Inlyta Dosage/Direction for Use

Posology: Treatment with Axitinib should be initiated by a physician experienced in the use of anticancer therapies.
The recommended starting oral dose of Axitinib is 5 mg twice daily. Administer axitinib doses approximately 12 hours apart with or without food (see Pharmacology: Pharmacokinetics under Actions). Axitinib should be swallowed whole with a glass of water.
Treatment should continue as long as clinical benefit is observed or until unacceptable toxicity occurs, that cannot be managed by concomitant medications or dose adjustments.
If the patient vomits or misses a dose, an additional dose should not be taken. The next prescribed dose should be taken at the usual time.
Dose adjustments: Dose increase or reduction is recommended based on individual safety and tolerability.
Patients who tolerate the Axitinib starting dose of 5 mg twice daily with no adverse reactions >Grade 2 (according to the Common Toxicity Criteria for Adverse Events [CTCAE]) for two consecutive weeks, are normotensive, and are not receiving antihypertensive medication, may have their dose increased to 7 mg twice daily. Subsequently, using the same criteria, patients who tolerate the axitinib dose of 7 mg twice daily, may have their dose increased to a maximum of 10 mg twice daily.
Management of some adverse drug reactions may require temporary or permanent discontinuation and/or dose reduction of axitinib therapy. When dose reduction is necessary, the axitinib dose may be reduced to 3 mg twice daily and further to 2 mg twice daily.
Dose adjustment is not required on the basis of patient age, race, gender, or body weight.
Concomitant strong CYP3A4/5 inhibitors: Co-administration of axitinib with strong CYP3A4/5 inhibitors should be avoided (e.g., ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin) as they may increase axitinib plasma concentrations. Grapefruit may also increase axitinib plasma concentrations. Selection of an alternate concomitant medication with no or minimal CYP3A4/5 inhibition potential is recommended.
Although axitinib dose adjustment has not been studied in patients receiving strong CYP3A4/5 inhibitors, if a strong CYP3A4/5 inhibitor must be co-administered, a dose decrease of axitinib to approximately half the dose (e.g., from a starting dose of 5 mg twice daily to a reduced dose of 2 mg twice daily) is recommended. If co-administration of the strong inhibitor is discontinued, a return to the axitinib dose used prior to initiation of the strong CYP3A4/5 inhibitor should be considered (after 3-5 half-lives of the inhibitor).
Concomitant strong CYP3A4/5 inducers: Co-administration of axitinib with strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentin, phenobarbital, and Hypericum perforatum [also known as St. John's wort]) may decrease axitinib plasma concentrations. Selection of an alternate concomitant medication with no or minimal CYP3A4/5 induction potential is recommended.
Although axitinib dose adjustment has not been studied in patients receiving strong CYP3A4/5 inducers, if a strong CYP3A4/5 inducer must be co-administered, a gradual dose increase of axitinib is recommended. If the dose of axitinib is increased, the patient should be monitored carefully for toxicity. If co-administration of the strong inducer is discontinued, the axitinib dose should be immediately returned to the dose used prior to initiation of the strong CYP3A4/5 inducer.
Use in pediatrics: The safety and efficacy of axitinib in children (<18 years) have not been established. No data are available.
Use in the elderly (≥65 years): No dose adjustment is required (see Pharmacology: Pharmacokinetics under Actions).
Hepatic impairment: No dose adjustment is required when administering axitinib to patients with mild hepatic impairment (Child-Pugh class A). A dose decrease is recommended when administering Axitinib to patients with moderate hepatic impairment (Child-Pugh class B) [e.g., the starting dose should be reduced from 5 mg twice daily to 2 mg twice daily]. Axitinib has not been studied in patients with severe hepatic impairment (Child-Pugh class C) and should not be used in this population (see Pharmacology: Pharmacokinetics under Actions and Precautions).
Renal impairment: No dose adjustment is required (see Pharmacology: Pharmacokinetics under Actions).
Virtually no data are available regarding axitinib treatment in patients with a creatinine clearance of <15 mL/min.