Axitinib

Axitinib is a prescription medication used for the treatment of renal cell carcinoma.

• Axitinib is available under the following different brand names: Inlyta

Adult dosage

Tablet

• 1mg
• 5mg

Renal Cell Carcinoma

Adult dosage

Monotherapy

• 5 mg orally twice daily  initially

Combination therapy with avelumab

• Axitinib 5 mg orally twice daily, plus
• Avelumab 800 mg IV every 2 weeks

Combination therapy with pembrolizumab

• Axitinib 5 mg orally twice daily, plus
• Pembrolizumab 200 mg IV every 3 weeks or 400 mg IV every 6 weeks

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of the Axitinib include:

• nausea, vomiting, diarrhea, constipation;
• rash, itching, redness, and peeling skin on the hands or feet;
• feeling weak or tired;
• increased blood pressure;
• decreased appetite, weight loss; or
• hoarse voice.

Serious side effects of the Axitinib include:

• chest pain or pressure, pain spreading to the jaw or shoulder, trouble breathing;
• sudden numbness or weakness, problems with vision or speech;
• headache, confusion, thinking problems, seizure (convulsions);
• a light-headed feeling;
• easy bruising, unusual bleeding, purple or red spots under the skin;
• heavy menstrual bleeding;
• any bleeding that will not stop;
• pink or brown urine;
• heart problems--swelling, rapid weight gain, feeling short of breath;
• signs of stomach bleeding--bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds; or
• signs of a thyroid problem--sudden weight gain or loss, feeling very weak or tired, muscle pain, feeling hot or cold, hair loss, hoarse or deepened voice.

Rare side effects of the Axitinib include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Axitinib has severe interactions with no other drugs.
• Axitinib has serious interactions with at least 77 other drugs.
• Axitinib has moderate interactions with at least 142 other drugs.
• Axitinib has minor interactions with the following drugs:
  • dexlansoprazole
  • famotidine
  • ibuprofen/famotidine

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Axitinib?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Axitinib?”

Cautions

• Hypertension and hypertensive crisis are 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 (e.g., DVT, PE, retinal vein occlusion, retinal vein thrombosis) were reported, including deaths
• Hemorrhagic events (e.g., 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 a 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
• Impaired wound healing
  • Impaired wound healing can occur in patients who receive drugs that inhibit the vascular endothelial growth factor (VEGF) signaling pathway
  • Therefore axitinib has the potential to adversely affect wound healing
  • Withhold for at least 2 days before elective surgery; do not administer for at least 2 weeks following major surgery and until adequate wound healing
  • Safety of resumption after resolution of wound healing complications has not been established
• Major adverse cardiovascular events (MACE)
  • Combination therapy with avelumab may cause severe and fatal cardiovascular events
  • Consider baseline and periodic evaluations of left ejection fraction; monitor signs and symptoms of cardiovascular events
  • Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia
  • Discontinue axitinib and avelumab for Grade 3-4 cardiovascular events
• In combination with avelumab or with pembrolizumab
  • Combination with avelumab or with pembrolizumab can cause hepatotoxicity with higher than expected frequencies of Grade 3 and 4 ALT and AST elevation; consider more frequent monitoring of liver enzymes as compared to when drugs are used as monotherapy
  • Withhold axitinib and avelumab for moderate (Grade 2) hepatotoxicity and permanently discontinue the combination for severe or life-threatening (Grade 3 or 4) hepatotoxicity; administer corticosteroids as needed
  • For elevated liver enzymes, interrupt axitinib and pembrolizumab and consider administering corticosteroids as needed.

Pregnancy and Lactation

• Based on the mechanism of action and findings from animal studies, the drug can cause fetal harm when administered to a pregnant woman; there are no available human data to inform drug-associated risk; in developmental toxicity studies in mice, axitinib was teratogenic, embryotoxic, and fetotoxic at maternal exposures that were lower than human exposures at recommended clinical dose
• When used in combination with avelumab or pembrolizumab, refer to the full prescribing information of avelumab or pembrolizumab for pregnancy information
• Contraception
  • Females: Therapy can cause fetal harm when administered to a pregnant woman; advise females of reproductive potential to use effective contraception during treatment and for 1 week after the last dose
  • Males: Based on findings in animal studies, advise males with female partners of reproductive potential to use effective contraception during treatment and for 1 week after the last dose
  • When is used in combination with avelumab or pembrolizumab, refer to the full prescribing information of avelumab or pembrolizumab for contraception information
• Infertility
  • Based on findings in animals, therapy may impair fertility in females and males of reproductive potential
• Lactation
  • There are no data on the presence of drugs in human milk or effects on the breastfed child or milk production; because of the potential for serious adverse reactions in a breastfed child, advise lactating women not to breastfeed during treatment and for 2 weeks after the final dose
  • When used in combination with avelumab or pembrolizumab, refer to the full prescribing information of avelumab or pembrolizumab for lactation information