Pazopanib

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Pazopanib

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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 Pazopanib

Property Description
Active ingredient Pazopanib (as hydrochloride salt)
Form Film-coated Tablet
Pharmacological class Kinase Inhibitor (Multi-targeted Receptor Tyrosine Kinase Inhibitor)
Common purpose Control the spread of advanced tumors
Origin Synthetic (Small molecule)

Pazopanib: Definition and Classification

Pazopanib is a synthetic small molecule compound that functions as a highly specific antineoplastic agent (anti-cancer medicine). It is formally classified within the advanced pharmacological class of Kinase Inhibitors, specifically as a multi-targeted receptor tyrosine kinase inhibitor (TKI). The active pharmaceutical ingredient is Pazopanib (INN), delivered as the hydrochloride salt, a specific formulation recognized for its suitability for oral absorption. This classification highlights that the drug is designed to interfere with specific molecular machinery within cells rather than broadly affecting dividing cells.

What Type of Kinase Inhibitor is Pazopanib?

Pazopanib's primary function is the selective inhibition of certain tyrosine kinases that are crucial for tumor survival. Specifically, the drug targets multiple key receptors, including the Vascular Endothelial Growth Factor Receptors (VEGFR-1, -2, and -3), Platelet-Derived Growth Factor Receptors (PDGFRs), and c-Kit. This multi-targeted approach is a differentiating factor, as it means the medicine works to control the spread of advanced tumors by both blocking cell growth signals and creating an anti-angiogenic effect, which hinders the development of new blood vessels needed to sustain the tumor.

Form and Core Composition of the Medication

Pazopanib is a single-agent medication intended for oral administration, supplied as a film-coated tablet. The composition includes the active ingredient, Pazopanib hydrochloride, combined with standard pharmaceutical excipients necessary to form the tablet core, such as microcrystalline cellulose and magnesium stearate. Its identity as a small molecule inhibitor allows for this oral route, providing a convenient systemic delivery method for sustained targeted treatment.

Regulatory References

  1. Pazopanib Hydrochloride - NCI Drug Dictionary

What side effects are possible with Pazopanib?

Pazopanib: Possible Side Effects and Safety Information

Pazopanib is associated with a distinct safety profile, including risks of serious and fatal events documented in regulatory labeling. The most Very Common (ge 1/10) adverse reactions reported across clinical studies include diarrhea, hypertension, hair color changes, nausea, vomiting, decreased appetite, fatigue/asthenia, headache, and dysgeusia (taste disturbance).

Serious and Clinically Significant Adverse Reactions

The most serious safety concerns identified in official documentation include severe and fatal hepatotoxicity, which requires frequent monitoring of liver function tests (ALT, AST, bilirubin). Cardiovascular risks are prominent, including hypertension (often occurring early in treatment), QT interval prolongation leading rarely to Torsades de Pointes, and fatal arterial and venous thromboembolic events (ATE/VTE). Other serious events requiring monitoring or discontinuation include Gastrointestinal perforation/fistula (fatal cases reported), Hemorrhagic events (fatal cases reported), Reversible Posterior Leukoencephalopathy Syndrome (RPLS)/PRES (fatal cases reported), and Interstitial Lung Disease (ILD)/Pneumonitis (fatal cases reported).

Safety Monitoring and Restrictions

Close monitoring is mandated for liver function, blood pressure, cardiac function (LVEF), and urine protein levels. Specific dose adjustments or interruptions are required to manage these reactions. Use is contraindicated in patients with known hypersensitivity to the drug. Pazopanib is not recommended for use in patients with severe hepatic impairment (bilirubin > 3 imes ULN) and should be used with caution and a reduced dose in moderate hepatic impairment. It is generally not recommended in pediatric patients due to potential effects on organ growth. Temporary suspension is advised before planned surgical procedures due to the risk of impaired wound healing.

Overdose and Emergency Response

Overdose and When to Seek Help

The official regulatory profile for Pazopanib overdose requires immediate medical attention and is based on managing severe clinical toxicity. Experience with acute overdose is limited, and documented clinical presentations reflect the severe, exaggerated expression of known signs, such as extreme tiredness.

Should a suspected overdose occur, official guidance mandates that individuals seek immediate medical attention and contact a Poison Control Center. Emergency medical services must be contacted immediately if the individual exhibits specific life-threatening clinical manifestations, including being collapsed, having a seizure, experiencing trouble breathing, or cannot be awakened.

The regulatory profile for overdose management confirms that no specific antidote for Pazopanib is available. Consequently, hospital intervention relies entirely on providing symptomatic treatment and supportive treatment, which requires close medical observation. Furthermore, official prescribing information notes that procedural attempts like hemodialysis are unlikely to be effective for clearing the drug due to its high plasma protein binding. No specific risk or severity adjustments are detailed for particular patient populations in the official overdose sections.

Therapeutic Uses of Pazopanib

Pazopanib is a systemic treatment that is relevant for managing two specific types of advanced malignancies. It focuses on supporting the control of disease activity and supports general well-being during symptomatic phases.

The treatment is indicated for advanced renal cell carcinoma (RCC) and for specific subtypes of advanced soft tissue sarcoma (STS) in adults who have received prior chemotherapy. It is applied across domains where additional symptomatic support is needed to manage widespread or progressive tumor activity.

This treatment is relevant in contexts involving heightened systemic burden, particularly when symptoms may intensify due to tumor spread or aggressive disease progression.

“This treatment supports the patient during difficult episodes by easing the overall symptom burden in symptomatic periods.”

The primary therapeutic benefit helps with managing disease progression, which generally contributes to a period of disease stability. The use of this treatment may assist with maintaining functional stability and helps address symptom clusters that may become intense or disruptive as a result of the aggressive nature of the malignancy.


Quick Fact: Relief for Symptoms Related to Tumor Growth

Eligibility and Restrictions for Use

Pazopanib is an antineoplastic agent with specific population-based eligibility rules defined by regulatory authorities like the FDA and EMA.

Who Is Eligible?

  • Adults (ge 18 years of age) with advanced renal cell carcinoma (RCC) or with specific subtypes of advanced soft tissue sarcoma (STS) who have received prior chemotherapy.

Absolute Contraindications (Must Not Use)

Contraindication Condition Source Basis
Hypersensitivity Known allergy to pazopanib or any component of the formulation. Regulatory Labeling
Age Pediatric patients less than 2 years of age. Regulatory Labeling

Eligibility-Related Restrictions

  • Hepatic Impairment: Use is not recommended in patients with severe hepatic impairment (total bilirubin >3 imes ULN). Patients with moderate hepatic impairment are eligible but require an official dose reduction.
  • Renal Impairment: Use is not recommended in patients with severe renal impairment (creatinine clearance <30 mL/min) due to a lack of experience in this population. No adjustment is required for mild-to-moderate impairment.
  • Clinical History: Pazopanib should not be used in patients with a history of hemoptysis, cerebral, or clinically significant gastrointestinal hemorrhage in the past six months.
  • Reproductive Status: Use during pregnancy is not recommended as the drug can cause fetal harm. Breastfeeding is not recommended during treatment. Women of childbearing potential must use effective contraception.

What should I know about interactions with other medicines?

Pazopanib's interaction profile is documented primarily by its metabolic and transporter activity, which determines how other medicines affect its systemic exposure. Strong CYP3A4 Inhibitors, such as ketoconazole, and P-glycoprotein/BCRP Inhibitors significantly increase Pazopanib plasma concentrations. Conversely, chronic co-administration with Strong CYP3A4 Inducers, like rifampin, is not recommended due to the potential for decreased exposure. Pazopanib also acts as an inhibitor of CYP3A4, CYP2D6, and CYP2C8, a property that requires caution with co-administered agents that have a narrow therapeutic window.

The regulatory profile also includes specific pharmacodynamic cautions. Co-administration with simvastatin is documented to increase the risk of ALT elevations. Additionally, caution is advised with medications that prolong the QT interval.

Administration is subject to mandatory timing rules. Food intake significantly increases Pazopanib exposure, mandating that the drug be administered without food, specifically one hour before or two hours after a meal. Agents that raise gastric pH, such as PPIs, should be avoided as they decrease Pazopanib exposure. Short-acting antacids require separation by several hours. For population-specific interaction considerations, use is not recommended in patients with severe hepatic impairment due to reduced and variable exposure.

Mechanism of Action

How Pazopanib Works: Mechanism of Action

Pazopanib functions as a multi-targeted Tyrosine Kinase Inhibitor (TKI). Its primary action is to bind to the intracellular ATP-binding pocket of several key Receptor Tyrosine Kinases (RTKs), notably VEGFR-1, -2, -3, PDGFR-alpha and -beta, and c-Kit. This molecular blockade prevents the phosphorylation and activation of these RTKs, thereby suppressing the initiation of subsequent intracellular signaling cascades .

By interfering with VEGFR signaling, Pazopanib disrupts the pathways essential for new blood vessel formation, consequently interfering with pathological angiogenesis. This process limits the blood supply and nutrient delivery to the affected tissue, which induces vascular regression and normalization.

The simultaneous inhibition of PDGFR and c-Kit limits the activation of critical downstream survival cascades, including the PI3K/AKT/mTOR and RAF/MEK/ERK pathways. This molecular interference modulates cell populations via decreased proliferation and increased apoptosis (programmed cell death).

Dosage and Administration Information

How to Use Pazopanib: Official Administration Guidelines

Pazopanib is a medicine for systemic treatment that is administered orally as a film-coated tablet. Official administration guidelines define a strict daily regimen to ensure consistent systemic exposure.


Standard Dosing and Frequency

The recommended standard starting dose for adults with advanced renal cell carcinoma (RCC) or advanced soft tissue sarcoma (STS) is 800 mg taken once daily. This dose of Pazopanib should not exceed 800 mg per day. The regimen is typically continuous, lasting until disease progression or development of intolerable side effects.

Administration adjustments are generally made in 200 mg increments or decrements based on individual tolerability. For instance, the dose must be reduced to 400 mg once daily if co-administered with a strong CYP3A4 inhibitor.


Administration Conditions and Handling

The oral tablets must be taken without food. Administration must occur at least one hour before or two hours after consuming a meal. The tablets should be swallowed whole with water and must not be crushed, broken, or chewed.

If a dose is missed, it should not be taken if the time until the next scheduled dose is less than 12 hours. For specific patient populations, such as those with moderate hepatic impairment, the dose should be reduced to 200 mg once daily. No initial dose adjustment is required for patients with renal impairment with a creatinine clearance of 30 mL/min or greater.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Pazopanib


Evidence for Use in Advanced Renal Cell Carcinoma (RCC)

Research has studied Pazopanib for use in patients with advanced kidney cancer. The main evidence comes from large-scale clinical trials, which often involved comparing Pazopanib to a placebo (an inactive substance) or to other study treatments. These studies were evaluated in conditions marked by functional limitations related to the advanced stage of the disease. They were designed to monitor the outcomes related to systemic or functional imbalance over defined time intervals.

The findings from these key trials suggest patterns that were observed when Pazopanib was studied, including in comparison to other study treatments or a placebo. The research describes patterns observed in the studies related to how the disease progressed in the observed populations. It is important to remember that these findings describe group patterns, not personal outcomes.


Evidence for Use in Advanced Soft Tissue Sarcoma (STS)

Pazopanib was studied for use in advanced soft tissue sarcoma (STS), a group of conditions where symptoms may vary in intensity. Research in this area explored how symptoms evolved in patients with several different subtypes of STS whose disease had continued to progress after prior chemotherapy. These studies were evaluated in a research context involving fluctuating or unstable symptoms. The key studies for STS indicate patterns related to outcomes reflecting daily functioning or activity level, which were observed during the study periods. The research highlights changes measured during the study period, helping to contextualize how patients reported their experience of the condition.


Long-Term Studies and Follow-Up

Research has also examined the long-term course of the conditions and the potential for a sustained response in patients who received Pazopanib. Information about long-term outcomes is mainly derived from extended observation of patients who participated in the initial trials. The data show patterns related to the time interval over which a response was observed in some studies. However, long-term effects are not fully established, and follow-up durations were limited in the initial pivotal trials.


Evidence in Specific Patient Groups (Special Populations)

Research has explored how Pazopanib affects groups whose health status or age might change how the body processes the medication. Specifically, studies were observed in older adults, as well as patients who had pre-existing conditions affecting the liver or kidneys. For patients with impaired liver function, studies show patterns related to how the body handles the medicine, which may be relevant to clinical considerations as studied in the research. Data for certain groups, such as children or populations related to pregnancy, remain insufficient.


What Is Still Uncertain About Pazopanib Research

While a significant body of research was studied for Pazopanib, several areas still require further investigation. Comparative evidence is lacking for direct, long-term comparisons with all competing therapies, and the research often focuses on short-term symptom changes rather than decade-long outcomes. The findings were mixed regarding the optimal sequence of therapies. The study results reflect the specific conditions under which they were conducted, and evidence quality varies across studies. This means that synthesizing the entire body of evidence still reveals main evidence gaps that future research may need to address to improve certainty for patients.

Key Studies & References

  1. Pazopanib Versus Placebo in Patients With Soft Tissue Sarcoma Whose Disease Has Progressed During or Following Prior Therapy (PALETTE)

Frequently Asked Questions (FAQ)

Common questions about Pazopanib (FAQ)


Q: Is Pazopanib the same as Votrient?

A: Votrient is the brand name under which the active pharmaceutical ingredient pazopanib hydrochloride is marketed. Therefore, they refer to the same medication.


Q: What is a 'tyrosine kinase inhibitor' in simple terms?

A: Pazopanib is formally classified as a targeted anti-cancer medicine called a protein-kinase inhibitor, or TKI. This means it blocks specific enzymes (kinases) within cancer cells that signal the tumor to grow, spread, and form new blood vessels.


Q: Does Pazopanib cause hair loss?

A: Hair color change (depigmentation) is listed as a very common side effect of Pazopanib in official product information. While hair thinning or loss (alopecia) is not always listed among the most frequent reactions, it has been reported.


Q: Does Pazopanib cause fluid retention or swelling?

A: Fluid retention (edema) or swelling is not typically listed among the very common side effects (seen in ge 1 in 10 patients) in official regulatory documents. Observation of any swelling or fluid retention requires consultation with a healthcare provider.


Q: What should I do if my skin changes color while using Pazopanib?

A: Changes in skin color (hypopigmentation) are a reported side effect of Pazopanib. Consultation with a healthcare provider is important if any new side effect, like skin discoloration, is observed.


Q: Are there any common long-term side effects from using Pazopanib?

A: Official documents state that the drug is often taken long-term, lasting until the disease progresses or side effects become intolerable. Serious safety risks like severe liver damage, high blood pressure, and heart issues require careful monitoring throughout the entire course of treatment, not just the beginning.


Q: What tests are done before starting Pazopanib treatment?

A: Regulatory documents require checking certain health markers before starting treatment. This includes blood tests to check liver function and monitoring of blood pressure is required as part of the check before starting treatment. Monitoring of heart function may also be considered for certain patients.


Q: Is it common for people to stop Pazopanib because of side effects?

A: Regulatory labels provide detailed rules for interrupting, reducing, or permanently stopping the dose if a serious side effect occurs. This indicates that managing serious adverse reactions is a known risk strategy documented in official guidance.


Q: Can Pazopanib interact with herbal supplements?

A: Yes, official product information states that strong CYP3A4 inducers, such as the herbal product St. John's Wort, are typically not recommended. Taking these can reduce the level of Pazopanib in your blood, potentially making it less effective.


Q: Does Pazopanib interact with common pain relievers like Tylenol?

A: Acetaminophen ( Tylenol^circledR) is generally mentioned in patient guides as an acceptable option for mild pain relief during this therapy. However, the official guidance states that a healthcare provider is the source for questions regarding new over-the-counter medication.


Q: Can I take multivitamins or supplements while on Pazopanib?

A: Consulting a healthcare provider is an important step before starting any vitamins, supplements, or natural health products. The regulatory information indicates that some of these products can interfere with how Pazopanib is processed in the body.


Q: What kind of diet is recommended while on Pazopanib?

A: The official regulatory label does not recommend a specific diet, such as a low-fat or high-protein regimen. The label specifies that the drug should be taken without food and that certain products, like grapefruit, are to be avoided.


Q: Does being on Pazopanib affect fertility?

A: Official product information states that based on animal studies, Pazopanib may cause harm to an unborn baby. For this reason, the use of effective contraception is a regulatory requirement for women who could become pregnant during treatment.


Q: Can men taking Pazopanib father a child?

A: Condom use is a specific regulatory requirement for men if their partner is pregnant or of childbearing potential, during treatment and for a period afterward. This precaution is necessary due to the risk of fetal harm.


Q: Is Pazopanib a palliative treatment or a curative one?

A: Pazopanib is indicated for advanced cancer, meaning the disease has started to spread. Official research evidence focuses on outcomes such as controlling the spread of tumors and extending progression-free survival.


Q: What is the difference between Pazopanib and Sunitinib?

A: These are different medicines, although both belong to the targeted therapy class of TKIs. Pazopanib was directly compared to Sunitinib in large clinical trials, where researchers noted different safety profiles between the two drugs, such as heart-related issues.


Q: What is the general success rate of Pazopanib in clinical studies?

A: Clinical studies measured the drug's effectiveness using endpoints like progression-free survival (PFS), which tracks how long a patient lives without the disease getting worse. For advanced kidney cancer, the median PFS for patients taking Pazopanib in the main study was 9.2 months, compared to 4.2 months for placebo.


Q: Has Pazopanib been studied in combination with other treatments?

A: Pazopanib was studied primarily as a monotherapy (single agent) in its pivotal trials. Official documents also mention studies where it was compared to or, in some cases, combined with other cancer treatments in a research setting.


Q: Are there ongoing clinical trials related to Pazopanib?

A: Regulatory approval is based on clinical research studies that have been completed. Information on any current or ongoing clinical trials related to Pazopanib can be found on official government trial registries, which tracks new research.


Q: Is there a generic version of Pazopanib available?

A: Yes, the U.S. FDA has approved generic versions of Pazopanib hydrochloride tablets.

How should Pazopanib be stored and disposed of?

How to Store and Dispose of Pazopanib

The following instructions are based on official regulatory requirements for storing and discarding Pazopanib tablets.

Storage Requirements

Pazopanib must be stored at controlled room temperature, specifically between 15°C and 30°C (59°F and 86°F). The medication must be kept in its original container with the cap tightly closed to protect it from excess heat and moisture; for this reason, storage in a bathroom is discouraged. For safety, Pazopanib must be stored out of the sight and reach of children and secured with a child-resistant cap.

Disposal Instructions

Unused or expired Pazopanib is classified as pharmaceutical waste and must not be disposed of in household trash or poured down a drain or toilet. Disposal must strictly adhere to local requirements for hazardous medicinal products. Patients should return unused medication to a pharmacy or a designated pharmaceutical waste collection program for proper destruction.

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

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