
DOI: 10.1080/14728214.2018.1527902
Abstract: ABSTRACT Introduction: The medical treatment of non-small cell lung cancer (NSCLC) has radically changed over the last 10 years thanks to new molecular-targeted drugs able to act on biological mechanisms involved in tumor development. One… read more here.
Keywords: alk inhibitors; alk; treatment; generation ... See more keywords
Ensartinib (X-396), a second-generation ALK TKI, in Chinese ALK-positive non-small cell lung cancer: A phase I, dose-escalation study.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2018.36.15_suppl.e21122
Abstract: e21122Background: Ensartinib (X-396) is a novel, selective, oral ALK inhibitor with 10-fold higher potency than crizotinib, which is effective and well tolerated in US ALK+ NSCLC patients at 225 mg... read more here.
Keywords: alk; alk tki; ensartinib 396; second generation ... See more keywords
How to select the best upfront therapy for metastatic disease? Focus on ALK-rearranged non-small cell lung cancer (NSCLC).
Sign Up to like & getrecommendations! Published in 2020 at "Translational lung cancer research"
DOI: 10.21037/tlcr-20-331
Abstract: Anaplastic lymphoma kinase (ALK) inhibitors have demonstrated robust clinical activity in patients with ALK-rearranged lung cancers. The echinoderm microtubule-associated protein-like (EML)-ALK translocation was first discovered in 2007 and 4 years later, crizotinib, a first-generation ALK… read more here.
Keywords: lung; alk; generation alk; alk inhibitors ... See more keywords
Targeting ALK Rearrangements in NSCLC: Current State of the Art
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Oncology"
DOI: 10.3389/fonc.2022.863461
Abstract: Anaplastic lymphoma kinase (ALK) alterations in non-small cell lung cancer (NSCLC) can be effectively treated with a variety of ALK-targeted drugs. After the approval of the first-generation ALK inhibitor crizotinib which achieved better results in… read more here.
Keywords: alk inhibitors; generation alk; alk rearrangements; targeting alk ... See more keywords
Silibinin Overcomes EMT-Driven Lung Cancer Resistance to New-Generation ALK Inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Cancers"
DOI: 10.3390/cancers14246101
Abstract: Simple Summary Epithelial-to-mesenchymal transition (EMT) is a cellular plasticity program that can confer invasiveness, dissemination, and therapy resistance to cancer cells. Although inhibitors of this cellular process are expected to work as good “partners” for… read more here.
Keywords: alk tkis; generation alk; resistance; alk ... See more keywords