Dosing & Uses
Dosage Forms & Strengths
Renal Cell Carcinoma
Indicated for treatment of advanced renal cell carcinoma after failure of 1 prior systemic therapy
Initial dose: 5 mg PO q12hr (see Dosage Modifications)
Dose increase or reduction based on individual safety and tolerability
- Criteria: Tolerated for at least 2 consecutive weeks with no adverse reactions (ie, not exceeding grade 2 toxicities) and are normotensive and not receiving antihypertension medications
- First dose increase: 7 mg PO BID
- Second dose increase: Using the same criteria, may further increase to 10 mg PO BID
Dose reduction or discontinuation
- Hypertension: If persistent hypertension occurs despite antihypertensive medications, reduce dose; discontinue if hypertension is severe and persists despite dose reduction
- Hypertensive crisis: Discontinue axitinib
- Hemorrhage: If any bleeding requires medical intervention, temporarily interrupt axitinib dose
- Surgery: Discontinue at least 24 hr prior to scheduled surgery
- Reversible posterior leukoencephalopathy syndrome: Discontinue axitinib
- Moderate-to-severe proteinuria: Reduce dose or temporarily interrupt treatment
- Strong CYP3A4/5 inhibitors: Avoid coadministration if possible, if axitinib must be coadministered, decrease dose by ~50% and then adjust according to safety and tolerance; if strong CYP3A4/5 inhibitor is discontinued, may increase to prior axitinib dose after waiting 3-5 half-lives of the inhibitor
Renal & Hepatic Impairment
- No dedicated renal impairment trial has been conducted
- Based on population pharmacokinetic analyses, no significant difference in clearance observed in patients with pre-existing mild-to-severe renal impairment
- Mild (Child-Pugh A): No adjustment of initial dose is required
- Moderate (Child-Pugh B): Decrease initial dose by ~50%; subsequent doses can be increased or decreased based on individual safety and tolerability
- Severe (Child-Pugh C): Has not been studied
Administer twice daily approximately 12 hr apart
May be taken with or without food
Swallow whole with a glass of water; do not split, crush, or chew
If patient vomits or misses a dose, an additional dose should not be taken; the next prescribed dose should be taken at the usual time
<18 years: Safety and efficacy not established
In clinical trials, 34% of participants 65 years or older
No overall differences were observed in the safety or efficacy between elderly and younger patients
No dosage adjustment required in elderly patients
Serious - Use Alternative
Significant - Monitor Closely
Decreased appetite (34%)
Palmar-plantar erythrodysesthesia syndrome (27%)
Weight decreased (25%)
Mucosal inflammation (15%)
Abdominal pain (14%)
Extremity pain (13%)
Dry skin (10%)
Upper abdominal pain (8%)
Increased lipase (3%)
Pulmonary embolism (2%)
Rectal hemorrhage (2%)
Retinal vein occlusion/thrombosis (1%)
Reversible posterior leukoencephalopathy syndrome
Hypertension and hypertensive crisis reported in clinical trials, typically within the first month of treatment; blood pressure increases may appear as early as 4 days after initiating; blood pressure should be well controlled before starting therapy; dosage modification or discontinuation of treatment may be required (see Dosage Modification)
Although rare, arterial thromboembolic events (including deaths) reported during clinical trials
Venous thromboembolic events (eg, DVT, PE, retinal vein occlusion, retinal vein thrombosis) reported, including deaths
Hemorrhagic events (eg, cerebral hemorrhage, hematuria, hemoptysis, GI bleeding, melena) may occur
Rare occurrences of GI perforation and fistula formation reported
May cause thyroid dysfunction; monitor thyroid function before initiating and periodically throughout therapy
Stop treatment 24 hr before scheduled surgery
May cause proteinuria; monitor proteinuria before initiating and periodically throughout therapy
Elevated liver enzymes reported; monitor ALT, AST, and bilirubin
Moderate hepatic impairment requires dose reduction (see Dosage modification)
Coadministration with strong CYP3A4/5 inhibitors or inducers should be avoided if possible (see Dosage modifications)
Cardiac failure reported with axitinib use; monitor for signs or symptoms of cardiac failure throughout treatment; may require permanent discontinuation of axitinib
Pregnancy & Lactation
Pregnancy Category: D; can cause fetal harm when administered to a pregnant woman based on its mechanism of action; axitinib was teratogenic, embryotoxic, and fetotoxic in mice at exposures lower than human exposures at the recommended starting dose
Lactation: Unknown whether distributed in breast milk; because of the potential for serious adverse reactions in nursing infants from axitinib, a decision should be made whether to discontinue breast feeding or to discontinue the drug, taking into account the importance of the drug to the mother
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Multi-targeted tyrosine kinase inhibitor
Inhibits receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3
Peak Plasma Time: 2.5-4.1 hr
Peak Plasma Concentration: 27.8 ng/mL
AUC: 265 ng•h/mL
Protein Bound: >99% (mostly to albumin, moderately to alpha1-acid glycoprotein)
Vd: 160 L
Metabolized primarily by CYP3A4/5 and to a lesser degree by CYP1A2, CYP2C19, and UGT1A1
Metabolites: Plasma levels detected the N-glucuronide metabolite (50%), sulfoxide metabolite (20%), and 20% unchanged drug
Total body clearance: 38 L/h
Excretion: feces 41% (12% unchanged), urine 23% (as carboxylic acid and sulfoxide metabolites)
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