2018
DOI: 10.1007/978-3-319-91442-8_17
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Alectinib

Abstract: Alectinib is an ATP-competitive small molecule and a second-generation inhibitor of ALK. EML4-ALK rearrangement is found in 3-5% of patients with NSCLC. The first-generation inhibitor crizotinib has changed the treatment dramatically, though most of the patients show disease progression within one year. Extra-thoracic progress, i.e., CNS metastases is common. The second-generation inhibitor alectinib has shown significant improvement in PFS and a remarkable prolongation of time to CNS progression. Alectinib ha… Show more

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Cited by 16 publications
(10 citation statements)
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“…ALK mutations, especially rearrangements, exhibit strong translational activity in NSCLC [ 81 ]. ALK-targeted agents such as alectinib [ 82 ] and brigatinib [ 83 ] have shown extraordinary efficacy in ALK-positive NSCLC and have become the first-line therapies [ 84 ]. Lorlatinib, an ALK inhibitor [ 85 ], appears as a burst word in 2020, and ALK-TKI and ALK rearrangement have a high weight from 2019 to 2020 ( Figure 3 ), both of which indicate the rapidly rising attention on ALK.…”
Section: Discussionmentioning
confidence: 99%
“…ALK mutations, especially rearrangements, exhibit strong translational activity in NSCLC [ 81 ]. ALK-targeted agents such as alectinib [ 82 ] and brigatinib [ 83 ] have shown extraordinary efficacy in ALK-positive NSCLC and have become the first-line therapies [ 84 ]. Lorlatinib, an ALK inhibitor [ 85 ], appears as a burst word in 2020, and ALK-TKI and ALK rearrangement have a high weight from 2019 to 2020 ( Figure 3 ), both of which indicate the rapidly rising attention on ALK.…”
Section: Discussionmentioning
confidence: 99%
“…In our case, tubular injury was the predominant manifestation, but the severity was lower than reported by Ramachandran et al Alectinib is an ATP-competitive small molecule, which has improved the progression free survival in ALK positive NCLSC through the inhibition of ALK and RET protein phosphorylation thus disrupting downstream signalling of cell proliferation. 10 11 . Whether this ability to inhibit cell proliferation signalling may also affect renal tubular cells to result in tubular injury is unclear but could be a possible explanatory mechanism.…”
Section: Discussionmentioning
confidence: 99%
“…Since HCoV-OC43, as other coronaviruses, is able to invade the CNS (Dubé et al, 2018), alectinib might be an interesting candidate for the treatment of HCoV-OC43 persistent infections in the brain. Moreover, the free levels of alectinib found in both plasma and cerebrospinal fluid are similar (Herden & Waller, 2018) and its EC 50 against HCoV-OC43 (0.6 uM) is lower than the maximum level attainable in human serum with daily recommended dosage (676 ng/mL corresponding to 1.4 μM) (Ly et al, 2018).…”
Section: Discussionmentioning
confidence: 99%