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Pazopanib: Indications, Adverse Effects, Contraindications and Dosage

Mechanism of Action of Pazopanib:

Pazopanib is an oral multikinase inhibitor, primarily targeting tyrosine kinases such as c-KIT, VEGF, and PDGF receptor kinases. Inhibiting these receptors blocks the signaling pathways that drive angiogenesis and tumor growth.

Urologic Indications of Pazopanib:

Pazopanib is a treatment option of metastatic renal cell carcinoma in patients with favorable risk who have contraindications to checkpoint inhibitors (Sternberg et al., 2010). Pazopanib is also used as a second-line therapy after progression on checkpoint inhibitors (e.g. nivolumab or pembrolizumab).

Pharmacokinetics of Pazopanib:

Administer orally on an empty stomach; take at least 1 hour before or 2 hours after a meal. Hepatic metabolism occurs predominantly via CYP3A4; the elimination half-life is approximately 31 hours, and elimination is primarily fecal.

Adverse Effects of Pazopanib:

Gastrointestinal Tract:

Very common nausea, vomiting, and diarrhea; common abdominal pain and mucositis; occasional gastrointestinal bleeding or perforation.

Skin:

Impaired wound healing, very common rash and hand-foot syndrome; common hypopigmentation (including hair depigmentation), alopecia, erythema, and pruritus.

Hematologic:

Common thrombocytopenia and neutropenia; consider monitoring for anemia.

Hepatic:

Common transaminase elevations and hepatotoxicity, occasionally presenting with hepatitis; rare liver failure.

Cardiovascular Adverse Effects:

Very common hypertension; common arterial or venous thromboembolic events; occasional myocardial infarction or heart failure; rare QT interval prolongation.

Other Adverse Effects:

Hypothyroidism, weakness/asthenia, epistaxis, hypophosphatemia, headache, proteinuria and peripheral edema.

Contraindications to Pazopanib:

• Severe hepatic impairment
• Pregnancy and lactation
• Discontinue Pazopanib for persistent or recurrent grade 3–4 toxicity despite dose modifications
• Pause perioperatively, until wound healing is complete.

Drug–Drug Interactions with Pazopanib:

Avoid strong CYP3A4 inhibitors or inducers when possible; if unavoidable, monitor closely and consider dose adjustment. Acid-reducing therapies (PPIs/H2 blockers) can substantially decrease pazopanib absorption and should be avoided or time-separated.

Dosing of Pazopanib:

Administer 800 mg orally once daily without planned treatment breaks; take on an empty stomach. For treatment-related adverse effects, reduce the dose in 200 mg steps.

Monitoring During Therapy:

Perform regular evaluations: complete blood count with differential; electrolytes including phosphate; liver tests including bilirubin; lipase; coagulation; blood glucose; serum creatinine/eGFR; urinalysis for proteinuria; thyroid function (TSH); skin and oral mucosa assessment; and blood pressure at baseline and periodically. Consider ECG monitoring for QT interval.

Supportive Care:

Use loperamide for diarrhea; employ regular mouth rinses for mucositis; for hand–foot reaction, reduce mechanical stress and use emollients (e.g., urea-based creams) and, if needed, topical corticosteroids; treat hypertension according to guidelines; replace thyroid hormone for hypothyroidism. If toxicity does not improve, consider dose reduction or treatment interruption.

References

Sternberg, C. N.; Davis, I. D.; Mardiak, J.; Szczylik, C.; Lee, E.; Wagstaff, J.; Barrios, C. H.; Salman, P.; Gladkov, O. A.; Kavina, A.; Zarbá, J. J.; Chen, M.; McCann, L.; Pandite, L.; Roychowdhury, D. F. & Hawkins, R. E. Pazopanib in locally advanced or metastatic renal cell carcinoma: results of a randomized phase III trial.
J Clin Oncol 2010, 28, 1061-1068.

  Deutsche Version: Nebenwirkungen, Kontraindikationen und Dosierung von Pazopanib

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