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Pazopanib

  • VEGFR multikinase inhibitorsVEGFR multikinase inhibitors
  • High alertAn error with this medicine can cause serious harm: double checks and protocols are used.
  • Pregnancy: avoidAvoid in pregnancy. Can harm the fetus; pregnancy is avoided during treatment, and the team is told about pregnancy or breastfeeding.

An oral VEGFR multikinase inhibitor for advanced kidney cancer and soft-tissue sarcoma. Boxed warning: liver damage; acid blockers cut its absorption.

Updated

Also called: pazopanib hydrochloride

Quick facts

Group
VEGFR multikinase inhibitors
Target
VEGFR1-3, PDGFR, FGFR and KIT tyrosine kinases
Used for
Advanced renal cell carcinoma
Key effects
Diarrhoea · Hypertension · Change of hair colour
Monitor
Liver tests before starting · Blood pressure
ATC
L01EX03

No doses: the clinician sets them by the current guideline.

Mechanism of action

No pazopanib structure was used: the figure shows axitinib, which occupies the same ATP pocket of human VEGFR2.

Target in 3D: VEGFR1-3, PDGFR, FGFR and KIT tyrosine kinases. PDB structure 4AG8 (RCSB PDB, public domain). View the structure at RCSB PDB

Pazopanib blocks the kinase of VEGFR1-3 together with FGFR, KIT, PDGFR and other kinases that support angiogenesis and tumour growth. In metastatic kidney cancer it is as effective as sunitinib and usually better tolerated.

  1. Blocks VEGFR1-3, PDGFR, FGFR and KIT kinases
  2. Tumour angiogenesis and growth signals stop

Indications

Adverse effects

Common

  • Diarrhoea, nausea, taste changes, weight loss
  • Hypertension
  • Change of hair colour, lighter patches of skin, brittle nails
  • Fatigue and muscle or joint pain
  • Red, tender palms and soles

Contraindications

  • Avoided when liver tests are already abnormal

Key interactions

Proton pump inhibitors and H2 blockers (omeprazole, esomeprazole, famotidine)
Lower its absorption; not started without the treating team's advice.
Strong CYP3A4 inhibitors (clarithromycin, itraconazole, ketoconazole, ritonavir) and grapefruit
Raise its levels and its toxicity.
Strong CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, St John's wort)
Lower its levels and can make it fail.
Other QT-prolonging drugs (some antiarrhythmics, macrolides, antipsychotics)
Additive risk of QT prolongation and arrhythmia.

What is monitored

  • Liver tests before starting, frequently in the first months, then regularly
  • Blood pressure
  • ECG and electrolytes

Administration and safety

  • Oral tablets once daily on an empty stomach, away from meals, swallowed whole and not crushed.
  • Grapefruit, its juice and St John's wort are avoided because they change its levels.
  • Check the medication list for acid-reducing drugs.

Pregnancy and breastfeeding

Avoid in pregnancy. Can harm the fetus; pregnancy is avoided during treatment, and the team is told about pregnancy or breastfeeding.

Nursing care

  • Make sure liver tests are done on schedule; teach to report jaundice or dark urine.
  • Measure blood pressure at every visit and teach home monitoring if ordered.
  • Explain that hair colour may change.
  • Teach to report bleeding, black stools, vomiting blood, severe abdominal pain, chest pain or stroke symptoms at once.

Pharmacokinetics

Absorption
Oral tablets, on an empty stomach; drugs that lower stomach acid reduce its absorption.
Metabolism
Liver, mostly CYP3A.
Half-life
About 31 hours.

Test yourself

Think of the answer, then tap the question to see it.

Why are proton pump inhibitors a problem with pazopanib?

They reduce stomach acid and with it pazopanib absorption.

Which test schedule follows pazopanib's boxed warning?

Liver tests before starting, frequently during the first months and regularly afterwards.

Besides kidney cancer, which tumour is pazopanib used for?

Advanced soft-tissue sarcoma after chemotherapy.

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Connections

← Back to the class: VEGFR multikinase inhibitors

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Pazopanib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2016); Pazopanib Hydrochloride - NCI (National Cancer Institute, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.