Osimertinib, known by the brand name Tagrisso, is an oral, third-generation, irreversible tyrosine kinase inhibitor (TKI) targeting the epidermal growth factor receptor (EGFR). It is specifically engineered to address both EGFR sensitizing mutations and EGFR T790M resistance mutations, providing a notable treatment option for patients with certain forms of non-small cell lung cancer (NSCLC). The 80 mg dose is the typical strength used once daily in various clinical contexts.

Mechanism of Action

Osimertinib, known by the brand name Tagrisso, is an oral, third-generation, irreversible tyrosine kinase inhibitor (TKI) targeting the epidermal growth factor receptor (EGFR). It is specifically engineered to address both EGFR sensitizing mutations and EGFR T790M resistance mutations, providing a notable treatment option for patients with certain forms of non-small cell lung cancer (NSCLC). The 80 mg dose is the typical strength used once daily in various clinical contexts.

Indications

Tagrisso is approved for treating:

Patients aged 18 years or older with metastatic NSCLC who have the EGFR T790M mutation (as determined by an FDA-approved test) and whose disease has progressed while on or after EGFR TKI therapy.

Initial therapy for patients with metastatic NSCLC whose tumors exhibit EGFR exon 19 deletions or L858R mutations in exon 21.

Adjuvante Therapie nach Tumorresektion bei Patienten mit NSCLC im Frühstadium (IB, II, IIIA) und EGFR-Mutationen.

Over time, these approvals have broadened due to robust clinical trial evidence demonstrating its capacity to significantly enhance progression-free survival and overall survival in comparison to older treatments.

Dosage and Administration

The suggested dosage is 80 mg taken orally once a day, with or without meals.

Tablets must be ingested intact; they should not be crushed, divided, or chewed.

In cases of adverse reactions, dose interruptions, reductions, or discontinuations may be necessary according to clinical judgment and guidelines.

Pharmacokinetics

Absorption: Osimertinib is well absorbed with peak plasma concentrations typically observed 6 hours after dosing.

Distribution: It has a large volume of distribution, indicating extensive tissue penetration.

Metabolism: Primarily metabolized by CYP3A4/5 enzymes into active metabolites (AZ5104 and AZ7550).

Elimination: Osimertinib has a terminal half-life of approximately 48 hours, supporting once-daily dosing.

Clinical Trials and Efficacy

Osimertinib INN 80 mg (Tagrisso) position in treatment is supported by several key studies:

AURA3 Trial: Showed enhanced progression-free survival in patients with T790M-positive NSCLC who had experienced progression on previous EGFR-TKI treatment.

FLAURA Trial: Demonstrated that using osimertinib as a first-line treatment markedly increased median progression-free survival and overall survival rates when compared to earlier EGFR TKIs such as erlotinib or gefitinib.

ADAURA Trial: Within the scope of adjuvant therapy, osimertinib reduced the risk of disease recurrence or death by 83% compared to placebo.

The results established osimertinib as not only a go-to treatment for resistant NSCLC but also a preferred first-line agent.

Safety and Side Effects

Common side effects of Tagrisso include:

Diarrhea

Rash

Dry skin

Nail toxicity

Fatigue

Decreased appetite

More serious adverse events can include:

Interstitial lung disease (ILD)/pneumonitis

QTc prolongation (heart rhythm changes)

Cardiomyopathy

Thrombotic events

Patients should be monitored regularly for signs of cardiac dysfunction and lung toxicity, with treatment modifications made if necessary.

Drug Interactions

Osimertinib plasma concentrations can be reduced by CYP3A inducers (such as rifampin), which may diminish its effectiveness.

Bei gleichzeitiger Anwendung von starken CYP3A-Inhibitoren (wie Ketoconazol) kann die Osimertinib-Exposition steigen.

It is advisable to be cautious when using Tagrisso in conjunction with other drugs that also extend the QT interval.

Application in Special Populations

Pregnancy: Tagrisso can be harmful to the fetus; effective contraception is recommended during treatment and for a specified duration after the final dose.

Lactation: Women should not breastfeed during treatment and for a defined time after the final dose.

Geriatric use: No specific dosage adjustments are generally required, but elderly patients should be monitored closely for adverse reactions.

Storage

Store at room temperature (20°C to 25°C; 68 °F to 77 °F).

Protect from moisture and light.

Conclusion

Osimertinib (Tagrisso) mit einer Dosierung von 80 mg stellt einen bedeutenden Fortschritt in der Behandlung von EGFR-mutiertem NSCLC dar. It has become a fundamental component of personalized lung cancer therapy due to its capacity to target both sensitizing and resistance mutations, as well as its manageable safety profile. As research continues, osimertinib’s role may grow, providing hope for better outcomes in a cancer type that has traditionally been challenging to treat.

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1. What is the purpose of Osimertinib (Tagrisso)?
Osimertinib (Tagrisso) is indicated for the treatment of non-small cell lung cancer (NSCLC) with specific mutations in the epidermal growth factor receptor (EGFR) gene, including T790M resistance mutations.

2. Osimertinib belongs to which drug class?
Osimertinib is a third-generation EGFR tyrosine kinase inhibitor (TKI) that is specifically designed to target mutations in the EGFR gene within cancer cells.

3. Is Osimertinib applicable as a first-line treatment?
Yes, Osimertinib is sanctioned for use as a first-line therapy in patients with EGFR-mutated advanced or metastatic NSCLC.

4. Which side effects of Osimertinib occur frequently?
Typical side effects comprise rash, diarrhea, dry skin, alterations in nails, fatigue, and reduced appetite.

5. Does Osimertinib work for brain metastases?
Yes, Osimertinib is capable of crossing the blood-brain barrier and has demonstrated efficacy in treating brain metastases linked to EGFR-mutant NSCLC.

6. Does Osimertinib carry significant risks?
Indeed, serious risks can encompass lung inflammation (interstitial lung disease), cardiac issues (QT prolongation), and decreased blood cell counts. It is important to monitor regularly.