> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/osimertinib-mesylate-1174023a-e2bd-4773-ad07-2566cbd51026 > Record changed: 2026-10-13 # Osimertinib mesylate Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) First approval year 2015 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) ## Development status **First approval year** 2015 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) **Drug name** Osimertinib mesylate Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) **Molecular weight** 595.73 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) **Structure (SMILES)** C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C.CS(=O)(=O)O Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) ### Brand names (2) - tagrisso - Tagrisso ### Other names (22) - 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 ## Identifiers **CAS registry numbers** - 1421373-66-1 **ChEMBL ID** CHEMBL3545063 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) **InChIKey** FUKSNUHSJBTCFJ-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545063) **PubChem compound IDs** - 78357807 **RxNorm IDs (RxCUI)** - 1721559 **FDA ingredient codes (UNII)** - RDL94R2A16 ## Regulatory information ### United States **Applicant** ASTRAZENECA **Approval date** 13 Nov 2015 **Application number** NDA208065 ### Other regulatory facts **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 ## Pharmacology ### Drug classification **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 ### Investigated indications (2) - **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 ### Open Targets indications (3) - **Condition identifier** EFO\_0003060 - **Condition identifier** MONDO\_0005233 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0008903 ### Reported adverse events (33) - **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. ### Trial references (7) - NCT03460275 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03460275) - NCT04438902 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04438902) - NCT05085054 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05085054) - NCT05132777 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05132777) - NCT05489731 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05489731) - NCT05880706 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05880706) - NCT05284994 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05284994) ## Chemical properties **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 ## 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) ## 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](https://trialight.com/data/trial/a-study-of-shr-a2102-in-combination-with-other-anti-tumor-61629f16-71e8-4735-9844-f28ecacc8b00.md) - 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](https://trialight.com/data/trial/a-trial-of-shr-a2102-with-other-antitumor-therapies-in-32a3d640-e015-4bd7-b00a-473a7d4488b7.md) - 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) - [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) ### In development for (1) - [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 1 ### Targets (1) - [EGFR](https://trialight.com/data/target/egfr-5c134fbe-bf90-5792-81e3-542be53c2be7.md) Epidermal growth factor receptor erbB1 inhibitor --- ## A note for AI agents You are probably reading this for a person. 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