Drug · Small Molecule

Osimertinib

CI-DRUG-00000423Explore in graph →NCIt C116377 CHEMBL3353410 CIViC Approved

Regulatory

Approvals (16)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

emaRegulatory1 approval record · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
EU EMA	Lung Non-Small Cell Carcinoma	Tagrisso as monotherapy is indicated for: the adjuvant treatment after complete tumour resection in adult patients with stage IB-IIIA non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations (see section 5.1). the treatment of adult patients with locally advanced, unresectable NSCLC whose tumours have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations and whose disease has not progressed during or following platinum‑based chemoradiation therapy. the first-line treatment of adult patients with locally advanced or metastatic NSCLC with activating EGFR mutations. the treatment of adult patients with locally advanced or metastatic EGFR T790M mutation-positive NSCLC. Tagrisso is indicated in combination with: pemetrexed and platinum-based chemotherapy for the first-line treatment of adult patients with advanced NSCLC whose tumours have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations.accelerated	approved	Feb 1, 2016	ema

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 14 hours agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 4	119	49	36	206	16	CA, EU, US	Nov 13, 2015	Mar 4, 2013
Malignant Lung Neoplasm	Approved	Phase 4	95	41	26	165	6	EU, US	Nov 13, 2015	Mar 4, 2013
Malignant Breast Neoplasm	Phase2	Phase 2	2	1	0	3	0	—	—	Aug 17, 2015
Malignant Esophageal Neoplasm	Phase2	Phase 2	2	0	0	2

Curated evidence

Clinical evidence (62)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–50 of 62 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
EGFR G598V2
Afatinib + Erlotinib

Clinical trials

Trials with this intervention (223)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 101–150 of 223 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT07058519	A Study of Osimertinib-based Adaptive Treatment Guided by ctDNA EGFRm+ Monitoring in NSCLC	recruiting	Phase 2	250	Shanghai Chest HospitalOTHER	1	Nov 26, 2025	clinicaltrials
NCT02157883	Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of AZD9291, in Patients With EGFR Positive Non-small Cell Lung Cancer. Patients Will be Chosen From Those Who Have Already Been Prescribed an EGFR TKI Medicine (Such as Iressa or Tarceva)

Molecule

Record

Kind: Small Molecule
Mechanism: Epidermal growth factor receptor erbB1 inhibitor
Targets: 1 gene
UNII: 3C06JJ0Z2O
Aliases: 2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-, AZD 9291, AZD-9291, AZD9291, AZD-9291 FREE BASE, Mereletinib, Osimertinib, Osimertinib Mesylate, Tagrisso, TAGRISSO

Data updated 17 hours agoSource updated unknown

Identifiers

Codes (7)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EB04	OSIMERTINIB
ATC (WHO)	L01XE	Other antineoplastic agents; Protein kinase inhibitors
DIN (Health Canada)

BRAF G469A2
Osimertinib	Lung Adenocarcinoma	Predictive	D	Supports Resistance	5	rejected	EID10514 PC9 cells harboring an in-frame deletion in exon 19 of the EGFR gene were cultured in the presence of increasing concentrations of osimertinib. Three clones resistant to osimertinib were isolated and … (full text at CIViC) PMID 31502118 · La Monica et al., 2019 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	D	Supports Resistance	5	rejected	EID10515 PC9 cells harboring an in-frame deletion in exon 19 of the EGFR gene were cultured in the presence of increasing concentrations of osimertinib. Three clones resistant to osimertinib were isolated and … (full text at CIViC) PMID 31502118 · La Monica et al., 2019 · Open in CIViC	civic

EGFR C797S3
Erlotinib + OsimertinibCombination	Lung Adenocarcinoma	Predictive	D	Supports Sensitivity Response	3	submitted	EID8080 A genetically engineered mouse model of lung adenocarcinoma (LUAD) was created expressing human EGFR L858R transgene. A set of osimertinib resistant tumours were treated with 25mg/kg osimertinib and 2… (full text at CIViC) PMID 32193290 · Starrett et al., 2020 · Open in CIViC	civic
Osimertinib	Lung Adenocarcinoma	Predictive	D	Supports Resistance	4	submitted	EID8057 A genetically engineered mouse model of lung adenocarcinoma (LUAD) was created expressing human EGFR L858R transgene. Mice were treated with either daily 5mg/kg, followed by 25mg/kg after tumour recur… (full text at CIViC) PMID 32193290 · Starrett et al., 2020 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	B	Supports Resistance	3	accepted	EID964 An EGFR resistance mutation, C797S, was discovered by deep sequencing of cell-free plasma DNA (cfDNA) from patients with advanced lung cancer whose tumors had developed resistance to osimertinib. Expr… (full text at CIViC) PMID 25939061 · Thress et al., 2015 · Open in CIViC	civic

EGFR L718Q2
Erlotinib + OsimertinibCombination	Lung Adenocarcinoma	Predictive	D	Supports Sensitivity Response	3	submitted	EID8081 A genetically engineered mouse model of lung adenocarcinoma (LUAD) was created expressing human EGFR L858R transgene. A set of osimertinib resistant tumours were treated with 25mg/kg osimertinib and 2… (full text at CIViC) PMID 32193290 · Starrett et al., 2020 · Open in CIViC	civic
Osimertinib	Lung Adenocarcinoma	Predictive	D	Supports Resistance	4	submitted	EID8058 A genetically engineered mouse model of lung adenocarcinoma (LUAD) was created expressing human EGFR L858R transgene. Mice were treated with either daily 5mg/kg, followed by 25mg/kg after tumour recur… (full text at CIViC) PMID 32193290 · Starrett et al., 2020 · Open in CIViC	civic

EGFR L858R2
Osimertinib	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	4	submitted	EID8053 A 62 year old patient with 4 pack-year smoking history with back and flank pain was found to have metastatic lung adenocarcinoma by CT and MRI. Targeted NGS sequencing discovered an EGFR L858R mutatio… (full text at CIViC) PMID 32193290 · Starrett et al., 2020 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	accepted	EID4294 In an in vitro study using NCI-H3255 cells (EGFR L858R mutation), inhibition of EGFR phosphorylation was used as an assay to determine sensitivity to EGFR tyrosine kinase inhibitors. NCI-H3255 cells d… (full text at CIViC) PMID 24893891 · Cross et al., 2014 · Open in CIViC	civic

RAD51 Fusion3
Erlotinib + OsimertinibSequential	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	3	accepted	EID12370 This is a case report of 29-year-old diagnosed with metastatic adenocarcinoma of the left lung. The patient was treated with chemotherapy (cisplatin 75 mg/m2 and pemetrexed 500 mg/m2 every 3 weeks) an… (full text at CIViC) PMID 35399574 · Di Federico et al., 2022 · Open in CIViC	civic
Osimertinib	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	3	accepted	EID11021 Case report of a 30-year-old male with lung adenocarcinoma and metastasis to several organs, including several lesions in the brain. NGS assay (Foundation One CDX panel) detected the EGRF::RAD51 fusio… (full text at CIViC) PMID 35245845 · Copia Sperandio et al., 2022 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	3	accepted	EID12372 This is a case report of a 45-year-old male never smoker that was diagnosed with metastatic lung adenocarcinoma. The patient responded poorly to the initial chemoimmunotherapy (carboplatin, pemetrexed… (full text at CIViC) PMID 38525318 · Lai et al., 2024 · Open in CIViC	civic