Osimertinib
 | |
| Systematic (IUPAC) name | |
|---|---|
|
N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide | |
| Clinical data | |
| Trade names | Tagrisso |
| Routes of administration | Oral tablets |
| Pharmacokinetic data | |
| Protein binding | probably high[1] |
| Metabolism | oxidation (CYP3A) |
| Biological half-life | 48 hours |
| Excretion | feces (68%), urine (14%) |
| Identifiers | |
| CAS Number | 1421373-65-0 |
| PubChem | CID 71496458 |
| ChemSpider | 31042598 |
| UNII | 3C06JJ0Z2O |
| ChEBI |
CHEBI:90943  |
| Chemical data | |
| Formula | C28H33N7O2 |
| Molar mass | 499.6 g/mol |
| |
Osimertinib (previously known as mereletinib[2] and AZD9291; trade name Tagrisso) is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug[3][4] developed by AstraZeneca Pharmaceuticals - for mutated EGFR cancers.
Approvals and indications
In November 2015, after a Priority Review, the US FDA granted accelerated approval to osimertinib for the treatment of metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA-approved test, which has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.[5][6]
The FDA approval made reference to two clinical trials, in which an EGFR T790M mutation was confirmed by a Cobas EGFR mutation test; osimertinib was given as 80 mg once daily.[1][7]
References
- 1 2 "Tagrisso (osimertinib) Tablet, for Oral Use. Full Prescribing Information" (PDF). AstraZeneca Pharmaceuticals LP, Wilmington, DE 19850. Retrieved 16 November 2015.
- ↑ "Proposed INN: List 113" (PDF). International Nonproprietary Names for Pharmaceutical Substances (INN) 29 (2): 285. 2015. Retrieved 16 November 2015.
- ↑ Ayeni D, Politi K, Goldberg SB (2015). "Emerging Agents and New Mutations in EGFR-Mutant Lung Cancer". Clin. Cancer Res. 21 (17): 3818–20. doi:10.1158/1078-0432.CCR-15-1211. PMID 26169963.
- ↑ Tan CS, Gilligan D, Pacey S (2015). "Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer". Lancet Oncol. 16 (9): e447–59. doi:10.1016/S1470-2045(15)00246-6. PMID 26370354.
- ↑ U.S. Food and Drug Administration. Hematology/Oncology (Cancer) Approvals & Safety Notifications.
- ↑ Xu M, Xie Y, Ni S, Liu H (2015). "The latest therapeutic strategies after resistance to first generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) in patients with non-small cell lung cancer (NSCLC)". Ann Transl Med 3 (7): 96. doi:10.3978/j.issn.2305-5839.2015.03.60. PMC 4430733. PMID 26015938.
- ↑ U.S. Food and Drug Administration. "Osimertinib".
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