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Osimertinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplasticATC null
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
[MHRA/CHM advice]. . Opioids: reminder of risk of potentially fatal respiratory
FDA category + note
Top interactionssee all 12
  • AbarelixSevereDatabaseDDInter
  • AbirateroneSevereDatabaseDDInter
  • AdalimumabSevereDatabaseDDInter
  • AdenosineSevereDatabaseDDInter

Mechanism

Osimertinib is an inhibitor of specific mutant forms of Epidermal Growth Factor Receptor (EGFR) tyrosine kinase. It targets EGFR exon 19 deletion or exon 21 (T790M, L858R) substitution mutations, thereby inhibiting downstream signaling pathways that promote cancer growth.

Indications

untreated EGFR mutation-positive non-small-cell lung cancerlung NSCLC (EGFR T790M mutation)first-line treatment of patients with metastatic NSCLC and adjuvant therapy after resection of NSCLC with EGFR exon 19 deletions or exon 21 L858R mutationspatients with metastatic NSCLC that progressed after prior EGFR TKI treatment and is positive for the EGFR T790M mutation

Dosing

Adult
EGFR T790M mutation-positive NSCLC: 80 mg once daily.

Pharmacokinetics

Half-life
48 h
Metabolism
CYP3A (substrate)
Excretion
primarily in the feces, to a lesser extent in the urine

Side effects

Common
DiarrheaSkin rashFatigueAnorexia
Serious
  • Pulmonary toxicity in the form of interstitial lung disease (ILD)
  • Cardiomyopathy and CHF
  • QT prolongation
  • interstitial lung disease
  • QTc prolongation
  • left ventricular dysfunction

Pregnancy & lactation

Pregnancy

[MHRA/CHM advice]. . Opioids: reminder of risk of potentially fatal respiratory

Drug interactions

Abarelix
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Abiraterone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Adenosine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alfuzosin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Alimemazine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amiodarone
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amisulpride
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amitriptyline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amoxapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Anagrelide
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Related guidelines

Other Tyrosine Kinase Inhibitor drugs

Ask House about Osimertinib

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Sources: Goodman & Gilman 14e, BNF·Verified: 2026-05-10 · House clinical team