-2%
Ositag is prescribed for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) who have specific epidermal growth factor receptor (EGFR) mutations, such as exon 19 deletions or exon 21 L858R mutations. These mutations must be identified using an FDA-approved test. Additionally, it is used for patients with metastatic NSCLC with the EGFR T790M mutation who have experienced disease progression after treatment with EGFR tyrosine kinase inhibitors (TKIs).
Osimertinib is a kinase inhibitor targeting specific mutant forms of EGFR (T790M, L858R, and exon 19 deletion), with minimal activity against normal EGFR. In both cell cultures and animal models, it has shown potent anti-tumor activity against NSCLC cell lines with EGFR mutations. Two active metabolites (AZ7550 and AZ5104) have been identified, contributing to its overall effectiveness. AZ5104, in particular, demonstrates greater potency against certain mutations and wild-type EGFR.
The drug exhibits dose-proportional pharmacokinetics between 20 and 240 mg. After oral administration, it accumulates over 15 days, achieving steady-state levels. It has a half-life of approximately 48 hours, with most of the drug being eliminated through feces (68%) and, to a lesser extent, urine (14%).