Osimertinib
TAGRISSO
What it isThird-generation EGFR tyrosine kinase inhibitor; EGFR-mutant lung cancer.
Why this oneIt targets the T790M resistance mutation and penetrates the CNS, so it treats brain metastases.
What limits itQT prolongation and rare interstitial lung disease and cardiomyopathy. CYP3A4-dependent.
FDA-approved for
- EGFR+ lung cancer (2015)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Adjuvant early-stage NSCLC (EGFR ex19del/L858R) | Adults | 80 mg QD | 80 mg QD | 80 mg QD |
| Stage III unresectable NSCLC after chemoradiation (EGFR ex19del/L858R) | Adults | 80 mg QD | 80 mg QD | 80 mg QD |
| Metastatic NSCLC, incl. T790M+ (EGFR); monotherapy or + pemetrexed/platinum | Adults | 80 mg QD | 80 mg QD | 80 mg QD |
Renal No adjustment for CLcr 15-89 mL/min; no recommended dose for ESRD (CLcr <15)
Hepatic No adjustment for mild-moderate (Child-Pugh A/B); no recommended dose for severe
Instructions
- Take with or without food
- May disperse tablet in 60 mL non-carbonated water (or via NG tube) if unable to swallow; do not crush, heat, or ultrasonicate
- Missed dose: skip and take next dose as scheduled
Cautions
- Interstitial lung disease/pneumonitis (can be fatal)
- QTc interval prolongation
- Cardiomyopathy / decreased LVEF
- Keratitis
- Erythema multiforme major, SJS, TEN
- Cutaneous vasculitis
- Aplastic anemia
- Embryo-fetal toxicity
Adverse reactions
- Diarrhea
- Rash
- Musculoskeletal pain
- Nail toxicity
- Dry skin
- Stomatitis
- Fatigue
- Leukopenia, lymphopenia, thrombocytopenia, anemia, neutropenia
Pregnancy Can cause fetal harm; use effective contraception during and 6 wks (females)/4 mo (males) after last dose
Lactation Do not breastfeed during treatment and for 2 weeks after last dose
NO BOXED WARNINGS
Principal riskInterstitial lung disease; QT prolongation
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2035 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Osimertinib ballicule
