Osimertinib
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| Systematic (IUPAC) name | |
|---|---|
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N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide
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| Clinical data | |
| Trade names | Tagrisso |
| AHFS/Drugs.com | entry |
| Legal status |
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| 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 |
| DrugBank | DB09330 |
| ChemSpider | 31042598 |
| UNII | 3C06JJ0Z2O |
| KEGG | D10766 |
| ChEBI | CHEBI:90943  |
| Chemical data | |
| Formula | C28H33N7O2 |
| Molecular mass | 499.62 g·mol−1 |
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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]
The EU gave a similar approval in Feb 2016[8] after two Phase II studies (AURA extension and AURA2).
Clinical trials
First-line use
Osimertinib has also given encouraging results in early trials as a first-line therapy.[9]
References
- ↑ 1.0 1.1 Lua error in package.lua at line 80: module 'strict' not found.
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
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- ↑ U.S. Food and Drug Administration. Hematology/Oncology (Cancer) Approvals & Safety Notifications. [1]
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ U.S. Food and Drug Administration. "Osimertinib". [2]
- ↑ TAGRISSO™ (OSIMERTINIB) APPROVED IN EU AS FIRST-IN-CLASS TREATMENT FOR PATIENTS WITH EGFR T790M MUTATION-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER
- ↑ First-Line Osimertinib Yields Nearly 80% Response in Advanced Lung Cancer. April 2016
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