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Osimertinib

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Information about Osimertinib

Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NSCLC). 

Osimertinib
Osimertinib

Liver safety of Osimertinib

Osimertinib is associated with a moderate rate of serum aminotransferase elevations during therapy and rare instances of clinically apparent acute liver injury

Mechanism of action of Osimertinib

Osimertinib (oh" sim er' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against the epidermal growth factor receptor (EGFR) that is rearranged and mutated in selected cancers including approximately 5% of non-small cell lung cancer (NSCLC).  The mutated, rearranged EGFR promotes unregulated cell growth and proliferation, and inhibition of its activity can result in death of cells that overexpress the receptor.  Osimertinib has been found to inhibit mutated EGFR in cell culture and, in several clinical trials, was found to induce objective responses in a proportion of patients with advanced EGFR mutated (T790M) NSCLC. 

FDA approval information for Osimertinib

Osimertinib received accelerated approval for use refractory, EGFR T790M-positive NSCLC in the United States in 2015.  Osimertinib is available in tablets of 40 and 80 mg under the brand name Tagrisso. 

Dosage and administration for Osimertinib

The recommended initial dose is 80 mg once daily, continued until progressive disease or intolerable toxicity occurs. 

Side effects of Osimertinib

Side effects are common and include diarrhea, rash, dry skin and nail toxicity.  Uncommon, but potentially severe side effects include interstitial lung disease, prolongation of the QTc interval, cardiomyopathy and embryo-fetal toxicity. 

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