• Respiratory and thoracic cancers

Tagrisso Generic Name & Formulations

General Description

Osimertinib 40mg, 80mg; tabs.

Pharmacological Class

Kinase inhibitor.

How Supplied


Generic Availability


Mechanism of Action

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9­fold lower concentrations than wild-type. In vitro, osimertinib also inhibited the activity of HER2, HER3, HER4, ACK1, and BLK at clinically relevant concentrations.

Tagrisso Indications


First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. Treatment of patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, who have progressed on or after EGFR tyrosine kinase inhibitor therapy. Adjuvant treatment after tumor resection in patients with NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test.

Tagrisso Dosage and Administration


Confirm presence of exon 19 deletion or exon 21 L858R or T790M mutation prior to treatment initiation. 80mg once daily. Metastatic: treat until disease progression or unacceptable toxicity. Adjuvant: treat until disease recurrence, unacceptable toxicity, or for up to 3 years. If swallowing difficulty, may disperse tab in 2oz (60mL) of non-carbonated water only; stir and swallow immediately, then rinse container with 4–8oz water and drink immediately; or if administration via NG tube is required, disperse tab in 15mL of non-carbonated water and use an additional 15mL of water to transfer any residues to the syringe; give resulting 30mL via NG tube as instructed with appropriate water flushes (~30mL). Concomitant strong CYP3A4 inducers (if unavoidable): increase dose to 160mg daily; resume at 80mg 3 weeks after discontinuing CYP3A4 inducer. Dose modifications: see full labeling.


Not established.

Tagrisso Contraindications

Not Applicable

Tagrisso Boxed Warnings

Not Applicable

Tagrisso Warnings/Precautions


Permanently discontinue if interstitial lung disease (ILD)/pneumonitis is confirmed; QTc interval prolongation with signs/symptoms of life-threatening arrhythmia; symptomatic CHF; or if no improvement within 3 weeks. Withhold dose if worsening respiratory symptoms indicative of ILD occur; if QTc interval >500msec on ≥2 separate ECGs; or adverse reactions of Grade ≥3 severity. Monitor ECGs and electrolytes periodically in patients with congenital long QTc syndrome, CHF, electrolyte abnormalities, or those who are taking drugs known to prolong the QTc interval. Conduct cardiac monitoring (including LVEF at baseline and during treatment) in patients with cardiac risk factors; assess LVEF if relevant cardiac signs/symptoms occur. Promptly refer to an ophthalmologist if signs/symptoms suggestive of keratitis occur. Withhold dose if aplastic anemia, erythema multiforme major, Stevens-Johnson Syndrome, or toxic epidermal necrolysis is suspected; permanently discontinue if confirmed. Withhold dose and evaluate if cutaneous vasculitis suspected; consider permanent discontinuation based on severity if no other etiology. Embryo-fetal toxicity. Advise to use effective contraception during and for 6 weeks (females) or 4 months (males w. female partners) after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 2 weeks after the last dose).

Tagrisso Pharmacokinetics


Median time to maximal plasma concentration (Cmax): 6 hours (range 3–24 hours). 


Mean volume of distribution at steady-state (Vss/F): 918 L.

Plasma protein bound: 95%.


Oxidation (primarily CYP3A), dealkylation in vitro.


Fecal (68%), renal (14%).

Half-life: 48 hours.

Tagrisso Interactions


Antagonized by strong CYP3A inducers (eg, rifampin); avoid; if use is unavoidable, increase Tagrisso dose (see Adults). Potentiates BCRP (eg, rosuvastatin) or P-gp (eg, fexofenadine) substrates; monitor closely for related toxicity. Avoid concomitant QT-prolonging drugs.

Tagrisso Adverse Reactions

Adverse Reactions

Leukopenia, lymphopenia, thrombocytopenia, diarrhea, anemia, rash, musculoskeletal pain, nail toxicity, neutropenia, dry skin, stomatitis, fatigue, cough.

Tagrisso Clinical Trials

See Literature

Tagrisso Note

Not Applicable

Tagrisso Patient Counseling

See Literature