Crizotinib


Other name

DB08865

International/Other brands

Xalkori

Groups

Approved

Structure

Prescription products

NameDosageStrengthRouteLabeller
XalkoriCapsule200 mgOralPfizer
XalkoriCapsule250 mgOralPfizer
XalkoriCapsule200 mg/1OralPfizer Laboratories Div Pfizer Inc.
XalkoriCapsule250 mg/1OralPfizer Laboratories Div Pfizer Inc.

Target

-

Description

Crizotinib an inhibitor of receptor tyrosine kinase for the treatment of non-small cell lung cancer (NSCLC). Verification of the presence of ALK fusion gene is done by Abbott Molecular's Vysis ALK Break Apart FISH Probe Kit. This verification is used to select for patients suitable for treatment. FDA approved in August 26, 2011.

Indications

Metastatic Non-Small Cell Lung Cancer

Other indications

-

Mechaism of action

-

Absorption

The peak serum concentration was reached in 4 to 6 hours following an oral single-dose administration. Steady state was reached within 15 days when a dose of 250 mg twice daily was administered. The mean absolute bioavailability was 43% (range of 32% to 66%) following a single 250 mg oral dose. When taken with high-fat meal, AUC and Cmax were reduced.

Metabolism

Crizotinib is metabolized by CYP3A4 and CYP3A5 in which these enzymes mediates the O-dealkylation of the drug.

Toxicity

-