What are the contraindications for Crizotinib/Xalkori?

Crizotinib is a small molecule tyrosine kinase inhibitor mainly used to treat ALK rearranged or ROS1-positive non-small cell lung cancer (NSCLC) . Although its efficacy is remarkable, there are still certain contraindications and usage restrictions during clinical application. Patients need to fully communicate with their doctors and strictly follow the instructions.

The clearest contraindication is in patients with a severe allergic reaction to crizotinib or components of its formulations. If you have experienced acute anaphylactic shock, severe rash, or difficulty breathing, you should not continue to use this medicine. Secondly, crizotinib should be used with caution in patients with hepatic impairment, especially those with severe hepatic insufficiency, because the drug is mainly metabolized by the liver. If the liver's detoxification function is significantly weakened, it may lead to drug accumulation and aggravation of toxic and side effects.

Heart taboos also deserve attention. Crizotinib may cause bradycardia, arrhythmia and even QT interval prolongation. Therefore, patients with previous severe arrhythmias, uncontrolled heart failure, or other drugs that may prolong the QT interval should avoid use or be closely monitored. For patients with obvious hypokalemia and hypomagnesemia, if they are not corrected in time, they are also potentially contraindicated.

In addition, crizotinib may affect vision, and some patients may experience symptoms such as blurred vision and light sensitivity. Although most of them are reversible, for people in occupations that require high visual sensitivity (such as drivers, pilots, etc.), extreme caution should be used when using them. The drug may also impose a certain burden on renal function, so patients with severe renal insufficiency require individualized dose adjustment.

Pregnant and breastfeeding women are specifically prohibited from using crizotinib. Animal studies have shown that it may have adverse effects on fetal development. Therefore, female patients who want to have children need to conduct a pregnancy test before treatment and take effective contraceptive measures while taking the medicine. Breastfeeding patients should avoid breastfeeding to prevent the potential harm of the drug to the baby through breast milk.

Reference materials:https://go.drugbank.com/drugs/DB08865