• First-line treatment of advanced renal cell carcinoma (in combination with avelumab or pembrolizumab).
• Treatment of advanced renal cell carcinoma following failure of one other systemic therapy.

Contraindicated in:

• Untreated brain metastases
• Recent active GI bleeding
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• History of hypertension (must be well-controlled prior to/during therapy)
• Hypertension, dyslipidemia or diabetes (when using with avelumab)
• Moderate hepatic impairment (dose ↓ recommended)
• Surgery (discontinue 24 hr prior if possible)
• End-stage renal disease (CCr <15 mL/min)
• Rep: Woman of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: hypertension, AORTIC ANEURYSM, ARTERIAL/VENOUS THROMBOEMBOLIC EVENTS, CARDIAC DEATH (WITH AVELUMAB), MI (WITH AVELUMAB), HF.

Derm: dry skin, palmar-plantar erythrodysesthesia (hand-foot syndrome), rash, alopecia, erythema, wound healing impairment, pruritus.

EENT: dysphonia.

Endo: hypothyroidism.

F and E: ↓bicarbonate, hyperglycemia, hyperkalemia, hypernatremia, hypoalbuminemia, hypocalcemia, hypoglycemia, hyponatremia, hypophosphatemia, hypercalcemia.

GI: hepatotoxicity, abdominal pain, altered taste, ↓appetite/weight, constipation, diarrhea, nausea, ↑liver enzymes, stomatitis, burning mouth, GI PERFORATION/FISTULA.

GU: ↑serum creatinine, proteinuria.

Hemat: anemia, neutropenia, thrombocytopenia, BLEEDING.

MS: arthralgia, extremity pain.

Neuro: dysphoria, fatigue, headache, REVERSIBLE POSTERIOR LEUKOENCEPHALOPATHY SYNDROME (RPLS).

Resp: cough.

Drug-Drug:

• Strong CYP3A4/5 inhibitors, including atazanavir, clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, voriconazole may ↑ levels and the risk of toxicity; avoid concurrent use, if possible; if concurrent use cannot be avoided, select alternative agent. If none is acceptable, ↓ axitinib dose by 50%..
• Strong CYP3A4/5 inducers, including carbamazepine, dexamethasone, phenobarbital, phenytoin, rifabutin, rifampin, and rifapentin as well as moderate CYP3A4/5 inducers, including bosentan, efavirenz, etravirine, modafanil, and nafcillin may ↓ levels and effectiveness; avoid concurrent use, if possible.

Drug-Natural Products:

• St. John's wort may ↓ levels and should be avoided.

Drug-Food:

• Grapefruit/grapefruit juice may ↑ levels and should be avoided.

• Tablets : 1 mg; 5 mg;

First-Line Treatment of Advanced Renal Cell Carcinoma

• PO (Adults): In combination with avelumab — 5 mg twice daily, approximately 12 hr apart initially; after tolerating therapy for 2 consecutive wk (i.e. no adverse reactions Grade >2, remaining normotensive, and are not receiving antihypertensive medications), may ↑ to 7 mg twice daily; after tolerating adjusted dose for 2 consecutive wk (using same criteria), may ↑ to 10 mg twice daily. Continue treatment until unacceptable toxicity or disease progression. In combination with pembrolizumab — 5 mg twice daily, approximately 12 hr apart initially; after tolerating therapy for 6 wk (i.e. no adverse reactions Grade >2, remaining normotensive, and are not receiving antihypertensive medications), may ↑ to 7 mg twice daily; after tolerating adjusted dose for 6 consecutive wk (using same criteria), may ↑ to 10 mg twice daily. Continue treatment until unacceptable toxicity or disease progression. Concurrent use of strong CYP3A4/5 inhibitors — ↓dose by approximately 50%.

Second-Line Treatment of Advanced Renal Cell Carcinoma

• PO (Adults): 5 mg twice daily, approximately 12 hr apart initially; after tolerating therapy for 2 consecutive wk (i.e. no adverse reactions Grade >2, remaining normotensive, and are not receiving antihypertensive medications), may ↑ to 7 mg twice daily; after tolerating adjusted dose for 2 consecutive wk (using same criteria), may ↑ to 10 mg twice daily. Continue treatment until unacceptable toxicity or disease progression.Concurrent use of strong CYP3A4/5 inhibitors — ↓dose by approximately 50%.

Inlyta

• Inhibits tyrosine kinases on various receptors including vascular endothelial growth factor receptors which may be involved in tumor angiogenesis/growth and cancer progression.

• Inhibited tumor growth with decreased disease progression.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: Well absorbed (58%) following oral administration.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized by the CYP3A4/5 enzyme system, some metabolism by CYP2C19 and UGT1A1 systems. 41% eliminated in feces (12% as unchanged drug); 23% eliminated in urine as metabolites.

Half-life: 2.5–6.1 hr.

(blood levels)

† Decreased progression of disease may last up to 18 mo.

• Instruct patient to take axitinib as directed. If a dose is vomited or missed, omit dose and take next dose at regular time; do not double doses. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
• Advise patient to avoid drinking grapefruit juice or eating grapefruit during axitinib therapy.
• Advise patient to notify health care professional of therapy prior to treatment, dental procedure, or surgery. Axitinib therapy should be interrupted in patients undergoing major surgery; hold dose for at least 2 days before surgery and for at least 2 wks after surgery and until adequate wound healing occurs.
• May cause bleeding or blood clots. Advise patient to notify health care professional immediately if unexpected bleeding or bleeding that lasts a long time; unusual bleeding of gums; heavier than normal menstrual bleeding; severe or uncontrollable bleeding; pink or brown urine; red or black stools; vomiting blood or dark “coffee ground” looking; unexpected pain, swelling, or joint pain; headaches; feeling dizzy; or weakness occur or if chest pain or pressure; pain in arms, back, neck or jaw; shortness of breath; numbness or weakness on one side of body; difficulty talking; headache; or vision changes occur.
• May cause stomach tear or intestinal wall perforation. Caution patient to notify health care professional if severe abdominal pain, vomiting blood, or red or black stools occur.
• Advise patient to notify health care professional promptly if signs and symptoms of reversible posterior leukoencephalopathy syndrome (RPLS) (headache, seizures, weakness, confusion, high BP, blindness or change in vision, problems thinking), thyroid problems (worsening or persistent tiredness, feeling hot or cold, voice deepens, weight gain or weight loss, hair loss, muscle cramps and aches), or HF (tiredness, swelling abdomen, legs or ankles, shortness of breath, protruding neck veins) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's Wort.
• Rep: May cause fetal harm. Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during therapy and for 1 wk after last dose. Advise female patients to avoid breastfeeding during therapy and for 2 wk after last dose. May impair fertility in male and female patients.

AX-i-ti-nib

NDC Code^*

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-0145- INLYTA
    • 0069-0145-01- 180 TABLET, FILM COATED in 1 BOTTLE (0069-0145-01)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-0151- INLYTA
    • 0069-0151-11- 60 TABLET, FILM COATED in 1 BOTTLE (0069-0151-11)

• 63539- U.S. Pharmaceuticals
  • 63539-026- INLYTA
    • 63539-026-01- 90 TABLET, FILM COATED in 1 BOTTLE (63539-026-01)

• 63539- U.S. Pharmaceuticals
  • 63539-044- INLYTA
    • 63539-044-01- 60 TABLET, FILM COATED in 1 BOTTLE (63539-044-01)

• 63539- U.S. Pharmaceuticals
  • 63539-044- INLYTA
    • 63539-044-02- 30 TABLET, FILM COATED in 1 BOTTLE (63539-044-02)