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Ceritinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test.
Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays.
Ceritinib inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice and rats. Ceritinib exhibited dose-dependent anti-tumor activity in mice bearing EML4 ALK-positive NSCLC xenografts with demonstrated resistance to crizotinib, at concentrations within a clinically relevant range.
The recommended dosage of Ceritinib is 450 mg orally once daily with food until disease progression or unacceptable toxicity. If a dose of Ceritinib is missed, make up that dose unless the next dose is due within 12 hours. If vomiting occurs during the course of treatment, do not administer an additional dose and continue with the next scheduled dose of Ceritinib.
The most common adverse reactions (incidence of ≥ 25%) in patients treated with Ceritinib 450 mg with food are diarrhea, nausea, abdominal pain, vomiting, and fatigue and with Ceritinib 750 mg under fasted conditions are diarrhea, nausea, vomiting, fatigue, abdominal pain, decreased appetite, and weight loss.
Based on animal studies and its mechanism of action, Ceritinib can cause fetal harm when administered to a pregnant woman. The limited available data on the use of Ceritinib in pregnant women are insufficient to inform risk. Administration of ceritinib to rats and rabbits during the period of organogenesis at maternal plasma exposures below the recommended human dose caused increases in skeletal anomalies in rats and rabbits. Advise a pregnant woman of the potential risk to a fetus.
There are no data regarding the presence of ceritinib or its metabolites in human milk, the effects of ceritinib on the breastfed child or its effects on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with Ceritinib and for 2 weeks following completion of therapy.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Ceritinib 150 mg