Axitinib (Monograph)

Brand name: Inlyta
Drug class: Antineoplastic Agents

Medically reviewed by Drugs.com on Dec 14, 2023. Written by ASHP.

Introduction

Antineoplastic agent; a second-generation tyrosine kinase inhibitor that selectively inhibits vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3.

Uses for Axitinib

Renal Cell Carcinoma

In combination with avelumab for the first-line treatment of advanced renal cell carcinoma.

In combination with pembrolizumab for the first-line treatment of advanced renal cell carcinoma.

Monotherapy for the treatment of advanced renal cell carcinoma following failure of one prior systemic therapy.

Has been used as monotherapy for the first-line treatment of metastatic renal cell carcinoma^{† [off-label]} .

Axitinib Dosage and Administration

General

Pretreatment Screening

• Assess baseline ALT, AST, and bilirubin concentrations.

• BP should be adequately controlled prior to initiating therapy. Do not initiate in patients with uncontrolled hypertension.

• Consider assessing left ventricular ejection fraction (LVEF) at baseline.

• Perform thyroid function tests at baseline; treat hypothyroidism and hyperthyroidism according to standard medical practice to maintain a euthyroid state.

• Assess for proteinuria.

• Verify pregnancy status of females of reproductive potential prior to initiation of therapy.

Patient Monitoring

• Monitor ALT, AST, and bilirubin concentrations periodically during therapy. When axitinib is used in combination with avelumab or pembrolizumab, consider more frequent monitoring.

• Consider periodically monitoring LVEF.

• Monitor for signs and symptoms of cardiac failure periodically during therapy.

• Monitor for manifestations of GI perforation or fistula.

• Monitor BP regularly.

• Monitor thyroid function periodically during therapy; treat hypothyroidism and hyperthyroidism according to standard medical practice to maintain a euthyroid state.

• Monitor for proteinuria periodically during therapy.

Dispensing and Administration Precautions

• Based on the Institute for Safe Medication Practices (ISMP), axitinib is a high-alert medication that has a heightened risk of causing significant patient harm when used in error.

Other General Considerations

• Clinicians should consult published protocols for information on the dosage, method of administration, and administration sequence of other antineoplastic agents used in combination regimens with axitinib.

• Withhold axitinib for ≥2 days prior to elective surgery and for ≥2 weeks following major surgery and until adequate wound healing occurs.

Administration

Oral Administration

Administer orally twice daily (in doses given approximately 12 hours apart) without regard to meals.

Swallow tablets whole with a full glass of water; do not crush or split.

If a dose is missed or vomited, do not double the dosage or take extra doses. Take the next dose at the regularly scheduled time.

NG Tube

Prepare each dose just prior to administration.

In clinical trials, axitinib has been given by NG tube after dissolving the tablets (without crushing) in 15 mL of USP-grade water in an amber-colored syringe; use of tap or bottled water was avoided. The NG tube was flushed with USP-grade water prior to and following administration of the dose. Do not expose prepared NG dose to direct light.

Avoid contact of prepared dose with skin or mucous membranes. If such contact occurs, flush affected area with water.

Dosage

Adults

Renal Cell Carcinoma

First-line Therapy: Combination Therapy with Avelumab

Oral

Initially, 5 mg twice daily (12 hours apart) in combination with avelumab (800 mg by IV infusion over 60 minutes every 2 weeks) until disease progression or unacceptable toxicity. In principal efficacy study, median duration of axitinib therapy was 9 months.

When axitinib is used in combination with avelumab, dose escalation of axitinib above the initial 5 mg dose may be considered at intervals of 2 weeks or longer. Consult the Full Prescribing Information for recommended avelumab dosing.

In patients who tolerate initial dosage for at least 2 consecutive weeks (no adverse effects greater than grade 2, normotensive, no antihypertensive use), may increase axitinib dosage to 7 mg twice daily, and then may increase further to 10 mg twice daily using the same criteria.

First-line Therapy: Combination Therapy with Pembrolizumab

Oral

Initially, 5 mg twice daily (12 hours apart) in combination with pembrolizumab IV (200 mg every 3 weeks or 400 mg every 6 weeks administered as an IV infusion over 30 minutes) until disease progression or unacceptable toxicity. In principal efficacy study, median duration of axitinib therapy was 10.4 months.

When axitinib is used in combination with pembrolizumab, dose escalation of axitinib above the initial 5 mg dose may be considered at intervals of 6 weeks or longer. Consult the Full Prescribing Information for recommended pembrolizumab dosing.

In patients who tolerate initial dosage for at least 2 consecutive weeks (no adverse effects greater than grade 2, normotensive, no antihypertensive use), may increase axitinib dosage to 7 mg twice daily, and then may increase further to 10 mg twice daily using the same criteria.

Second-line Therapy: Monotherapy

Oral

Initially, 5 mg twice daily (12 hours apart). In principal efficacy study, therapy was continued until disease progression or unacceptable toxicity occurred; median duration of therapy was 6.4 months.

In patients who tolerate initial dosage for at least 2 consecutive weeks (no adverse effects greater than grade 2, normotensive, no antihypertensive use), may increase dosage to 7 mg twice daily, and then may increase further to 10 mg twice daily using the same criteria.

Dosage Modification for Toxicity

Oral

Adjust dosage based on individual safety and tolerability. Recommended dosage reductions for adverse reactions are provided in Table 1.

Hypertension

Oral

If systolic blood pressure (SBP) >150 mmHg or diastolic blood pressure (DBP) >100 mmHg despite antihypertensive therapy, reduce dosage by one dosage level. If SBP >160 mmHg or DBP >105 mmHg, withhold axitinib until BP <150/100 mm Hg; then resume at a reduced dosage.

For grade 4 hypertension or hypertensive crisis, permanently discontinue axitinib.

Hemorrhage

Oral

For grade 3 or 4 hemorrhage, withhold axitinib until resolution to grade 0 or 1 or baseline. Resume at either a reduced dosage or discontinue axitinib, depending on the severity and persistence of the adverse reaction.

Cardiac Failure

Oral

For asymptomatic cardiomyopathy (left ventricular ejection fraction >20% but <50% below baseline or below the lower limit of normal if baseline was not obtained), withhold axitinib until resolution to grade 0 or 1 or baseline; then resume at a reduced dosage.

For clinically manifested congestive heart failure, discontinue axitinib permanently.

Impaired Wound Healing

Oral

The safety of resumption of axitinib after resolution of any grade of wound healing has not been established. For any grade, either resume axitinib at a reduced dosage or discontinue, depending on the severity and persistence of the adverse reaction.

Reversible Posterior Leukoencephalopathy Syndrome

Oral

For any grade of reversible posterior leukoencephalopathy syndrome, discontinue axitinib permanently.

Proteinuria

Oral

For patients with ≥2 grams of proteinuria over 24 hours, withhold axitinib until resolution to <2 grams of proteinuria over 24 hours. Then resume axitinib at a reduced dosage.

Other Adverse Reactions

Oral

For any other grade 3 adverse reactions, reduce dosage by one level. For any other grade 4 reactions, withhold axitinib until resolution to grade 2, then resume at a reduced dosage.

Liver Enzyme Elevations

Oral

Combination therapy with avelumab or pembrolizumab: If elevations in ALT or AST concentrations are ≥3 times the ULN, but <10 times the ULN without concurrent total bilirubin concentration at least 2 times the ULN, withhold both axitinib and avelumab or pembrolizumab until hepatotoxicity resolves to grade 1 or less. Consider rechallenge with axitinib and/or avelumab or pembrolizumab; if rechallenging with axitinib, consider dosage reduction per Table 1. If ALT or AST increases to >3 times the ULN with concurrent total bilirubin at least 2 times the ULN or ALT or AST ≥10 times the ULN, permanently discontinue both axitinib and avelumab or pembrolizumab.

Diarrhea

Oral

Combination therapy with avelumab or pembrolizumab: If grade 1 or 2 diarrhea occurs, initiate treatment with symptomatic medications. For grade 3 diarrhea, interrupt axitinib and initiate symptomatic medications. If diarrhea is controlled, axitinib may be resumed at either the same dosage or reduced by one dosage level. For grade 4 diarrhea, withhold axitinib until resolution to grade <2, then restart axitinib at a dosage reduced by one level.

Major Adverse Cardiac Events

Oral

Combination therapy with avelumab: For grade 3 or 4 major adverse cardiac events (MACE), permanently discontinue.

Concomitant Use with Drugs Affecting Hepatic Microsomal Enzymes

Oral

Avoid concomitant use of axitinib with drugs that are potent inhibitors of CYP3A4 or 3A5. If concomitant use cannot be avoided, reduce axitinib dosage by approximately 50% (i.e., one half). Subsequent increases or decreases in axitinib dosage may be made based on individual safety and tolerability. If concurrent administration of the potent inhibitor is discontinued, return axitinib dosage (after 3–5 elimination half-lives of the CYP3A4/5 inhibitor) to the dosage used prior to initiation of the potent CYP3A4/5 inhibitor.

Special Populations

Hepatic Impairment

Mild preexisting hepatic impairment (Child-Pugh class A): No initial dosage adjustment required.

Moderate preexisting hepatic impairment (Child-Pugh class B): Reduce initial dosage by approximately 50% (i.e., to 2.5 mg twice daily); may increase or decrease subsequent dosages based on individual safety and tolerability.

Severe hepatic impairment (Child-Pugh class C): Not studied.

Renal Impairment

Mild to severe preexisting renal impairment (Cl_cr 15–89 mL/minute): No initial dosage adjustment required.

End-stage renal disease (Cl_cr <15 mL/minute): Use with caution.

Geriatric Use

No dosage adjustment required.

Related/similar drugs

Keytruda, pembrolizumab, Avastin, bevacizumab, nivolumab, Afinitor

Cautions for Axitinib

Contraindications

• None.

Warnings/Precautions

Hypertension and Hypertensive Crisis

Hypertension and hypertensive crisis reported in 40% (grade 3 or 4 in 16%) and <1% of axitinib-treated patients, respectively, in the primary efficacy study. Median time to onset of hypertension is within the first month; BP increases have been observed as early as 4 days after initiating therapy.

Control BP well prior to initiating axitinib therapy. Monitor for hypertension during therapy and treat as needed with standard antihypertensive therapy. Temporarily interrupt axitinib treatment and then reduce the dosage or permanently discontinue therapy depending on severity of hypertension. Permanently discontinue therapy if grade 4 hypertension or hypertensive crisis occurs.

Arterial Thromboembolic Events

Arterial thromboembolic events (e.g., TIA, cerebrovascular accident, MI, retinal artery occlusion), including fatal cases, reported. Not evaluated in patients who had an arterial thromboembolic event within the past 12 months.

Use with caution in patients who are at risk for, or have a history of, arterial thromboembolic events. Permanently discontinue if an arterial thromboembolic event occurs.

Venous Thromboembolic Events

Venous thromboembolic events (VTE; e.g., PE, DVT, retinal vein occlusion, retinal vein thrombosis), including fatal cases, reported. Not evaluated in patients who had VTE within the past 6 months.

Monitor patients for signs and symptoms of VTE and PE. If symptoms occur, temporarily interrupt therapy and then resume at the same dose or discontinue permanently based on severity of the event.

Hemorrhage

Hemorrhagic events, including fatal cases, reported. Grade 3 or 4 hemorrhagic events have included cerebral hemorrhage, hematuria, hemoptysis, lower GI hemorrhage, and melena.

Not evaluated in patients with evidence of untreated brain metastasis or recent, active GI bleeding; avoid use in such patients. If hemorrhagic events occur, withhold axitinib therapy and then reduce the dosage or discontinue based on severity and persistence of hemorrhage.

Cardiac Failure

Cardiac failure, including fatal cases, reported.

Monitor for signs or symptoms of cardiac failure. Reduction of dosage, interuption of therapy, or permanent discontinuance of axitinib may be necessary.

GI Perforation and Fistula Formation

GI perforation (including one death) and fistula formation reported in axitinib-treated patients in clinical trials.

Use with caution in patients at risk for GI perforation or fistula. Monitor for symptoms of GI perforation or fistula formation periodically during treatment.

Thyroid Dysfunction

Thyroid dysfunction (hypothyroidism or hyperthyroidism) requiring thyroid hormone replacement therapy reported with certain tyrosine kinase inhibitors, including axitinib.

Assess baseline thyroid function prior to initiation of therapy and then monitor periodically during treatment. Treat hypothyroidism and hyperthyroidism according to standard medical practice to maintain a euthyroid state.

Wound Healing Complications

VEGFR inhibitors, such as axitinib, may impair wound healing.

Discontinue axitinib ≥2 days prior to elective surgery and for ≥2 weeks following major surgery. Decision to resume therapy postoperatively should be based on clinical assessment of adequacy of wound healing. Resume at a reduced dosage or discontinue based on severity and persistence of the impaired wound healing. Safety of resuming axitinib after resolution of wound healing complications has not been established.

Reversible Posterior Leukoencephalopathy Syndrome

Reversible posterior leukoencephalopathy syndrome (RPLS), a neurologic disorder, reported in one axitinib-treated patient in the primary efficacy study; 2 additional cases reported in other clinical trials. May manifest with headache, seizures, lethargy, confusion, blindness, and other visual and neurologic disturbances; mild to severe hypertension also may occur. Magnetic resonance imaging (MRI) is necessary to confirm diagnosis.

In patients who develop signs or symptoms of RPLS, permanently discontinue axitinib. Safety of reinitiating axitinib in patients previously experiencing RPLS not known.

Proteinuria

Proteinuria reported.

Monitor for proteinuria prior to initiation of, and periodically during, therapy. For moderate to severe proteinuria, withhold therapy, then reduce dosage.

Hepatotoxicity

ALT elevations, sometimes severe, reported in 22% of patients receiving axitinib monotherapy in the primary efficacy study. Monitor serum aminotransferase (ALT and AST) and bilirubin concentrations prior to initiation of, and periodically during, axitinib monotherapy. More frequent monitoring of liver tests should be considered when axitinib is used in combination with avelumab or pembrolizumab. For elevated liver enzymes, interrupt or permanently discontinue axitinib and avelumab or pembrolizumab, and administer corticosteroids as needed.

Axitinib in combination with avelumab or pembrolizumab can cause hepatotoxicity with higher than expected frequencies of grade 3 or 4 ALT or AST elevations.

Major Adverse Cardiovascular Events

Cardiovascular events, sometimes severe and fatal, reported when used in combination with avelumab.

Consider assessing LVEF at baseline and periodically. Monitor for signs and symptoms of cardiovascular events, and optimize management of cardiovascular risk factors (e.g., hypertension, diabetes, dyslipidemia). Permanently discontinue axitinib and avelumab if grade 3 or 4 cardiovascular events occur.

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm; teratogenicity, embryotoxicity, and fetotoxicity demonstrated in animals.

Avoid pregnancy during therapy. If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.

Combination Therapy

When axitinib is used in combination with avelumab or pembrolizumab, consider the usual cautions, precautions, and contraindications associated with avelumab and pembrolizumab in addition to those associated with axitinib.

Infertility

Based on findings in animals, axitinib may impair fertility in females and males of reproductive potential.

Specific Populations

Pregnancy

May cause fetal harm.

Lactation

Not known whether axitinib is distributed into human milk. Do not breast-feed during therapy and for 2 weeks after the last dose.

Females and Males of Reproductive Potential

Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during treatment with axitinib and for 1 week after the last dose.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age. Pharmacokinetics of axitinib in pediatric patients not studied.

Thickened growth plates in bone and abnormalities in growing incisor teeth observed in juvenile animals receiving oral axitinib for ≥1 month; other toxicities of potential concern not evaluated in juvenile animal studies.

Geriatric Use

No overall differences in safety and efficacy relative to younger patients, but increased sensitivity cannot be ruled out.

Hepatic Impairment

Systemic exposure not affected by mild hepatic impairment (Child-Pugh class A).

Increased systemic exposure in patients with moderate hepatic impairment (Child-Pugh class B); initial dosage reduction recommended.

Not studied in patients with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

Mild to severe renal impairment unlikely to substantially affect pharmacokinetics (e.g., clearance) of axitinib; no initial dosage adjustment necessary.

Limited data in patients with end-stage renal disease; use with caution.

Common Adverse Effects

Combination therapy with avelumab for the first-line treatment of advanced renal cell carcinoma (≥20%): Diarrhea, fatigue, hypertension, musculoskeletal pain, nausea, mucositis, palmar-plantar erythrodysesthesia (hand-foot syndrome), dysphonia, decreased appetite, hypothyroidism, rash, hepatotoxicity, cough, dyspnea, abdominal pain, headache.

Combination therapy with pembrolizumab for the first-line treatment of advanced renal cell carcinoma (≥20%): Diarrhea, fatigue/asthenia, hypertension, hypothyroidism, decreased appetite, hepatotoxicity, palmar-plantar erythrodysesthesia (hand-foot syndrome), nausea, stomatitis/mucosal inflammation, dysphonia, rash, cough, constipation.

Monotherapy for the second-line treatment of advanced renal cell carcinoma (≥20%): Diarrhea, hypertension, fatigue, decreased appetite, nausea, dysphonia, palmar-plantar erythrodysesthesia (hand-foot syndrome), weight loss, vomiting, asthenia, constipation.

Drug Interactions

Metabolized principally by CYP3A4/5 and, to a lesser extent, by CYP1A2, CYP2C19, and uridine diphosphate-glucurosyltransferase (UGT) 1A1.

Has potential to inhibit CYP isoenzymes 1A2 and 2C8 in vitro.

In vitro studies indicate that axitinib does not inhibit CYP2A6, 2C9, 2C19, 2D6, 2E1, 3A4/5, or UGT1A1 at therapeutic plasma concentrations.

Inhibition of P-glycoprotein (P-gp) not expected at therapeutic plasma concentrations.

Axitinib does not induce CYP1A1, CYP1A2, or CYP3A4/5 in human hepatocytes in vitro.

Drugs and Foods Affecting Hepatic Microsomal Enzymes

Potent CYP3A4/5 inhibitors: Possible pharmacokinetic interaction (increased plasma concentrations of axitinib). Avoid concomitant use; select an alternative agent with no or minimal enzyme inhibition potential. If concomitant therapy cannot be avoided, reduce axitinib dosage by approximately 50%; may increase or decrease subsequent dosages based on individual safety and tolerability. If the potent CYP3A4/5 inhibitor is discontinued, resume axitinib (after 3–5 elimination half-lives of the CYP3A4/5 inhibitor) at the dosage used prior to initiation of the potent CYP3A4/5 inhibitor.

CYP3A4/5 inducers: Possible pharmacokinetic interaction (decreased plasma concentrations of axitinib). Avoid concomitant use of potent CYP3A4/5 inducers; select an alternative agent with no or minimal enzyme induction potential. Also avoid concomitant use of moderate CYP3A4/5 inducers if possible.

Drugs Metabolized by Hepatic Microsomal Enzymes

Substrates of CYP isoenzymes 1A2 or 2C8: Clinically important pharmacokinetic interactions unlikely.

Drugs Affecting Gastric Acidity

Pharmacokinetic interaction (possible decreased solubility of axitinib) with drugs that increase pH of upper GI tract. Clinically important pharmacokinetic interaction unlikely.

Specific Drugs and Foods

Axitinib Pharmacokinetics

Absorption

Bioavailability

Readily absorbed following oral administration; peak plasma concentrations are attained within 2.5–4.1 hours.

Steady-state concentrations expected within 2–3 days.

Mean absolute bioavailability after single-dose oral administration is 58%.

Use in combination with avelumab or pembrolizumab does not appear to result in clinically relevant changes in exposure to axitinib, avelumab, or pembrolizumab compared to use of each drug alone.

Food

Administration with a high-fat, high-calorie meal increased AUC by 19% compared with overnight fasting; administration with a moderate fat meal decreased AUC by 10%.

Special Populations

Mild hepatic impairment (Child-Pugh class A) does not substantially affect systemic exposure. Moderate hepatic impairment (Child-Pugh class B) increases systemic exposure. Not studied in severe hepatic impairment (Child-Pugh class C).

Distribution

Extent

Not known whether distributed into human milk.

Plasma Protein Binding

>99% (preferentially to albumin and moderately to α₁-acid glycoprotein).

Elimination

Metabolism

Predominantly metabolized in liver by CYP3A4/5 and, to a lesser extent, by CYP1A2, CYP2C19, and UGT1A1.

Use in combination with avelumab does not appear to result in clinically relevant changes in clearance of avelumab compared to use of each agent alone.

Elimination Route

Primarily eliminated in feces (approximately 41%), mainly as unchanged drug, and in urine (approximately 23%), mainly as carboxylic acid and sulfoxide metabolites.

Half-life

2.5–6.1 hours.

Special Populations

Mild to severe renal impairment did not substantially alter clearance of axitinib in a population pharmacokinetic analysis. Data in end-stage renal disease very limited.

Stability

Storage

Oral

Tablets

20–25°C; excursions permitted between 15–30ºC.

Actions

• Potently and selectively inhibits receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3. VEGFR receptors are involved in tumor angiogenesis, tumor growth, and metastatic spread.

• Axitinib is 50–450 times more potent at blocking VEGFR receptors compared with first-generation VEGFR inhibitors (i.e., sorafenib, sunitinib, pazopanib).

• Compared with first-generation VEGFR inhibitors, axitinib has relatively less potent or minimal inhibitory activity against other receptor kinases, including platelet-derived growth factor beta receptors (e.g., PDGFR-β), stem cell factor receptor (e.g., c-Kit), colony stimulating factor receptor type 1 (CSF-1R), fms-like tyrosine kinase 3 (Flt-3), fibroblast growth factor receptor (FGFR)-1, ret proto-oncogene (RET), epidermal growth factor receptor (EGFR), and met proto-oncogene encoding hepatocyte growth factor (c-MET).

• Inhibits VEGF-mediated endothelial cell proliferation and survival in vitro and in mice.

• Inhibits tumor growth and VEGFR-2 phosphorylation in mice.

Advice to Patients

• Importance of reading the manufacturer’s patient information prior to beginning axitinib therapy and rereading it each time the prescription is refilled.

• If a dose of axitinib is missed or vomited, take the next dose at the regularly scheduled time. Do not take more than one dose at a time.

• Importance of swallowing axitinib tablets whole with a full glass of water. Avoid grapefruit or grapefruit juice while taking the drug.

• Risk of hypertension. Importance of monitoring blood pressure regularly during treatment.

• Risk of arterial and venous thromboembolic events. Importance of getting emergency help and contacting clinician if any symptoms suggestive of a thromboembolic event occur (e.g., chest pain or pressure, shortness of breath, unilateral numbness or weakness, difficulty talking, headache, vision changes, or arm, back, neck, or jaw pain).

• Risk of bleeding. Importance of promptly informing clinician of any episodes of bleeding (e.g., unusual bleeding, bruising).

• Increased risk of cardiac failure. Importance of advising patients of signs and symptoms of cardiac failure.

• Risk of GI disorders. Importance of advising patients that GI disorders such as diarrhea, nausea, vomiting, and constipation may develop and to seek immediate medical attention if symptoms of GI perforation or fistula (e.g., persistent or severe abdominal pain, vomiting blood, red or black stools) occur.

• Risk of thyroid dysfunction. Importance of informing clinician if symptoms of thyroid dysfunction occur (e.g., persistent or worsening fatigue, deepened voice, hair loss, weight gain or loss, myalgia, feeling hot or cold).

• Risk of wound healing complications. Importance of informing clinician of any scheduled surgery or wounds that do not heal.

• Risk of reversible posterior leukoencephalopathy syndrome (RPLS). Importance of immediately informing clinician if headache, seizures, weakness, lethargy, confusion, hypertension, blindness, or other visual and neurologic disturbances occur.

• Risk of fetal harm and fetal loss. Importance of women informing their clinicians if they are or plan to become pregnant. Importance for men who are taking axitinib to inform their clinician if their female partner becomes pregnant. Necessity of advising women and men receiving axitinib to use effective methods of contraception during axitinib therapy and for 1 week after the last dose. Necessity of advising women to avoid pregnancy during therapy. Advise women of the potential risk to the fetus (e.g., birth defects) and/or the potential risk for loss of the pregnancy.

• Inform patients of the signs and symptoms of hepatotoxicity. Advise patients to contact their healthcare provider immediately for signs or symptoms of hepatotoxicity.

• Risk of infertility. Importance of informing patients of the potential risk of infertility.

• Importance of advising women to avoid breast-feeding while receiving axitinib and for 2 weeks after the last dose.

• Risk of proteinuria and importance of monitoring for proteinuria before and during therapy.

• Risk of hepatotoxicity; importance of liver function test monitoring during therapy.

• Risk of major adverse cardiovascular effects. Importance of advising patients receiving axitinib in combination with avelumab to report signs or symptoms of cardiovascular events (e.g., chest discomfort, dyspnea, peripheral edema).

• Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements (e.g., St. John’s wort), as well as any concomitant illnesses (e.g., hypertension or other cardiovascular disease, cerebrovascular disease, thyroid disease, hepatic disease, bleeding disorders).

• Importance of informing patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Axitinib can only be obtained through designated specialty pharmacies. Contact manufacturer for specific availability information.

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Frequently asked questions

• How are Inlyta and Keytruda used in kidney cancer?

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