Osimertinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2015
- First approval year
- 2015
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Osimertinib
- Molecular weight
- 499.62
- Structure (SMILES)
- C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C
- tagrisso
- Tagrisso
- 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
- CAS registry numbers
- 1421373-65-0
- ChEMBL ID
- CHEMBL3353410
- InChIKey
- DUYJMQONPNNFPI-UHFFFAOYSA-N
- PubChem compound IDs
- 71496458
- FDA ingredient codes (UNII)
- 3C06JJ0Z2O
- L01EB04
- L01XE
Sources for recorded values
- 1721559
- 1721560
- Applicant
- ASTRAZENECA
- Approval date
- 13 Nov 2015
- Application number
- NDA208065
- 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
- 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 name
- osimertinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- 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
- 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
- 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.
- 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.
- NCT01802632
- NCT02094261
- NCT02143466
- NCT02157883
- NCT02163733
- NCT02179671
- NCT02197247
- NCT02228369
- NCT02296125
- NCT02317016
- NCT02411448
- NCT02442349
- NCT02454933
- NCT02496663
- NCT02503722
- NCT02511106
- NCT02529995
- NCT02664935
- NCT02771314
- NCT02789345
- NCT02803203
- NCT02811354
- NCT02824952
- NCT02841579
- NCT02856893
And 126 more, listed on the interactive page.
- Dose
- 80 mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- With or without food
- 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
- 0310-1248
- 0310-1251
- 0310-1349
- 0310-1350
- Recorded assays
- 3,378
- Active assays
- 988
- Confirmatory
- Other
- Screening
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
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
- 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
- Neoplasm
In development for (11)
- Adenocarcinoma Phase 2
- Brain neoplasm Phase 1
- Carcinoma Phase 2
- Colorectal cancer Phase 2
- Glioblastoma Phase 2
- Lung adenocarcinoma Phase 2
- Lung cancer Phase 3
- Lung neoplasm Phase 3
- Melanoma Phase 3
- Non-small cell lung carcinoma Phase 3
- Squamous cell carcinoma Phase 2
Targets (1)
- EGFR Epidermal growth factor receptor erbB1 inhibitor