Differential Chemoproteomics Reveals MARK2/3 as Cell Migration‐Relevant Targets of the ALK Inhibitor Brigatinib
Sign Up to like & getrecommendations! Published in 2023 at "ChemBioChem"
DOI: 10.1002/cbic.202200766
Abstract: Metastasis poses a major challenge in cancer management, including EML4‐ALK‐rearranged non‐small cell lung cancer (NSCLC). As cell migration is a critical step during metastasis, we assessed the anti‐migratory activities of several clinical ALK inhibitors in… read more here.
Keywords: brigatinib; cell; eml4 alk; alk ... See more keywords
Effect of severe renal impairment on the pharmacokinetics of brigatinib
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DOI: 10.1007/s10637-021-01095-5
Abstract: Background Brigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor, targets activated, mutant forms of ALK and overcomes mechanisms of resistance to the ALK inhibitors crizotinib, ceritinib, and alectinib. Brigatinib is approved in multiple countries for… read more here.
Keywords: patients severe; severe renal; brigatinib; impairment ... See more keywords
Brigatinib in Patients With Alectinib‐Refractory ALK‐Positive NSCLC
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DOI: 10.1016/j.jtho.2018.06.005
Abstract: Introduction: The second‐generation anaplastic lymphoma kinase (ALK) inhibitor alectinib recently showed superior efficacy compared to the first‐generation ALK inhibitor crizotinib in advanced ALK‐rearranged NSCLC, establishing alectinib as the new standard first‐line therapy. Brigatinib, another second‐generation… read more here.
Keywords: positive nsclc; alectinib refractory; alk; alk positive ... See more keywords
Health-related quality of life in the randomized phase III trial of brigatinib vs crizotinib in advanced ALK inhibitor-naive ALK + non-small cell lung cancer (ALTA-1L).
Sign Up to like & getrecommendations! Published in 2021 at "Lung cancer"
DOI: 10.1016/j.lungcan.2021.03.005
Abstract: OBJECTIVE In ALTA-1 L, first-line brigatinib versus crizotinib significantly prolonged progression-free survival in advanced ALK-positive (ALK+) non-small cell lung cancer (NSCLC). We report health-related quality of life (HRQOL) outcomes from ALTA-1 L. MATERIALS AND METHODS HRQOL was… read more here.
Keywords: alk; crizotinib; brigatinib; lung cancer ... See more keywords
Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00373
Abstract: Proteolysis-targeting chimera (PROTAC) is an attractive technology in drug discovery. Canonically, targets act as a basic starting point in the most previous PROTAC design. Here, we designed degraders considering from the view of clinical benefits.… read more here.
Keywords: degrader siais164018; kinome; metastasis; discovery ... See more keywords
Brigatinib as a treatment of ALK-positive non-small cell lung cancer
Sign Up to like & getrecommendations! Published in 2021 at "Expert Review of Precision Medicine and Drug Development"
DOI: 10.1080/23808993.2021.1954907
Abstract: ABSTRACT Introduction Anaplastic lymphoma kinase (ALK) gene rearrangements and resulting fusion proteins occur in 3%-7% of patients with non-small-cell lung cancer (NSCLC), conferring sensitivity to treatment with ALK Tyrosine-Kinase Inhibitors. After the first-generation ALK inhibitor… read more here.
Keywords: alk; treatment; alk positive; brigatinib ... See more keywords
Multidisciplinary treatment of advanced or metastatic ALK-positive non-small cell lung cancer: Real-world data on Brigatinib combined with local therapy
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DOI: 10.1097/md.0000000000042297
Abstract: Anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) often shows incomplete responses and progression despite tyrosine kinase inhibitor (TKI) therapy. Preliminary data suggest that combining brigatinib, an ALK-selective TKI, with surgery or radiotherapy may… read more here.
Keywords: brigatinib; treatment; therapy; local therapy ... See more keywords
Population Pharmacokinetic and Exposure-Response Analyses From ALTA-1L: Model-Based Analyses Supporting the Brigatinib Dose in ALK-Positive NSCLC.
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DOI: 10.1111/cts.13231
Abstract: The ALK in Lung Cancer Trial of brigAtinib in 1st Line (ALTA-1L) compared brigatinib versus crizotinib in ALK inhibitor-naive patients with ALK+ NSCLC. A population pharmacokinetic (PK) model was used to estimate brigatinib exposures for… read more here.
Keywords: time; exposure; line; model ... See more keywords
Preliminary results of single arm phase 2 trial of brigatinib in patients (pts) with progression disease (PD) after next-generation (NG) anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitors (TKIs) in ALK + non-small cell lung cancer (NSCLC).
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2019.37.15_suppl.9027
Abstract: 9027 Background: NG ALK TKIs are the standard first-line therapy for patients with advanced ALK + NSCLC. Brigatinib has activity against ALK resistance mutations and has CNS activity. The efficacy of brigatinib after NG ALK… read more here.
Keywords: kinase; alk; activity; next generation ... See more keywords
The cost-effectiveness of brigatinib in adult patients with ALK inhibitor-naive ALK-positive non-small cell lung cancer from a US perspective.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of managed care & specialty pharmacy"
DOI: 10.18553/jmcp.2022.28.9.970
Abstract: BACKGROUND: The discovery of specific oncogenic drivers in non-small cell lung cancer (NSCLC) has led to the development of highly targeted anaplastic lymphoma kinase tyrosine kinase inhibitors (ALKis). Brigatinib is a next-generation ALKi associated with… read more here.
Keywords: brigatinib; cost; cost effectiveness; naive alk ... See more keywords
Alectinib Efficacy Post-Brigatinib Against Advanced ALK+ Non-Small Cell Lung Cancer (BrigALK2-GFPC 02-2019 Study)
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DOI: 10.2147/lctt.s522038
Abstract: Background Brigatinib and alectinib are next-generation anaplastic lymphoma kinase inhibitors (ALKis) showing efficacy against naïve and post-crizotinib-treated advanced ALK+ non-small-cell lung cancers (NSCLCs). Real-world data on alectinib efficacy after brigatinib failure are lacking. Methods Alectinib… read more here.
Keywords: brigatinib; advanced alk; alectinib efficacy; post brigatinib ... See more keywords