Medical Pharmacology Practice Questions: Tyrosine Kinase
Inhibitor (VEGFR-1,2,3) : axitinib (Inlyta)
Click on the correct answer.
Axitinib is classified as a potent VEGF-R inhibitor.
True
False
Axitinib (Inlyta):
Associated with inhibition of VEGFR1, 2, 3 kinase activity.
Associated with inhibition of pathologic angiogenesis by means of the drug's effect on VEGFR.
Both
Neither
Axitinib pharmacodynamic/pharmacokinetics:
Rapid drug absorption
High level of protein binding (mainly albumin).
Both
Neither
Axitinib pharmacodynamics/pharmacokinetics:
Metabolism involves the liver microsomal drug metabolizing P450 system. Metabolism is due mainly to CYP3A4/5 cytochrome P450 isoforms.
Excretion occurs bothin the feces and urine.
Both
Neither
Axitinib clinical indication(s):
Treatment of patients with advanced non-small cell lung cancer who have failed prior treatment with oxaliplatin.
Treatment of patients with advanced renal cell carcinoma who have failed one prior systemic protocol
Both
Neither
Axitinib is considered a second-line treatment option in patients with renal cell carcinoma.
True
False
Inactivation of axitinib:
Associated with CYP3A4-catalyzed sulfoxidation.
Associated with phase II N-glucuronidation
Both
Neither
Hypertension associated with VEGF-R inhibitor treatment may be a predictor of a positive therapeutic effect.
True
Major adverse effect(s) associated with axitinib administration:
Hypertension
Thrombosis
Bleeding
A & B
B & C
A & C
A, B & C
Adverse effects on pregnancy may occur with axitinib; accordingly, a pregnancy test prior to treatment is appropriate and effective contraception should be used not only during axitinib treatment but also for a period of one week after the last axitinib dose.
