Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical research in toxicology"
DOI: 10.1021/acs.chemrestox.2c00057
Abstract: Masitinib is a small molecule tyrosine kinase inhibitor under investigation for the treatment of amyotrophic lateral sclerosis, mastocytosis, and COVID-19. Hepatotoxicity has been reported in some patients while taking masitinib. The liver injury is thought… read more here.
Keywords: metabolic activation; kinase inhibitor; p450; tyrosine kinase ... See more keywords
Efficacy and Safety of Masitinib in Corticosteroid-Dependent Severe Asthma: A Randomized Placebo-Controlled Trial
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DOI: 10.2147/jaa.s337284
Abstract: Background Masitinib is an oral tyrosine kinase inhibitor that selectively targets mast cell activity and platelet-derived growth factor receptor (PDGFR) signaling, both of which are implicated in various mechanisms of asthma pathogenesis. Objective Assessment of… read more here.
Keywords: placebo; masitinib; severe asthma; dependent severe ... See more keywords
ALS Clinical Trials Review: 20 Years of Failure. Are We Any Closer to Registering a New Treatment?
Sign Up to like & getrecommendations! Published in 2017 at "Frontiers in Aging Neuroscience"
DOI: 10.3389/fnagi.2017.00068
Abstract: Amyotrophic lateral sclerosis (ALS) is a devastating condition with an estimated mortality of 30,000 patients a year worldwide. The median reported survival time since onset ranges from 24 to 48 months. Riluzole is the only… read more here.
Keywords: treatment; clinical trials; masitinib; edaravone ... See more keywords
'Piperazining' the catalytic gatekeepers: unraveling the pan-inhibition of SRC kinases; LYN, FYN and BLK by masitinib.
Sign Up to like & getrecommendations! Published in 2019 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2018-0354
Abstract: Aim: Blocking oncogenic signaling of B-cell receptor (BCR) has been explored as a viable strategy in the treatment of diffuse large B-cell lymphoma. Masitinib is shown to multitarget LYN, FYN and BLK kinases that propagate… read more here.
Keywords: fyn; blk; lyn fyn; fyn blk ... See more keywords