Product Details
Crizotinib, a new drug for the treatment of tumors
Crizotinib is administered in combination with an inducer
? A single dose of Crizotinib is taken orally, combined with the strong inducer rifampicin ( ?, once daily), crizotinib's and? were reduced by ?%? and %?, respectively, compared with crizotinib alone. However, the magnitude of the effect of inducers on steady-state crizotinib exposure has not been established [see Drug Interactions]. ?
Crizotinib and antacids are used together?
????The water solubility of crizotinib depends on the value. The higher the value (acidic), the lower the solubility. Drugs that increase intragastric values (such as proton pump inhibitors, receptor blockers, or antacids) may decrease the solubility of crizotinib and subsequently reduce its bioavailability. However, no formal pharmaceutical studies on the interaction between crizotinib and antacids have been conducted. ?
Combined use with other substrates?
In vitro studies have shown that although crizotinib is an inhibitor of the metabolism of substrates such as ?, B, ?, or ?, it will not be clinically Drug interactions occur. An in vitro study in human hepatocytes showed that although crizotinib is a mediating inducer of substrate metabolism, clinical drug interactions do not occur. ?
Used in combination with transport substrates?
????Crizotinib is an in vitro inhibitor of ??glycoprotein (?). Therefore, when crizotinib is used concomitantly with drugs that are glycoprotein substrates, its plasma concentration may be increased. In vitro studies found that therapeutic concentrations of crizotinib did not inhibit human hepatic uptake transporters ?B or B. Therefore, although crizotinib is a mediated inhibitor of hepatic uptake of certain transported substrates, no clinical drug interactions will occur.
?Pharmacokinetics in Special Populations?
Hepatic Impairment: The use of crizotinib in patients with hepatic impairment has not been studied. Since crizotinib is primarily metabolized in the liver, hepatic impairment is likely to increase crizotinib plasma concentrations. Clinical studies excluded patients who were ? or ? times the upper limit of normal or whose total bilirubin was ? times the upper limit of normal due to liver metastasis. Therefore, patients with hepatic impairment should be treated with caution when using crizotinib capsules.
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