Osimertinib / Tagrisso (Everest)

Product Overview

Osimertinib (Brand name: Tagrisso) is a third-generation oral, irreversible EGFR tyrosine kinase inhibitor (EGFR-TKI) originally developed by AstraZeneca under the research code AZD9291.

It is indicated for the treatment of advanced non-small cell lung cancer (NSCLC) and selectively targets both EGFR-sensitive mutations and the EGFR T790M resistance mutation. Osimertinib received approval for import and clinical use in China in March 2017.

The T790M mutation commonly develops in patients who have received long-term treatment with first-generation EGFR-targeted therapies such as gefitinib, icotinib, or erlotinib. Approximately 55–60% of patients may develop the T790M resistance mutation after 1–2 years of treatment, leading to reduced effectiveness of previous therapies and uncontrolled tumor progression.

Osimertinib was specifically developed to overcome this resistance mechanism and provide patients with an additional targeted treatment option. It may also be effective in patients found to carry the T790M mutation prior to receiving treatment.

Compared with earlier EGFR-targeted therapies, Osimertinib demonstrates strong selectivity against T790M-mutated cancer cells and is generally associated with relatively manageable side effects, most commonly including skin rash, nail changes, and diarrhea.

Indications

Osimertinib is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) that carries epidermal growth factor receptor (EGFR) T790M mutations.

It is commonly prescribed for patients who have developed resistance to prior EGFR-targeted therapies such as gefitinib, icotinib, erlotinib, or afatinib.

Dosage and Administration

• Recommended dosage: 80 mg orally once daily until disease progression or unacceptable toxicity occurs
• May be taken with or without food
• Swallow tablets whole with water; do not crush, split, or chew

Dose Adjustments

Treatment interruption or dose reduction may be considered depending on individual tolerance and adverse reactions. If dose reduction is necessary, the recommended reduced dose is 40 mg once daily.

Special Populations

No dose adjustment is generally required based on age, body weight, gender, race, or smoking status.