Inlyta

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Inlyta

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Inlyta

What is Inlyta? (Overview)

Property Description
Active Ingredient Axitinib
Form Film-coated tablet (oral formulation)
Pharmacological Class Tyrosine Kinase Inhibitor (TKI)
Common Use Targeted therapy for advanced kidney cancer
Origin Synthetic organic compound

What Type of Medicine is Inlyta (Axitinib)?

Inlyta is a prescription-only medication developed by Pfizer, containing the single active substance axitinib, which is characterized as a synthetic small molecule drug. Its primary classification is an antineoplastic agent, used in the treatment of cancer, and it belongs specifically to the class of Tyrosine Kinase Inhibitors (TKI). Axitinib is a second-generation TKI. This distinction reflects its improved selectivity toward the receptors crucial for tumor survival compared to some earlier agents in its class.

Composition, Form, and Origin of Axitinib

The core component, axitinib, is a chemically manufactured compound identified as an indazole derivative. The drug is consistently supplied in the form of a solid, red film-coated tablet intended for oral administration, a differentiating factor from treatments requiring intravenous delivery. The formulation is a single-ingredient product where axitinib is combined with standard tablet excipients, including lactose monohydrate.

General Purpose: How Inlyta Supports Treatment

The general function of Inlyta is to manage the progression of advanced disease by interfering with the biological processes that enable aggressive tumors to grow. Axitinib works as an inhibitor by specifically targeting the Vascular Endothelial Growth Factor Receptors (VEGFR-1, VEGFR-2, and VEGFR-3). This mechanism blocks the action of an abnormal protein that signals cancer cells to multiply. By performing this targeted VEGF signaling pathway blockade, the medication achieves angiogenesis inhibition, restricting the formation of new blood vessels needed by the tumor for sustained nourishment and expansion.

What side effects are possible with Inlyta?

Possible side effects and safety information

The safety profile of Inlyta (axitinib) is established through official regulatory documentation, which classifies potential effects by frequency and the body system affected. These classifications are based on observed data from clinical use and are not intended as medical advice.

Very Common (ge 1/10 incidence) adverse reactions documented in regulatory sources include diarrhea, hypertension (high blood pressure), fatigue, nausea, decreased appetite, vomiting, and Palmar-Plantar Erythrodysesthesia Syndrome (PPE). Other very common effects involve the nervous system, such as headache and dysgeusia (taste disturbance), and the renal system, such as proteinuria (protein in the urine).

Serious adverse reactions are explicitly documented in official labels. These include hemorrhage (bleeding events, sometimes fatal), arterial and venous thromboembolic events (blood clots), gastrointestinal perforation and fistula formation, and Hypertensive Crisis. Hepatotoxicity (liver problems) and Reversible Posterior Leukoencephalopathy Syndrome (RPLS) are also listed as serious events.

Regulatory documentation also provides specific safety parameters for certain populations. The medicine is not recommended for use in patients with severe hepatic impairment (Child-Pugh C) due to anticipated increased exposure. Furthermore, the label mandates routine monitoring of several physiological factors, including blood pressure, thyroid function, and liver enzymes, as well as the presence of proteinuria.

Time-related patterns noted in official labeling include the observation that hypertension often appears early in the course of treatment.

Overdose and Emergency Response

The official regulatory profile for Inlyta (axitinib) overdose is defined by specific severe clinical events documented in cases of high-dose exposure, such as receiving starting doses of 10 mg or 20 mg twice daily. The specific clinical manifestations observed may include hypertension and general dizziness.

Of greater regulatory concern are the severe and potentially life-threatening outcomes reported in these high-dose situations, including seizures associated with hypertension and fatal hemoptysis (coughing up blood). The documentation of these severe and fatal events establishes the critical need for immediate medical intervention.

In any case of suspected overdose, regulatory guidance strictly mandates that Inlyta should be withheld immediately, and supportive care must be instituted. This management approach is defined by the fact that the official prescribing information states no specific treatment or antidote is known for axitinib overdose. Therefore, the immediate goal of medical intervention is to manage the symptoms and maintain the patient's vital functions, utilizing supportive measures entirely due to the absence of a pharmaceutical reversal agent. The regulatory information does not explicitly document population-specific overdose considerations for any specific age group or patient condition.

Therapeutic Uses of Inlyta

What Inlyta Treats: Main Uses and Benefits

Inlyta (axitinib) is a targeted therapy used in the management of advanced renal cell carcinoma (RCC), a condition characterized by periods of heightened symptoms. Its therapeutic domain focuses on providing support in situations involving symptoms linked to organ-specific functional stress.

This medication is utilized for the treatment of advanced RCC. It is used as a single agent for patients whose cancer has progressed after one prior systemic therapy, and it is also used in combination with other immunotherapies for initial treatment. In summary, its primary uses cover advanced RCC after one prior systemic therapy and in combination with immunotherapy as initial treatment.

This therapeutic approach contributes to easing the overall symptom load. This clinical application may assist with maintaining functional stability and supports patients during episodes of heightened discomfort.

Quick Fact: Relief for symptoms that create noticeable physiological strain.

This approach is considered relevant for easing symptoms that become more disruptive during flare-ups, offering symptomatic relief that helps patients cope more steadily with symptom fluctuations.

Regulatory References

  1. National Cancer Institute overview of Axitinib

Eligibility and Restrictions for Use

Inlyta (axitinib) is a prescription medication approved for the treatment of advanced renal cell carcinoma (RCC), a type of kidney cancer that has spread or cannot be removed by surgery.

It is used in two main settings:

  • First-line treatment: In combination with other therapies, such as pembrolizumab or avelumab, for patients who have not received prior systemic treatment for advanced RCC.
  • Monotherapy: Alone, for patients whose advanced RCC has progressed after receiving one prior systemic treatment.

Contraindications and Cautions

There are no absolute contraindications listed for Inlyta; however, the drug should not be used in certain circumstances due to the risk of serious complications. Always discuss your complete medical history with your healthcare provider before starting treatment.

Condition Recommendation/Risk
Pregnancy Can cause fetal harm; effective contraception is required during treatment and for a period afterward.
Severe Hepatic Impairment Not studied and should generally be avoided in patients with severe liver disease (Child-Pugh class C).
Recent Bleeding/Brain Metastasis Should not be used in patients with untreated brain metastasis or recent, active gastrointestinal bleeding.
Uncontrolled High Blood Pressure Should be controlled before starting Inlyta, as the drug commonly causes or worsens hypertension.
Surgery May impair wound healing; treatment should be stopped at least 2 days prior to elective surgery and not restarted until adequate healing is confirmed.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile of Inlyta (axitinib) is primarily defined by the influence of co-administered substances on its metabolism via the CYP3A4/5 enzyme system. Official regulatory documents classify these interactions into categories based on their clinical significance, resulting in specific constraints to avoid significant changes in axitinib exposure.


Pharmacokinetic Interactions

Interacting Substance Category Constraint and Rationale
Strong CYP3A4/5 Inhibitors (e.g., ketoconazole) Avoid co-administration due to the risk of increased axitinib plasma concentration. If avoidance is not possible, the axitinib dose requires adjustment.
Strong CYP3A4/5 Inducers (e.g., rifampin, phenobarbital, phenytoin) Avoid co-administration due to the risk of decreased axitinib plasma concentration, potentially reducing effectiveness.
Moderate CYP3A4/5 Inducers Avoid if possible due to potential reduction in axitinib plasma concentration.

Food, Herbal, and Population Constraints

Official labeling specifically requires the avoidance of certain substances that influence CYP3A4/5 activity. Patients should avoid grapefruit or grapefruit juice and the herbal product St. John's wort (Hypericum perforatum). Additionally, specific population-based constraints exist: the starting dose of axitinib is lower for patients with moderate hepatic impairment (Child-Pugh B), reflecting their reduced capacity to clear the drug.

Mechanism of Action

Targeted Inhibition of Key Growth Receptors

Axitinib acts as a highly specific small-molecule inhibitor by directly targeting the intrinsic tyrosine kinase activity of the Vascular Endothelial Growth Factor Receptors ( VEGFR-1, -2, and -3). The drug accomplishes this by competitively binding to the receptor’s intracellular ATP site, which prevents the required autophosphorylation and suppresses the signaling mechanism that drives cellular proliferation.


Blockade of the Angiogenesis Signaling Cascade

By shutting down VEGFR signaling, axitinib disrupts the entire angiogenesis cascade, which is the biological process of forming new blood vessels. This molecular blockade inhibits the subsequent proliferation and migration of endothelial cells, leading to the core physiological consequence of diminished vascular supply and flow of oxygen and nutrients to the target tissue.


️ Constraint of Tissue Vascular Development

The ultimate physiological effect of this mechanism is the constraint of tissue vascular development, which imposes a restricted capacity for cellular mass to increase. The mechanistic effect is directly linked to the drug concentration achieved at the molecular target site, meaning the action can be constrained by local drug levels or the development of biological resistance mechanisms over time.

Dosage and Administration Information

Official Administration Guidelines for Inlyta (Axitinib)

Inlyta is administered as an oral medication, provided in the form of a film-coated tablet for long-term use in approved indications. The administration schedule is structured around continuous, twice-daily dosing.


Standard Dosing and Frequency

Treatment is initiated with a standard starting dose of 5 mg taken twice daily (BID), with doses separated by approximately 12 hours. The standard maintenance approach is continuous dosing, meaning treatment proceeds without scheduled breaks, often continuing until disease progression or unacceptable toxicity. The total daily dosage may be adjusted, or titrated, based on the individual's ability to tolerate the medicine, with the dose potentially increasing to a maximum of 10 mg twice daily or being reduced to as low as 2 mg twice daily if necessary.


Administration Requirements and Adjustments

The tablets should be swallowed whole with water and must not be crushed, broken, or chewed. Inlyta may be taken with or without food.

Procedural Instructions:

  • Missed Dose: If a patient misses a scheduled dose or vomits after taking a dose, an additional dose should not be taken. The patient should simply resume the usual schedule with the next planned dose at the prescribed time.
  • Hepatic Impairment: A modification is required for patients with moderate hepatic impairment (Child-Pugh Class B), for whom the standard initial dose should be reduced by approximately half to account for altered drug metabolism.
  • Co-Administration: If a strong CYP3A4/5 inhibitor cannot be avoided, the Inlyta dose should also be decreased by approximately half due to the potential for increased drug exposure.

Recent Clinical Evidence

Research Evidence: Overview of Studies for Inlyta (Axitinib)


Evidence for Use in Advanced Kidney Cancer as Monotherapy (Second-Line)

The research supporting the use of Inlyta as a single agent (monotherapy) for advanced renal cell carcinoma (RCC) after prior systemic treatment was primarily evaluated in a pivotal Phase III Randomized Controlled Trial (RCT). This type of large-scale, randomized research is used in regulatory assessments of a medicine. The studies examined key time-based outcomes, including Progression-Free Survival (PFS), which was studied for tracking the time before the disease progressed, and Overall Survival (OS). The population was studied for advanced clear-cell RCC, generally focusing on adults with a good functional status.

The trial reported measurements of PFS for the axitinib group and a comparator group (sorafenib). The research also described patterns in the Objective Response Rate (ORR). When researchers examined the overall time patients lived (OS), the findings did not indicate a statistically significant difference between the axitinib group and the sorafenib group. The results apply only to the populations studied, meaning there is limited information for long-term outcomes in certain patient subgroups, such as those with a poor functional status.


Evidence for Use in Combination Therapy (First-Line)

Inlyta was studied for use as a starting treatment (first-line) for advanced RCC when given in combination with specific immune checkpoint inhibitors. The research examined two separate large, randomized Phase III RCTs. These studies compared the combination treatment against sunitinib monotherapy.

These trials explored two critical outcomes: Overall Survival (OS) and Progression-Free Survival (PFS). They also monitored the Objective Response Rate (ORR). Studies described patterns of the measured outcomes (OS and PFS) in the combination treatment groups and the sunitinib monotherapy groups. These findings contribute to the broader evidence landscape for the combination therapy.


Evidence in Less Common Kidney Cancer Subtypes

The research base for Inlyta in less common kidney cancer subtypes, such as the non-clear cell forms of RCC, is distinct. The evidence was evaluated in smaller-scale Phase II clinical trials and observational studies, which have sample sizes that were modest when compared to the large Phase III trials. These studies monitored the ORR and measured time-based outcomes. The limited comparative evidence from large, randomized trials for non-clear cell RCC subtypes remains a key research gap.

Key Studies & References

  1. Pembrolizumab Plus Axitinib Versus Sunitinib as First-line Treatment of Advanced Renal Cell Carcinoma: 43-month Follow-up of the Phase 3 KEYNOTE-426 Study

Frequently Asked Questions (FAQ)

Common questions about Inlyta (FAQ)


Q: How is Inlyta different from other kidney cancer medications I've heard about?

A: According to official information, Inlyta (axitinib) belongs to a class of medicines called tyrosine kinase inhibitors (TKIs), similar to some other kidney cancer drugs. Clinical studies often compare Inlyta to these other agents, such as sunitinib or sorafenib. Regulatory documents describe Inlyta as a highly targeted inhibitor of the VEGFR receptors. Some clinical studies suggest it exhibits a high affinity for these specific receptors.

Q: Does Inlyta work by shrinking tumors or stopping them from growing?

A: Inlyta works by targeting the receptors that signal the formation of new blood vessels, a process called angiogenesis. By suppressing this signaling, the drug restricts the blood and nutrient supply to the tumor. This mechanism of action is intended to restrict the blood supply, which may help limit the expansion and growth of cancerous cells.

Q: Are there long-term side effects associated with taking Inlyta for years?

A: The official product label details the common and serious adverse reactions observed in clinical trials, such as high blood pressure and thyroid changes. Since treatment can be long-term, ongoing monitoring is essential to manage any side effects that may persist or develop over time. The duration of treatment and long-term safety profile are best reviewed with a prescribing healthcare professional.

Q: How does Inlyta affect the heart?

A: Regulatory documents indicate that Inlyta can be associated with serious cardiac issues, including heart failure and the formation of blood clots in the arteries (arterial thromboembolic events). Due to these potential risks, routine monitoring for changes in heart function is often part of the treatment plan.

Q: Why is proper hydration important while taking Inlyta?

A: Official safety information notes that very common side effects of Inlyta include diarrhea and vomiting. These conditions can lead to fluid loss and dehydration. Addressing and managing these gastrointestinal effects is an important part of the treatment management plan.

Q: Does Inlyta cause any changes to skin or hair?

A: Yes, regulatory sources list skin-related events as common side effects. A very common reaction is Palmar-Plantar Erythrodysesthesia Syndrome (PPE), which involves redness, swelling, or peeling on the palms of the hands and soles of the feet. Other reported skin reactions include general rash.

Q: Are there any known drug interactions with common herbal supplements and Inlyta?

A: The official product information specifically advises avoiding the herbal product St. John's wort (Hypericum perforatum). This is because St. John's wort can significantly decrease the amount of Inlyta in the blood, which may reduce the drug's effectiveness.

Q: Are there certain medications I should tell my doctor about before starting Inlyta?

A: Official patient counseling information emphasizes the importance of informing the healthcare provider about all prescription and non-prescription medicines, vitamins, and herbal supplements being taken. Medications that affect the CYP3A4/5 enzyme system are of particular concern as they can greatly change the levels of Inlyta in your body.

Q: How effective is Inlyta in controlling the spread of kidney cancer?

A: Clinical studies measure the effectiveness of Inlyta using metrics like Progression-Free Survival (PFS) and Overall Survival (OS). PFS tracks the time until the disease spreads or worsens. In clinical trials, Inlyta demonstrated favorable outcomes, such as extended PFS, when compared to a prior standard of care, contributing to the evidence base for managing disease progression.

Q: How long does it usually take to see if Inlyta is working?

A: Official clinical trial results track the Objective Response Rate (ORR), which indicates the percentage of patients who experience tumor shrinkage. While the exact timing of response is individual, clinical trials often evaluate patterns of tumor response and disease stability during the first few months of therapy.

Q: How long do most patients stay on Inlyta treatment?

A: According to the official prescribing information, Inlyta is generally continued for as long as the treatment is benefiting the patient. Treatment is generally intended to continue until there is evidence of disease progression or until the patient experiences unacceptable toxicity.

Q: Can I take over-the-counter pain relievers while on Inlyta?

A: Patient counseling guidelines advise informing your healthcare provider about all over-the-counter medications you use, including pain relievers. This is important because even non-prescription drugs could potentially affect Inlyta’s metabolism or increase the risk of side effects like bleeding.

Q: Is it normal to have some mouth sores when taking this medication?

A: Official adverse event reports indicate that mouth sores (stomatitis or inflammation of the mouth lining) are listed as a common reaction associated with Inlyta.

Q: Can people with diabetes safely use Inlyta?

A: The official label instructs patients to inform their healthcare team about all existing medical conditions, including diabetes. Clinical trial data has shown that hyperglycemia, or high blood sugar, is a common laboratory abnormality observed in patients taking Inlyta.

Q: Does Inlyta increase sensitivity to the sun?

A: Photosensitivity (increased sun sensitivity) is not explicitly listed as a common or serious adverse reaction in the key regulatory documents. However, skin reactions like rash are reported. Management of sun exposure is a topic that should be reviewed with a healthcare professional.

Q: Is it normal for my hands and feet to feel tingly or numb on Inlyta?

A: Peripheral neuropathy (tingling or numbness) is not commonly listed in the official adverse reaction reports for Inlyta. Any new or unusual sensations should be brought to the attention of a healthcare professional.

Q: Does Inlyta cause swelling in the face or limbs?

A: Edema (swelling in the limbs or face due to fluid retention) is a known adverse reaction associated with Inlyta. Swelling is also noted as a potential symptom of more serious, underlying conditions that require monitoring, such as heart issues or proteinuria.

Q: Can Inlyta affect cholesterol levels?

A: Some product monographs and clinical studies list dyslipidaemia, which refers to abnormal lipid or cholesterol levels, as an adverse drug reaction. Healthcare providers may monitor your lipid levels periodically.

Q: What are the key differences between Inlyta and Sutent?

A: Both Inlyta (axitinib) and Sutent (sunitinib) are officially approved tyrosine kinase inhibitors used for kidney cancer. Clinical studies have compared the two drugs, and official information indicates they have different side effect profiles and may be used in different treatment settings, such as Inlyta in combination therapy.

Q: Can Inlyta be taken with blood thinners?

A: Official warnings state that Inlyta has been associated with an increased risk of bleeding (hemorrhage) and blood clots. Patients receiving concurrent treatment with medicines that affect blood clotting, such as blood thinners, require close supervision by a healthcare professional.

Q: Is Inlyta safe for people who have existing liver problems?

A: Regulatory guidance requires a dose reduction for patients diagnosed with moderate hepatic impairment (Child-Pugh Class B). Inlyta is generally not recommended for use in patients who have severe liver impairment (Child-Pugh Class C).

Q: Can Inlyta affect fertility in men or women?

A: According to the official prescribing information, Inlyta may cause fertility problems in both males and females. This risk of impaired fertility is listed in the official prescribing information.

Q: What should I do if I experience severe diarrhea while taking Inlyta?

A: Severe or persistent diarrhea is covered by official dose management guidance, which may include dose interruption or reduction, along with the use of symptomatic medications. Such events should be reported to a healthcare professional.

How should Inlyta be stored and disposed of?

Storage and Disposal Conditions for Inlyta (axitinib)

Inlyta tablets must be stored at Controlled Room Temperature, specifically between 20 C to 25 C (68 F to 77 F), with permitted temporary excursions. The medication must be kept in the container it came in and the bottle must remain tightly closed. Storage should be away from excess heat and moisture.

Child Safety and Disposal

Inlyta must be stored securely out of the sight and reach of children. Regarding disposal, do not flush the tablets down the toilet or pour them into a drain. Unused or expired medication should be disposed of by taking it to a medicine take-back program. If a take-back program is unavailable, official guidelines recommend mixing the tablets with an undesirable substance, sealing the mixture in a bag, and discarding it in the trash.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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