Tagrisso (Osimertinib )

What is Tagrisso?

Tagrisso is an oral targeted therapy used for the treatment of non‑small cell lung cancer (NSCLC) in patients with epidermal growth factor receptor (EGFR) mutations. It is the brand name for the active ingredient osimertinib, a third‑generation EGFR tyrosine kinase inhibitor (TKI) that has demonstrated superior efficacy and improved survival outcomes compared to earlier generation EGFR inhibitors.

Reference: U.S. FDA Tagrisso Prescribing Information; Soria et al., NEJM, 2018 (NCT02296125)

What are the other popular names for Tagrisso?

Tagrisso is primarily marketed under its brand name Tagrisso. It is also referred to by its generic name, osimertinib. In clinical literature, you may encounter both terms, but Tagrisso remains the widely recognized brand.

Reference: MedlinePlus; U.S. FDA

What is the drug classification of Tagrisso?

Tagrisso is classified as an EGFR tyrosine kinase inhibitor (TKI), specifically a third‑generation TKI. It belongs to the broader category of molecular targeted therapies used in oncology for the treatment of EGFR‑mutated NSCLC.

Reference: World Health Organization (WHO) Oncology Guidelines; U.S. FDA

What is the mode of action of Tagrisso?

Tagrisso works by irreversibly binding to the mutant forms of the EGFR—including the T790M resistance mutation—thereby blocking the intracellular signaling pathways (e.g., MAPK and PI3K/AKT) that promote cancer cell proliferation and survival. This results in reduced tumor growth and the induction of apoptosis in cancer cells.

Reference: PubMed (Lynch et al., 2004; Soria et al., 2018 NEJM); U.S. FDA

What are the primary uses of Tagrisso?

Tagrisso is used in the treatment of:

• Advanced NSCLC: Particularly in patients with EGFR‑mutated NSCLC, including those with T790M mutation who have progressed on prior EGFR‑TKI therapy.
• First‑line Treatment: It is also approved as a first‑line therapy for patients with EGFR‑mutated metastatic NSCLC.

Reference: U.S. FDA; ClinicalTrials.gov (NCT02296125, NCT02511106)

What is the recommended dosage and administration for Tagrisso?

• Dosage: The standard dose of Tagrisso is 80 mg once daily taken orally.
• Administration:
  • Tagrisso should be taken at the same time each day, with or without food.
  • Consistency in dosing helps maintain steady plasma levels for optimal efficacy.

Reference: U.S. FDA Tagrisso Prescribing Information; ClinicalTrials.gov

What prescribing information is important for Tagrisso?

• Indications:
  • Tagrisso is indicated for the treatment of patients with metastatic NSCLC whose tumors have specific EGFR mutations.
• Contraindications:
  • It is contraindicated in patients with a known hypersensitivity to osimertinib or any of its ingredients.
• Monitoring:
  • Regular monitoring for adverse effects, including pulmonary symptoms, liver function, and QT interval changes via ECG, is recommended.
• Special Considerations:
  • EGFR mutation testing is essential prior to initiating therapy.
  • Use caution in patients with a history of interstitial lung disease.

Reference: U.S. FDA; NCCN Guidelines; ClinicalTrials.gov

What safety information, side effects, warnings, and cautions are associated with Tagrisso?

• Common Side Effects:
  • Diarrhea, rash, dry skin, nail toxicity, and paronychia (inflammation around the nails).
  • Mild pulmonary symptoms such as cough.
• Serious Side Effects:
  • Interstitial lung disease (ILD)/pneumonitis, which can be life‑threatening.
  • QT interval prolongation, which may lead to cardiac arrhythmias.
• Warnings & Cautions:
  • Pulmonary Toxicity: Patients must be monitored for new or worsening respiratory symptoms.
  • Cardiac Monitoring: ECG monitoring is recommended due to the risk of QT prolongation.
  • Hepatotoxicity: Liver enzymes should be monitored periodically.
  • Dermatologic Reactions: Severe skin reactions, although rare, require immediate medical attention.
• Pregnancy and Lactation:
  • Tagrisso is contraindicated in pregnant women due to potential teratogenic effects. Women of childbearing potential must use effective contraception during treatment.

Reference: U.S. FDA Tagrisso Prescribing Information; NEJM; PubMed

What drug interactions should be considered with Tagrisso?

• CYP3A4 Inhibitors/Inducers:
  • Strong CYP3A4 inhibitors (e.g., ketoconazole) may increase osimertinib levels, while inducers (e.g., rifampin) may decrease its effectiveness.
• Other QT-Prolonging Drugs:
  • Concurrent use with drugs that prolong the QT interval should be avoided or monitored carefully.
• Antacids:
  • While not a major interaction, antacids may slightly affect the absorption of Tagrisso; it is advisable to separate administration by a couple of hours.

Reference: U.S. FDA; Clinical Pharmacology Reviews on PubMed

Frequently Asked Questions (FAQs)

Q: How soon can I expect to see results with Tagrisso?
A: Many patients begin to experience symptom improvement within a few weeks, although full clinical benefits may take several months of continuous therapy.

Q: Is EGFR mutation testing necessary before starting Tagrisso?
A: Yes, EGFR mutation testing is essential to identify patients who are likely to benefit from Tagrisso therapy.

Q: Can Tagrisso be taken with food?
A: Yes, Tagrisso can be taken with or without food; however, it should be taken at the same time each day to ensure consistent plasma levels.

Q: What should I do if I experience respiratory symptoms while on Tagrisso?
A: Report any new or worsening respiratory symptoms immediately, as they could be signs of interstitial lung disease, a serious adverse reaction.

Q: Can I take Tagrisso if I am pregnant?
A: Tagrisso is contraindicated during pregnancy due to the risk of fetal harm. Women of childbearing potential should use effective contraception during treatment.

Reference: U.S. FDA; NCCN Guidelines; PubMed

Where can I find additional clinical evidence and detailed information about Tagrisso?

For further information on clinical studies, dosing guidelines, and safety monitoring, please refer to:

• U.S. Food and Drug Administration (FDA) Website: FDA.gov
• ClinicalTrials.gov: Search for Tagrisso studies (e.g., NCT02296125, NCT02511106)
• New England Journal of Medicine (NEJM): Publications on Tagrisso efficacy in NSCLC
• PubMed: For peer‑reviewed research articles on osimertinib
• National Comprehensive Cancer Network (NCCN) Guidelines: For NSCLC treatment protocols

Reference: U.S. FDA; ClinicalTrials.gov; NEJM; PubMed; NCCN

Final Thoughts

Tagrisso (osimertinib) is a critical targeted therapy for patients with EGFR‑mutated non‑small cell lung cancer. Its ability to irreversibly inhibit EGFR tyrosine kinase activity—including resistant T790M mutations—translates into improved progression‑free survival and overall outcomes in patients with advanced NSCLC. However, careful patient selection through molecular testing, regular monitoring for adverse events (especially pulmonary and cardiac), and management of potential drug interactions are essential to ensure safe and effective use. Always consult your healthcare provider to determine whether Tagrisso is appropriate for your specific condition and to manage its use as part of a comprehensive treatment plan.

Disclaimer: This guide is provided for educational purposes only and should not replace professional medical advice. Always consult with your healthcare provider before initiating or modifying any medication regimen.