> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/osimertinib-ea23982c-3bd5-4728-8d62-eb03035b3315
> Record changed: 2026-10-13

# Osimertinib

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

First approval year

2015

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

## Development status

**First approval year**

2015

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

**Drug name**

Osimertinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

**Molecular weight**

499.62

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

**Structure (SMILES)**

C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

### Brand names (2)

- tagrisso
- Tagrisso

### Other names (19)

- azd 9291
- azd 9291 free base
- Azd-9291
- AZD-9291
- AZD-9291 FREE BASE
- azd9291
- AZD9291
- mereletinib
- Mereletinib
- osimertinib
- Osimertinib
- osimertinib \[INN\]
- OSIMERTINIB \[MI\]
- OSIMERTINIB \[USAN\]
- Osimertinib \[WHO-DD\]
- osimertinib inn
- osimertinib mi
- osimertinib usan
- osimertinib who dd

## Identifiers

**CAS registry numbers**

- 1421373-65-0

**ChEMBL ID**

CHEMBL3353410

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

**InChIKey**

DUYJMQONPNNFPI-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

**PubChem compound IDs**

- 71496458

**FDA ingredient codes (UNII)**

- 3C06JJ0Z2O

### ATC classification codes (2)

- L01EB04
- L01XE

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3353410)

### RxNorm IDs (RxCUI) (2)

- 1721559
- 1721560

## Regulatory information

### United States

**Applicant**

ASTRAZENECA

**Approval date**

13 Nov 2015

**Application number**

NDA208065

### European Union

**Status**

Authorised

**Status date**

1 Feb 2016

**Authorisation date**

1 Feb 2016

**Approved indications**

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.

**Product number**

EMEA/H/C/004124

**Authorisation holder**

AstraZeneca AB

**Priority medicines scheme**

No

**Generic**

No

**Biosimilar**

No

**Generic medicines**

0

**Biosimilar medicines**

0

**Advanced therapy**

No

**Conditional approval**

No

**Additional monitoring**

No

**Accelerated assessment**

Yes

**Exceptional circumstances**

No

#### Therapeutic areas

- Carcinoma, Non-Small-Cell Lung

European medicines record

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/tagrisso)

### Other regulatory facts

**Patents**

0

**Designations**

8

**First in class**

No

**Fast track**

Yes

**Breakthrough designation**

Yes

**Orphan designation**

No

**Priority review**

Yes

**Orphan exclusivity**

No

**Accelerated approval**

Yes

**Availability**

Prescription only

## Pharmacology

### Drug classification

**Pharmacology name**

osimertinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (2)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
epidermal growth factor receptor

**Gene symbol**  
EGFR

**Protein identifier**  
P00533

**Median affinity**

6.31

**Affinity units**  
pIC50
- **Mechanism**  
Epidermal growth factor receptor erbB1 inhibitor

**Action type**  
Inhibitor

**Target**  
Epidermal growth factor receptor

**Protein identifier**  
P00533

### Open Targets mechanisms

- **Mechanism**  
Epidermal growth factor receptor erbB1 inhibitor

**Action type**  
Inhibitor

**Target**  
Epidermal growth factor receptor

### DrugCentral mechanisms

- **Action type**  
Inhibitor

**Gene symbol**  
EGFR

**Protein identifier**  
P00533

**Organism**  
Homo sapiens

**Target development level**  
Clinical

### Investigated indications (12)

- **Condition**  
Adenocarcinoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000228

**Subject identifier**  
D000230
- **Condition**  
Carcinoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000313

**Subject identifier**  
D002277
- **Condition**  
Glioblastoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000519

**Subject identifier**  
D005909
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Carcinoma, Squamous Cell

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000707

**Subject identifier**  
D002294
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Brain Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0003833

**Subject identifier**  
D001932
- **Condition**  
Adenocarcinoma of Lung

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0005288

**Subject identifier**  
D000077192
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179
- **Condition**  
Lung Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0008903

**Subject identifier**  
D008175
- **Condition**  
Lung Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0021117

**Subject identifier**  
D008175

### Open Targets indications (31)

- **Condition identifier**  
EFO\_0000313

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000519

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000756

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0003060
- **Condition identifier**  
EFO\_0003833

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0005288

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1001012

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001056

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005061

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005062

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005065

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005070

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005089

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005097

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005105

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005575
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005580

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008170

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008433

**Highest recorded phase**  
1

And 6 more, listed on the interactive page.

### Reported adverse events (30)

- **Event**  
acquired gene mutation

**Reports**  
178

**Reporting signal score**

919.378
- **Event**  
decreased appetite

**Reports**  
129

**Reporting signal score**

69.3201
- **Event**  
dermatitis acneiform

**Reports**  
41

**Reporting signal score**

94.5778
- **Event**  
diarrhoea

**Reports**  
252

**Reporting signal score**

50.1676
- **Event**  
disease progression

**Reports**  
110

**Reporting signal score**

84.3018
- **Event**  
drug resistance

**Reports**  
386

**Reporting signal score**  
1,168.27
- **Event**  
egfr gene mutation

**Reports**  
37

**Reporting signal score**

174.287
- **Event**  
electrocardiogram qt prolonged

**Reports**  
73

**Reporting signal score**

71.8517
- **Event**  
erythema multiforme

**Reports**  
38

**Reporting signal score**

55.716
- **Event**  
headache

**Reports**  
27

**Reporting signal score**

47.62
- **Event**  
hepatic function abnormal

**Reports**  
97

**Reporting signal score**

131.157
- **Event**  
interstitial lung disease

**Reports**  
185

**Reporting signal score**

319.364
- **Event**  
liver disorder

**Reports**  
59

**Reporting signal score**

55.9655
- **Event**  
lung disorder

**Reports**  
79

**Reporting signal score**

105.229
- **Event**  
lymphangiosis carcinomatosa

**Reports**  
19

**Reporting signal score**

66.9427
- **Event**  
malignant neoplasm progression

**Reports**  
615

**Reporting signal score**  
1,695.69
- **Event**  
malignant transformation

**Reports**  
30

**Reporting signal score**

141.383
- **Event**  
metastases to bone

**Reports**  
54

**Reporting signal score**

99.9758
- **Event**  
metastases to central nervous system

**Reports**  
100

**Reporting signal score**

268.899
- **Event**  
metastases to liver

**Reports**  
43

**Reporting signal score**

71.1637
- **Event**  
metastases to lung

**Reports**  
39

**Reporting signal score**

75.7304
- **Event**  
metastases to meninges

**Reports**  
41

**Reporting signal score**

148.01
- **Event**  
multiple-drug resistance

**Reports**  
19

**Reporting signal score**

42.5732
- **Event**  
pain

**Reports**  
16

**Reporting signal score**

47.3181
- **Event**  
paronychia

**Reports**  
74

**Reporting signal score**

226.95

And 5 more, listed on the interactive page.

### Trial references (151)

- NCT01802632  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01802632)
- NCT02094261  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02094261)
- NCT02143466  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02143466)
- NCT02157883  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02157883)
- NCT02163733  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02163733)
- NCT02179671  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02179671)
- NCT02197247  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02197247)
- NCT02228369  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02228369)
- NCT02296125  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02296125)
- NCT02317016  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02317016)
- NCT02411448  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02411448)
- NCT02442349  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02442349)
- NCT02454933  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02454933)
- NCT02496663  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02496663)
- NCT02503722  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02503722)
- NCT02511106  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02511106)
- NCT02529995  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02529995)
- NCT02664935  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02664935)
- NCT02771314  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02771314)
- NCT02789345  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02789345)
- NCT02803203  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02803203)
- NCT02811354  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02811354)
- NCT02824952  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02824952)
- NCT02841579  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02841579)
- NCT02856893  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02856893)

And 126 more, listed on the interactive page.

## Dosing

**Dose**

80 mg

**Route**

Oral

**How often**

Once daily

### Conditions of use

- With or without food

## Chemical properties

**Hydrogen bond acceptors**

8

**Hydrogen bond donors**

2

**Polar surface area**

87.55

**Calculated partition coefficient (ALogP)**

4.51

**Calculated partition coefficient (XLogP)**

3.7

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

10

**Heavy atoms**

37

**Molecular formula**

C28H33N7O2

**Monoisotopic mass**

499.26957332

**Natural product**

Yes

## National Drug Codes

- 0310-1248
- 0310-1251
- 0310-1349
- 0310-1350

## Evidence counts

**Recorded assays**

3,378

**Active assays**

988

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Pharmacologic actions

- Tyrosine Kinase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000092004.html)
- Antineoplastic Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html)

## Biological measurements

These details could not be displayed.

## Related records

### Trials (264)

- (HARMONY) Study of BLU-701 in EGFR-mutant NSCLC
- (SYMPHONY) Phase 1/2 Study Targeting EGFR Resistance Mechanisms in NSCLC
- 18F-FDG PET and Osimertinib in Evaluating Glucose Utilization in Patients with EGFR Activated Recurrent Glioblastoma
- A Clinical Study of JMT101 in Combination With Osimertinib Versus Osimertinib Alone as First-Line Treatment for Patients With Locally Advanced or Metastatic Non-Squamous Non-Small Cell Lung Cancer (NSCLC) Harboring Epidermal Growth Factor Receptor (EGFR) Sensitive Mutations
- A ctDNA-guided Phase II Trial of Osimertinib in Combination With Sacituzumab Tirumotecan in EGFR-mutated Advanced NSCLC Patients With Positive ctDNA After lead-in Osimertinib Monotherapy
- A Global Study to Assess the Effects of Osimertinib Following Chemoradiation in Patients With Stage III Unresectable Non-small Cell Lung Cancer (LAURA)
- A Global Study to Assess the Effects of Osimertinib in Participants With EGFRm Stage IA2-IA3 NSCLC Following Complete Tumour Resection
- A Molecular Profiling Study of Patients With EGFR Mutation-positive Locally Advanced or Metastatic NSCLC Treated With Osimertinib
- A Multicenter Phase II Randomized Trial of Limertinib Followed by Sintilimab and Chemotherapy vs. Limertinib Followed by Limertinib and Chemotherapy as Neoadjuvant Therapy in Resectable Stage II-IIIB EGFR-Mutant NSCLC
- A Phase 1a/1b Study to Determine the Recommended Phase 2 Dose, of Tepotinib in Participants With MET Alterations and Brain Tumors
- A Phase 2 Study of Osimertinib and S-1 in Treatment Resistant EGFR Mutant NSCLC
- A Phase 2 Study of Osimertinib in Combination With Selumetinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer
- A Phase I, Open-label Study to Assess Bioavailability of a Single Oral Dose of AZD9291 vs an IV Dose of \[14C\]AZD9291
- A Phase Ib/II Clinical Study of GH21 Capsules Combined With Osimertinib Mesylate Tablets in Patients With NSCLC
- [A Phase II Study of AK146D1 in Combination With AK112 in Advanced Non-Small Cell Lung Cancer](https://trialight.com/data/trial/a-phase-ii-study-of-ak146d1-in-combination-with-ak112-in-01bd3edc-5e3c-43c7-b785-486fd26d7726.md)
- A Phase Ⅲ Clinical Study of SYS6010 in Combination With Osimertinib in Patients With Locally Advanced or Metastatic NSCLC
- A Pilot Study of Dacomitinib With or Without Osimertinib for Patients With Metastatic EGFR Mutant Lung Cancers With Disease Progression on Osimertinib.
- A Precision Medicine Approach (SMMART-ACT) for the Treatment of Patients With Advanced Sarcoma, Prostate, Breast, Ovarian or Pancreatic Cancer
- A Prospective Study of Pembrolizumab Combining Chemotherapy in Advanced NSCLC Patients With EGFR Exon 21 Point Mutation.
- A Randomised Phase II Trial of Osimertinib With or Without SRS for EGFR Mutated NSCLC With Brain Metastases

### Approved for (2)

- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- Neoplasm

### In development for (11)

- [Adenocarcinoma](https://trialight.com/data/condition/adenocarcinoma-b5c321d1-7c49-5bf9-abd0-dfa99dbd5f29.md) Phase 2
- [Brain neoplasm](https://trialight.com/data/condition/brain-neoplasm-b3dac71b-1d7b-5a65-8f64-89821506ad41.md) Phase 1
- [Carcinoma](https://trialight.com/data/condition/carcinoma-575e4c82-5fa5-5455-b1b7-30972eca1a2f.md) Phase 2
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2
- Glioblastoma Phase 2
- [Lung adenocarcinoma](https://trialight.com/data/condition/lung-adenocarcinoma-1cff3624-1dd5-5076-89a7-1f8a28c087a6.md) Phase 2
- [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 3
- [Lung neoplasm](https://trialight.com/data/condition/lung-neoplasm-d4ce75ac-7517-5ab7-9f47-34c0f7b81786.md) Phase 3
- [Melanoma](https://trialight.com/data/condition/melanoma-457e9de6-dcd9-56fb-be48-0290fb4386ef.md) Phase 3
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 3
- [Squamous cell carcinoma](https://trialight.com/data/condition/squamous-cell-carcinoma-44944de3-3c1f-5714-9da2-a28db7d896c2.md) Phase 2

### Targets (1)

- [EGFR](https://trialight.com/data/target/egfr-5c134fbe-bf90-5792-81e3-542be53c2be7.md) Epidermal growth factor receptor erbB1 inhibitor

---

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