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VEGFR Tyrosine Kinase Inhibitor (Specialist Oncology Drug)

Axitinib

Brand names: Inlyta

Adult dose

Dose: Refer to BNF, SmPC, and current SACT protocol
Route: Oral
Frequency: As per SACT/MDT guidance (typically 5 mg twice daily)

Clinical pearls

  • Indicated for: (1) second-line treatment of renal cell carcinoma (RCC) after prior therapy; (2) first-line RCC in combination with pembrolizumab (KEYNOTE-426) or avelumab
  • NICE TA333 (2015): axitinib monotherapy for second-line advanced RCC; NICE TA645 (2020): axitinib + pembrolizumab for first-line advanced RCC
  • Hypertension management is key — can actually be a surrogate for good drug exposure; treat with antihypertensives and continue axitinib
  • Titrate dose based on blood pressure and tolerability (5 mg → 7 mg → 10 mg BD if tolerated and BP controlled)
  • Thyroid function should be monitored (hypothyroidism in ~30%)
  • VEGFR inhibitor class: antiangiogenic — wound healing impaired; hold perioperatively

Contraindications

  • See SmPC
  • Untreated brain metastases (relative)
  • Major surgery within 24 hours (bleeding risk)

Side effects

  • Hypertension (very common — manage to allow continued treatment)
  • Diarrhoea
  • Fatigue
  • Nausea
  • Palmar-plantar erythrodysaesthesia (hand-foot syndrome)
  • Hypothyroidism
  • Mucositis
  • Proteinuria
  • Hepatotoxicity
  • Arterial thromboembolic events

Interactions

  • Strong CYP3A4/5 inhibitors — increase axitinib levels; reduce dose
  • Strong CYP3A4/5 inducers (rifampicin, phenytoin) — reduce axitinib levels; avoid
  • QT-prolonging drugs — monitor

Monitoring

  • Blood pressure (twice daily initially, then regularly — target <140/90 mmHg)
  • Tumour response per SACT protocol
  • Thyroid function (TSH) every 6–8 weeks
  • Urine protein (24-hour urine or protein:creatinine ratio)
  • LFTs
  • FBC

Reference: BNF; NICE TA333 (Axitinib for renal cell carcinoma after prior therapy, 2015); NICE TA645 (Axitinib + pembrolizumab for first-line advanced RCC, 2020); KEYNOTE-426 trial (NEJM 2019); ESMO RCC Guidelines; https://bnf.nice.org.uk/drugs/axitinib/. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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