Axitinib
Axitinib is a kinase inhibitor (a targeted cancer medicine) used to treat advanced renal cell carcinoma (kidney cancer), either with another cancer drug as first treatment or alone after one earlier treatment has failed.
🧬 Where this information comes from Click to expand
The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 2 clinical label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →
Axitinib (Inlyta), on the U.S. market since about 2012, is a specialist kidney cancer medicine that blocks VEGF receptors, which tumors need to grow new blood vessels; for advanced renal cell carcinoma it is paired with the immunotherapy avelumab or pembrolizumab as a first treatment, or used alone after one earlier therapy fails. Most people can stay on it with dose adjustments, though diarrhea, tiredness, a hoarse voice and sore, red palms and soles (hand-foot syndrome) are common. The one to watch is blood pressure, which often rises early, so check it at home and report a severe headache, confusion or vision changes right away.
Clinical pearls
- Avoid grapefruit and St. John's wort, and have new prescriptions checked, since ketoconazole, rifampin and carbamazepine change axitinib levels.
- Axitinib is stopped at least 2 days before planned surgery and restarted only after wounds heal, so tell any surgeon early.
- Expect regular thyroid, liver and urine protein tests, since an underactive thyroid is common and usually treatable with thyroid hormone.
- Both women and men with female partners should use effective contraception during treatment and for 1 week after the last dose.
Patient information guide A plain-language walkthrough of Axitinib, written from its FDA label.
What Axitinib is used for
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Axitinib is used for advanced renal cell carcinoma (kidney cancer). Inlyta is the brand supplied here.
- Inlyta with avelumab: first-line treatment of advanced renal cell carcinoma.
- Inlyta with pembrolizumab: first-line treatment of advanced renal cell carcinoma.
- Inlyta as a single agent: advanced renal cell carcinoma after failure of one prior systemic therapy.
How Axitinib works
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Axitinib is a kinase inhibitor. It blocks VEGF receptors (VEGFR-1, -2 and -3), which are involved in forming new blood vessels that feed tumors.
By blocking these signals, it limits tumor growth. In lab and mouse studies it slowed tumor growth.
Axitinib dosage
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Inlyta tablets are taken by mouth twice a day, about 12 hours apart, with or without food.
- Swallow tablets whole with a full glass of water.
- If you miss a dose or vomit, do not take an extra dose. Take the next dose at the usual time.
- Your prescriber may raise or lower your dose based on how well you tolerate it.
- When used with avelumab or pembrolizumab, those drugs are given by IV infusion.
Dosing details from the FDA-approved label
From the Axitinib prescribing information (“Dosage and Administration”). Doses are set by your prescriber for your product, condition, kidney function and age — never change a dose on your own.
- First-Line Advanced RCC: INLYTA in combination with avelumab
- 5 mg orally twice daily (12 hours apart) with or without food, with avelumab 800 mg as an intravenous infusion over 60 minutes every 2 weeks until disease progression or unacceptable toxicity
- Dose escalation above the initial 5 mg dose may be considered at intervals of two weeks or longer
- First-Line Advanced RCC: INLYTA in combination with pembrolizumab
- 5 mg orally twice daily (12 hours apart) with or without food, with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks as an intravenous infusion over 30 minutes until disease progression or unacceptable toxicity
- Dose escalation above the initial 5 mg dose may be considered at intervals of six weeks or longer
- Second-Line Advanced RCC: INLYTA as a single agent
- Recommended starting oral dose is 5 mg twice daily, approximately 12 hours apart with or without food
- Dose increases: first 7 mg twice daily, second 10 mg twice daily; reductions: 3 mg twice daily, then 2 mg twice daily
- Patients taking a strong CYP3A4/5 inhibitor
- Decrease the INLYTA dose by approximately half
- Patients with moderate hepatic impairment
- Decrease the starting dose by approximately half
Read the label’s full dosing text
2 DOSAGE AND ADMINISTRATION • INLYTA 5 mg orally twice daily with avelumab 800 mg every 2 weeks. ( 2.1 ) • INLYTA 5 mg orally twice daily with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks. ( 2.1 ) • INLYTA as a single agent the starting dose is 5 mg orally twice daily. ( 2.1 ) • Dose adjustments can be made based on individual safety and tolerability. ( 2.2 ) • Administer INLYTA dose approximately 12 hours apart with or without food. ( 2.1 ) • INLYTA should be swallowed whole with a glass of water. ( 2.1 ) • See Full Prescribing Information for dosage modifications for adverse reactions. ( 2.2 ) • If a strong CYP3A4/5 inhibitor is required, decrease the INLYTA dose by approximately half. ( 2.2 ) • For patients with moderate hepatic impairment, decrease the starting dose by approximately half. ( 2.2 ) 2.1 Recommended Dosing First-Line Advanced RCC INLYTA in Combination with Avelumab The recommended starting dosage of INLYTA is 5 mg orally taken twice daily (12 hours apart) with or without food in combination with avelumab 800 mg administered as an intravenous infusion over 60 minutes every 2 weeks until disease progression or unacceptable toxicity. When INLYTA is used in combination with avelumab, dose escalation of INLYTA above the initial 5 mg dose may be considered at intervals of two weeks or longer. Review the Full Prescribing Information for recommended avelumab dosing information. INLYTA in Combination with Pembrolizumab The recommended starting dosage of INLYTA is 5 mg orally twice daily (12 hours apart) with or without food in combination with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks administered as an intravenous infusion over 30 minutes until disease progression or unacceptable toxicity. When INLYTA is used in combination with pembrolizumab, dose escalation of INLYTA above the initial 5 mg dose may be considered at intervals of six weeks or longer. Review the Full Prescribing Information for recommended pembrolizumab dosing information. Second-Line Advanced RCC When INLYTA is used as a single agent, the recommended starting oral dose is 5 mg twice daily. Administer INLYTA doses approximately 12 hours apart with or without food. Important Administration Instructions Advise patients to swallow INLYTA whole with a full glass of water. If the patient vomits or misses a dose, an additional dose should not be taken.
Excerpted — the section continues on the label. Read the full Dosage and Administration section on DailyMed →
Axitinib side effects
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Common side effects depend a bit on whether Inlyta is used alone or with avelumab or pembrolizumab. They include:
Common side effects
- Diarrhea
- Fatigue or weakness
- High blood pressure
- Decreased appetite
- Nausea
- Hoarse or weak voice (dysphonia)
- Hand-foot syndrome (redness, soreness on palms and soles)
- Underactive thyroid (hypothyroidism)
- Liver test changes or liver problems (more with combinations)
- Constipation or weight loss (single agent)
When to get medical help
- Call your doctor right away for signs of bleeding, especially if serious or lasting.
- Get urgent help for signs of a blood clot or stroke, such as chest pain, sudden weakness, or trouble speaking.
- Seek help for severe high blood pressure, including a hypertensive crisis.
- Tell your doctor about swelling, shortness of breath or other signs of heart failure.
- Report severe stomach pain, which may signal a tear or abnormal connection (perforation or fistula) in the gut.
- Report severe headache, seizures, confusion or vision changes, which can be signs of RPLS (a brain swelling condition).
- Tell your doctor about signs of liver problems or thyroid problems.
- Tell your doctor if you have a wound that is not healing.
Axitinib warnings and precautions
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- High blood pressure: including hypertensive crisis. Control it before starting and monitor during treatment.
- Blood clots: arterial and venous events can be fatal. Inlyta is stopped permanently if an arterial clot occurs.
- Bleeding: including fatal events.
- Heart failure: watch for symptoms throughout treatment.
- Gut perforation and fistula
- Underactive thyroid, protein in urine and liver injury: monitored with tests.
- Impaired wound healing: stop before and after surgery as directed.
- RPLS: a brain condition; Inlyta is stopped permanently if it occurs.
- Fetal harm
Axitinib interactions
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Some drugs and foods change how much axitinib is in your body.
- Strong CYP3A4/5 inhibitors (such as ketoconazole) raise levels; avoid them or lower the dose.
- Grapefruit and grapefruit juice may raise levels; avoid them.
- Strong inducers (rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentine, phenobarbital, St. John's wort) lower levels; avoid them.
- Moderate inducers (bosentan, efavirenz, etravirine, modafinil, nafcillin) may lower levels; avoid if possible.
Interactions listed in the FDA-approved label
From the Axitinib prescribing information (“Drug Interactions”): what the manufacturer studied or reported to the FDA.
- Strong CYP3A4/5 inhibitors (e.g., ketoconazole): Ketoconazole, a strong inhibitor of CYP3A4/5, increased the plasma exposure of axitinib in healthy volunteers. Avoid co-administration; select concomitant medication with no or minimal CYP3A4/5 inhibition potential. If a strong inhibitor must be co-administered, reduce the INLYTA dose.
- Grapefruit or grapefruit juice: May also increase axitinib plasma concentrations. Should be avoided.
- Strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentine, phenobarbital, St. John's wort): Rifampin, a strong inducer of CYP3A4/5, reduced the plasma exposure of axitinib in healthy volunteers. Avoid co-administration; select concomitant medication with no or minimal CYP3A4/5 induction potential.
- Moderate CYP3A4/5 inducers (e.g., bosentan, efavirenz, etravirine, modafinil, nafcillin): May also reduce the plasma exposure of axitinib. Should be avoided if possible.
Read the label’s full interactions text
7 DRUG INTERACTIONS • Avoid strong CYP3A4/5 inhibitors. If unavoidable, reduce the INLYTA dose. ( 2.2 , 7.1 ) • Avoid strong CYP3A4/5 inducers. ( 7.2 ) 7.1 CYP3A4/5 Inhibitors Co-administration of ketoconazole, a strong inhibitor of CYP3A4/5, increased the plasma exposure of axitinib in healthy volunteers. Co-administration of INLYTA with strong CYP3A4/5 inhibitors should be avoided. Grapefruit or grapefruit juice may also increase axitinib plasma concentrations and should be avoided. Selection of concomitant medication with no or minimal CYP3A4/5 inhibition potential is recommended. If a strong CYP3A4/5 inhibitor must be co-administered, the INLYTA dose should be reduced [see Dosage and Administration (2.2) and Clinical Pharmacology (12.3) ] . 7.2 CYP3A4/5 Inducers Co-administration of rifampin, a strong inducer of CYP3A4/5, reduced the plasma exposure of axitinib in healthy volunteers. Co-administration of INLYTA with strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentine, phenobarbital, and St. John's wort) should be avoided. Selection of concomitant medication with no or minimal CYP3A4/5 induction potential is recommended [see Dosage and Administration (2.2) , Clinical Pharmacology (12.3) ] . Moderate CYP3A4/5 inducers (e.g., bosentan, efavirenz, etravirine, modafinil, and nafcillin) may also reduce the plasma exposure of axitinib and should be avoided if possible.
Not a complete list. The label covers the interactions the manufacturer studied or reported, and our own interaction database does not cover every medicine either. Bring your full medication list, including vitamins and herbal products, to your pharmacist.
Before taking Axitinib
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- There are no listed contraindications, but blood pressure should be controlled first.
- Tell your doctor about clot, bleeding or gut perforation risk.
- Do not use with untreated brain metastasis or recent active stomach or bowel bleeding.
- Moderate liver impairment needs a lower starting dose; severe impairment is not studied.
- Pregnancy: can cause fetal harm; test before starting and use effective contraception during treatment and for 1 week after.
- Do not breastfeed during treatment and for 2 weeks after the last dose.
- May impair fertility.
- Not established for children.
Axitinib overdose
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There is no specific treatment for an Inlyta overdose. At higher doses in studies, people had high blood pressure, seizures linked to high blood pressure, and fatal coughing up of blood. If an overdose is suspected, Inlyta is withheld and supportive care is given, so get medical help.
What Axitinib does in the body
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In a study of 35 healthy people, a single dose of Inlyta caused no large change in the QTc interval (a heart rhythm measure). Small increases were seen when it was taken with ketoconazole.
How your body processes Axitinib
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After a dose by mouth, levels peak in about 2.5 to 4 hours, and the half-life is about 2.5 to 6 hours. Steady state is reached in 2 to 3 days. Food has only a small effect on absorption.
Axitinib is broken down mainly in the liver by CYP3A4/5 and leaves the body mostly through feces, with some in urine.
How to store Axitinib
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Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) .
Written from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
Supplements & herbs that interact with Axitinib
138 supplements and herbal products have documented interactions with Axitinib in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.
- Major · 3
- Moderate · 94
- Minor · 41
Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.
Axitinib: pharmacist answers to common questions
Quick, plain-English answers to the questions patients ask most about Axitinib — the kind of thing our pharmacy team would talk through with you at the counter.
What is axitinib for?
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How should I take it?
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What side effects are common?
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When should I call my doctor right away?
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Can I eat grapefruit or take other medicines with it?
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What if I'm pregnant or planning a family?
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Is Axitinib available over the counter?
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When was Axitinib first available?
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Who makes Axitinib?
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Answers drafted from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
More about Axitinib on HelloPharmacist
Axitinib forms and strengths (how it comes)
Axitinib is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.
Tablet
How this form is used
- Inlyta is used with avelumab for first-line treatment of advanced renal cell carcinoma.
- Inlyta is used with pembrolizumab for first-line treatment of advanced renal cell carcinoma.
- Inlyta is used alone for advanced renal cell carcinoma after failure of one prior systemic therapy.
- Inlyta is taken by mouth twice daily, about 12 hours apart, with or without food.
- Swallow Inlyta whole with a full glass of water.
- If you vomit or miss a dose of Inlyta, do not take an extra dose; take the next one at the usual time.
Axitinib on the U.S. market: products, makers and brands
How Axitinib appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.
2 companies list 4 Axitinib product records with the FDA, mostly as tablet; the earliest marketing or approval year on record is 2012. Brand names on the directory include Inlyta; the rest are generics.
Also listed with the FDA, not a patient dose form: Powder (3) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.
Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.
How widely Axitinib is used (Medicaid data)
A general measure of how commonly Axitinib is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.
Think of this as a proxy for how widely Axitinib is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.
How commonly is Axitinib prescribed? Of the 1,601 medications we measure, Axitinib ranks #1,236 by Medicaid prescriptions — more than 23% of them.
Utilization by Axitinib product
Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.
axitinib 5 MG Oral Tablet Most dispensed
Summed across the 1 of 3 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 1243012
axitinib 1 MG Oral Tablet
Summed across the 1 of 2 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 1243004
Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.
Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Axitinib, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 2 of 5 listed Axitinib NDCs with Medicaid activity.
Compare Axitinib products
A representative set of FDA-listed product records for Axitinib — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)
| Strength | Route | Manufacturer / Labeler | Category ⓘ | Details |
|---|---|---|---|---|
| 💊Tablet | ||||
| 1 mg | Oral | Pfizer Laboratories Div Pfizer Inc | NDA | View NDC → |
| 5 mg | Oral | Pfizer Laboratories Div Pfizer Inc | NDA | View NDC → |
| 1 mg | Oral | U.S. Pharmaceuticals | NDA | View NDC → |
| 5 mg | Oral | U.S. Pharmaceuticals | NDA | View NDC → |
Showing 4 of 4 products — FDA National Drug Code Directory. See every product, package size and price: browse all 4 Axitinib NDCs →
Axitinib side effects reported to the FDA (FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Axitinib — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Axitinib in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
Axitinib FDA approval history
How Axitinib went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
Axitinib recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
The FDA’s enforcement reports list no Axitinib recalls since July 2021.
✅No Axitinib recalls on record since July 2021Source: FDA enforcement (recall) reports, via openFDA; our copy was last updated Sep 24, 2026.
RxNorm Concept Web — From Ingredient to Every Form and Strength
This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.
RxCUI 1242999 1 dose form · 2 strengths
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Dose form (SCDF) Oral Tablet RxCUI 1243003In current FDA listings
Look up RxCUI 1242999 in the RxCUI Atlas →
RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.
Axitinib supply and shortage status
Whether Axitinib is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
Axitinib brand names
Axitinib is sold under one brand name in the FDA directory — Inlyta. A brand and its generic contain the same active ingredient; the brand name belongs to one company's product.
Who makes Axitinib: manufacturers and labelers
2 companies list Axitinib products with the FDA. By number of product records, the largest are Pfizer Laboratories Div Pfizer Inc, U.S. Pharmaceuticals. Labelers include manufacturers and repackagers; the product in your bottle depends on which one your pharmacy stocks.
Axitinib drug class (RxNorm)
Axitinib belongs to the Kinase Inhibitor class.
Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.
Sources for this Axitinib page
Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.
How this page is built
HelloPharmacist combines public FDA and NLM records and does not author the underlying clinical facts. The plain-language sections are written with AI from the FDA-approved label text and reviewed by our pharmacy team before publication. U.S. Pharmaceuticals is the representative DailyMed label linked for verification and dates. This is general education, not medical advice: always talk to your doctor or pharmacist about your own medicines. How we build and review drug pages →