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FLT3 Inhibitor Pregnancy: Contraindicated — embryotoxic; effective contraception required during and for 6 months after treatment

Gilteritinib

Brand names: Xospata

Adult dose

Dose: 120 mg once daily
Route: Oral
Frequency: Once daily
Max: 120 mg/day
Relapsed/refractory AML with FLT3 mutation (ITD or TKD); FLT3 mutation testing mandatory; continue until disease progression or unacceptable toxicity or stem cell transplant bridging

Paediatric dose

Dose: Not established N/A/kg
Route: N/A
Frequency: N/A
Max: N/A
Not licensed in paediatrics

Dose adjustments

Renal

No dose adjustment required

Hepatic

Mild-moderate: no adjustment; severe hepatic impairment: limited data

Paediatric weight-based calculator

Not licensed in paediatrics

Clinical pearls

  • ADMIRAL trial (Perl et al. NEJM 2019): gilteritinib significantly improved OS vs salvage chemotherapy in R/R FLT3-mutated AML (9.3 vs 5.6 months) — first FLT3 inhibitor to improve OS in R/R setting
  • Differentiation syndrome is class effect; monitor for fever, respiratory distress, weight gain, pericardial/pleural effusions — treat with dexamethasone; hold gilteritinib if grade ≥3
  • MHRA 2020 approved; NICE TA666 for R/R FLT3-mutated AML; FLT3 prevalence ~30% of AML (ITD most common) — companion diagnostic testing required
  • PRES: rare but serious — presents with headache, seizures, visual disturbance, hypertension; diagnose with MRI; permanently discontinue gilteritinib if confirmed
  • Bridge to allogeneic SCT: gilteritinib can achieve composite remission in ~55% patients, enabling transplantation — often used as bridging therapy with intent to transplant in eligible patients

Contraindications

  • No FLT3 mutation on testing
  • Known QTc >500 ms at baseline
  • Known hypersensitivity

Side effects

  • Differentiation syndrome
  • QTc prolongation
  • Posterior reversible encephalopathy syndrome (PRES)
  • Pancreatitis
  • Hepatotoxicity
  • Fatigue
  • Nausea
  • Myalgia

Interactions

  • Strong CYP3A4 inhibitors — increase gilteritinib exposure; monitor or avoid
  • P-gp inhibitors — may increase gilteritinib levels
  • QTc-prolonging agents — additive QTc risk
  • Combined P-gp and strong CYP3A4 inducers (rifampicin) — avoid; substantially reduces gilteritinib levels

Monitoring

  • ECG (baseline, day 8, then monthly)
  • FBC and differential (weekly ×4, then biweekly, then monthly)
  • LFTs and amylase/lipase
  • Blood pressure
  • Neurological assessment (PRES symptoms)
  • MRD testing (FLT3)

Reference: BNFc; BNF 90; ADMIRAL trial (Perl et al. NEJM 2019); NICE TA666; MHRA SPC Xospata. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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