2017
DOI: 10.1097/md.0000000000008652
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Crizotinib resistance overcome by ceritinib in an ALK-positive non-small cell lung cancer patient with brain metastases

Abstract: Rationale:The treatment of non-small cell lung cancer (NSCLC) has now changed dramatically in recent years and anaplastic lymphoma receptor tyrosine kinase (ALK) inhibitors are developing rapidly.Patient concerns:Here we reported a 57-year-old ALK-positive NSCLC man with brain metastases.Diagnoses:A case of lung adenocarcinoma with brain metastases.Interventions:Crizotinib was administered orally at a dose of 250mg twice a day until the brain metastases were found. Treatment with orally administered ceritinib … Show more

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Cited by 8 publications
(2 citation statements)
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“…Notably, the concentration of 1 µM ceritinib that we used in long-term experiments can be achieved in the plasma of patients [22]. Lung cancer patients with brain metastases also respond to the treatment with ceritinib, suggesting that this drug is effective across the blood–brain barrier [29]. The concentration achieved in the mouse brain after oral administration was low, with a brain-to-plasma ratio below 0.3 [30], but the blood-to-brain exposure ratio of ceritinib in humans has yet to be determined.…”
Section: Discussionmentioning
confidence: 99%
“…Notably, the concentration of 1 µM ceritinib that we used in long-term experiments can be achieved in the plasma of patients [22]. Lung cancer patients with brain metastases also respond to the treatment with ceritinib, suggesting that this drug is effective across the blood–brain barrier [29]. The concentration achieved in the mouse brain after oral administration was low, with a brain-to-plasma ratio below 0.3 [30], but the blood-to-brain exposure ratio of ceritinib in humans has yet to be determined.…”
Section: Discussionmentioning
confidence: 99%
“…Ceritinib inhibits kinases such as ROS proto-oncogene 1 (ROS1), INSR, and IGF1R, although it is most active against ALK [9]. Lung cancer patients with brain metastases also respond to the treatment with ceritinib, suggesting that this drug is effective across the BBB [58]. The concentration achieved in the mouse brain after oral administration is low, with a brain-to-plasma ratio below 0.3 [59], but the blood-to-brain exposure ratio of ceritinib in humans is yet to be determined.…”
Section: Discussionmentioning
confidence: 99%