Osimertinib mesylate
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 mesylate
- Molecular weight
- 595.73
- Structure (SMILES)
- C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C.CS(=O)(=O)O
- tagrisso
- Tagrisso
- azd 9291 mesylate
- AZD-9291 MESYLATE
- azd9291 mesylate
- AZD9291 mesylate
- mereletinib mesilate
- Mereletinib mesilate
- mereletinib mesylate
- Mereletinib mesylate
- osimertinib mesilate
- Osimertinib mesilate
- OSIMERTINIB MESILATE [JAN]
- Osimertinib mesilate [WHO-DD]
- osimertinib mesilate jan
- osimertinib mesilate who dd
- osimertinib mesylate
- Osimertinib mesylate
- OSIMERTINIB MESYLATE [MI]
- OSIMERTINIB MESYLATE [ORANGE BOOK]
- OSIMERTINIB MESYLATE [USAN]
- osimertinib mesylate mi
- osimertinib mesylate orange book
- osimertinib mesylate usan
- CAS registry numbers
- 1421373-66-1
- ChEMBL ID
- CHEMBL3545063
- InChIKey
- FUKSNUHSJBTCFJ-UHFFFAOYSA-N
- PubChem compound IDs
- 78357807
- RxNorm IDs (RxCUI)
- 1721559
- FDA ingredient codes (UNII)
- RDL94R2A16
- Applicant
- ASTRAZENECA
- Approval date
- 13 Nov 2015
- Application number
- NDA208065
- Patents
- 5
- Designations
- 0
- Earliest recorded loss of exclusivity
- 26 Nov 2042
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Drug name stem
- -tinib
Administration routes
- Oral
Mechanisms of action
- 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
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Lung Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0008903
- Subject identifier
- D008175
- Condition identifier
- EFO_0003060
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0008903
- Event
- acquired gene mutation
- Reports
- 182
- Reporting signal score
- 943.259
- Event
- decreased appetite
- Reports
- 129
- Reporting signal score
- 68.8584
- Event
- dermatitis acneiform
- Reports
- 41
- Reporting signal score
- 94.3823
- Event
- diarrhoea
- Reports
- 254
- Reporting signal score
- 50.9625
- Event
- disease progression
- Reports
- 110
- Reporting signal score
- 83.8677
- Event
- drug resistance
- Reports
- 397
- Reporting signal score
- 1,211.11
- Event
- egfr gene mutation
- Reports
- 37
- Reporting signal score
- 174.104
- Event
- ejection fraction decreased
- Reports
- 35
- Reporting signal score
- 39.9131
- Event
- electrocardiogram qt prolonged
- Reports
- 73
- Reporting signal score
- 71.5471
- Event
- erythema multiforme
- Reports
- 38
- Reporting signal score
- 55.5452
- Event
- gene mutation
- Reports
- 16
- Reporting signal score
- 40.0445
- Event
- headache
- Reports
- 28
- Reporting signal score
- 46.6156
- Event
- hepatic function abnormal
- Reports
- 97
- Reporting signal score
- 130.724
- Event
- interstitial lung disease
- Reports
- 187
- Reporting signal score
- 323.856
- Event
- liver disorder
- Reports
- 59
- Reporting signal score
- 55.7218
- Event
- lung disorder
- Reports
- 79
- Reporting signal score
- 104.878
- Event
- lymphangiosis carcinomatosa
- Reports
- 19
- Reporting signal score
- 66.8498
- Event
- malignant neoplasm progression
- Reports
- 618
- Reporting signal score
- 1,703.92
- Event
- malignant transformation
- Reports
- 30
- Reporting signal score
- 141.235
- Event
- metastases to bone
- Reports
- 54
- Reporting signal score
- 99.7241
- Event
- metastases to central nervous system
- Reports
- 100
- Reporting signal score
- 268.412
- Event
- metastases to liver
- Reports
- 43
- Reporting signal score
- 70.9667
- Event
- metastases to lung
- Reports
- 39
- Reporting signal score
- 75.5479
- Event
- metastases to meninges
- Reports
- 41
- Reporting signal score
- 147.809
- Event
- multiple-drug resistance
- Reports
- 19
- Reporting signal score
- 42.4832
And 8 more, listed on the interactive page.
- NCT03460275
- NCT04438902
- NCT05085054
- NCT05132777
- NCT05489731
- NCT05880706
- NCT05284994
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 87.55
- Calculated partition coefficient (ALogP)
- 4.51
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 10
- Heavy atoms
- 42
- Molecular formula
- C29H37N7O5S
- Monoisotopic mass
- 595.25768848
- Natural product
- No
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
Related records
Trials (18)
- A Study Evaluating Furmonertinib Plus Platinum-based Doublet Chemotherapy Versus Osimertinib in Patients With Epidermal Growth Factor Receptor (EGFR) Sensitizing Mutation-Positive Non-squamous Non-Small Cell Lung Cancer (NSCLC) and Brain Metastases
- A Study of APG-1252 Plus Osimertinib(AZD9291) in EGFR TKI Resistant NSCLC Patients
- A Study of BL-B01D1 and BL-B01D1 in Combination With Osimertinib Mesylate Tablets in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer
- A Study of BL-B01D1 in Combination With Osimertinib Mesylate Tablets in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer
- A Study of SHR-A2102 in Combination With Other Anti-tumor Therapies for Resectable Non-small Cell Lung Cancer
- A Study to Assess the Effect of Food on the Pharmacokinetics of TY-9591 in Healthy Volunteers
- A Study to Evaluate the Efficacy and Safety of Glumetinib Combined With Osimertinib Mesylate Versus Platinum-based Doublet Chemotherapy in Non-Small Cell Lung Cancer Patients After Resistance to EGFR-TKIs
- A Study to Evaluate the Efficacy of Osimertinib in Patients With EGFR-sensitive Mutated Non-small Cell Lung Cancer Progression After Receiving Adjuvant Targeted Therapy Following Radical Surgery
- A Trial of SHR-A2102 With Other Antitumor Therapies in Advanced Solid Tumors
- Efficacy and Safety of JMT101 Combined With Osimertinib in Patients With Non-Small Cell Lung Cancer
- Glumetinib Combined With Osimertinib Treatment for Non-Small Cell Lung Cancer Patients
- Osimertinib as First-line Therapy for Patients With Late-stage Lung Cancer
- Osimertinib Combined With Anlotinib in EGFR T790M Mutated NSCLC Patients With Progression on Osimertinib Treatment
- Phase II Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Antitumor Activity of ALK202 for Injection in Combination With Drugs in NSCLC Participants.
- Salvage Surgery Following Downstaging of Advanced Non-small Cell Lung Cancer by Targeted Therapy (SDANT)
- Study of ONO-7475 in Combination With Osimertinib in EGFR Gene Mutation-positive Non-small Cell Lung Cancer
- TQ-B3525 Tablets Combined With Osimertinib Mesylate Tablets in the Treatment of Advanced Non-Small Cell Lung Cancer
- VIC-1911 Combined With Osimertinib for EGFR -Mutant Non-small Cell Lung Cancer
Approved for (1)
In development for (1)
- Lung cancer Phase 1
Targets (1)
- EGFR Epidermal growth factor receptor erbB1 inhibitor