page_title: Alectinib
section_title: Pharmacokinetics
hierarchical_section_title: Alectinib / Pharmacology / Pharmacokinetics
context_page_description: Alectinib is an oral drug that blocks the activity of anaplastic lymphoma kinase and is used to treat non-small-cell lung cancer. It was developed by Chugai Pharmaceutical Co. Japan, which is part of the Hoffmann-La Roche group.
context_section_description: When taken with a meal, the absolute bioavailability of the drug is 37%, and highest blood plasma concentrations are reached after four to six hours. Steady state conditions are reached within seven days. Plasma protein binding of alectinib and M4 is over 99%. The enzyme mainly responsible for alectinib metabolism is CYP3A4; other CYP enzymes and aldehyde dehydrogenases only play a small role. Alectinib and M4 account for 76% of the circulating substance, while the rest are minor metabolites.
  Plasma half-life of alectinib is 32.5 hours, and that of M4 is 30.7 hours. 98% are excreted via the faeces, of which 84% are unchanged alectinib and 6% are M4. Less than 1% are found in the urine.
caption: Proposed metabolism of alectinib. Alectinib itself and the active metabolite M4 are the main compounds found in the circulation, while the others are minor metabolites.[12]