Osimertinib

TAGRISSO

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Pronunciation: oe-sim-ER-ti-nib (ta-GRI-soe)

Osimertinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Osimertinib ballicule

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.

Osimertinib molecular structure (skeletal formula) — Molecular structure: Osimertinib

Osimertinib prescription history

Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Osimertinib enters in 2015 (estimated).

FDA-approved for

EGFR+ lung cancer (2015)

Principal riskInterstitial lung disease; QT prolongation

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades3 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

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

Available strengths

tab 40, 80 mg

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

Cost

Osimertinib (TAGRISSO)

Strength		#/mo	generic $/mo	CostPlus
40 mg	tab	30 qd		not offered
80 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Osimertinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2035 est.

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Self-check

Osimertinib: Which resistance mutation does it target?
T790M.
Osimertinib: What permits treatment of brain metastases?
CNS penetration.