Osimertinib is a third-generation irreversible EGFR tyrosine kinase inhibitor (TKI) that is used to treat specific forms of non-small cell lung cancer (NSCLC). It is sold under the trade name Tagrisso. Tagrisso, which is produced by AstraZeneca, is intended to particularly target cancers that have EGFR mutations, such as the T790M resistance mutation. It comes in 40 mg and 80 mg oral tablet forms, enabling adjustable dosage according to the patient’s requirements and stage of treatment.

Indications and Usage

Osimertinib is approved for the following indications:

First-line therapy should be administered to adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors include EGFR exon 19 deletions or exon 21 L858R substitution mutations.

Second-Line Treatment: For patients with metastatic EGFR T790M mutation-positive NSCLC who have progressed on or after EGFR TKI therapy.

Adjuvant Therapy: For adult patients with early-stage (IB, II, or IIIA) NSCLC with EGFR mutations following complete tumor resection.

These approvals are based on robust clinical trial data demonstrating superior progression-free survival and overall survival compared to previous-generation EGFR inhibitors.

Mechanism of Action

Osimertinib 40mg & 80mg (Tagrisso) works by irreversibly binding to mutant forms of the EGFR, including the T790M resistance mutation, which often arises after first- or second-generation EGFR TKI therapy. In contrast to previous TKIs, Osimertinib preserves wild-type EGFR while selectively inhibiting sensitizing mutations (exon 19 deletions and L858R) and the T790M mutation. This selectivity reduces off-target effects and improves tolerability.

Additionally, Osimertinib has central nervous system (CNS) activity, making it effective against brain metastases, a common complication in advanced EGFR-mutated NSCLC.

Dosage and Administration

The suggested dosage is 80 milligrams once daily, with or without food.

Alternative Strength: The 40mg tablet is primarily used when a dose reduction is required due to adverse effects.

Dosage adjustments may be necessary for patients experiencing severe side effects or in those with hepatic impairment. For optimal effects, osimertinib should be taken orally at the same time every day.

Formulation and Packaging

There are two dose strengths for Tagrisso:

The film-coated, yellow, oval, biconvex tablets have 40 mg and the words “AZ 40” printed on one side.

The 80mg tablets are film-coated, oval, biconvex, and beige with the words “AZ 80” printed on one side.

Every tablet is packaged separately, either in a blister or a bottle, guaranteeing correct dosage and appropriate storage.

Pharmacokinetics Absorption: Osimertinib is efficiently absorbed when taken orally, and it takes six hours for plasma concentrations to peak.

Distribution: Excellent tissue penetration, including the brain, and highly protein-bound.

Metabolic: mostly broken down by the liver’s CYP3A4 and CYP3A5 enzymes.

Elimination: Once-daily dose is supported by a half-life of roughly 48 hours.

Side Effects

Typical adverse effects consist of:

Having diarrhea

Rash

Skin that is dry

Toxicology of nails

Weariness

Diminished appetite

Serious yet uncommon side effects:

Pneumonia with interstitial lung disease (ILD)

lengthening of the QTc interval

Heart disease

thrombocytopenia or severe neutropenia

To identify and control these occurrences early, routine monitoring is recommended. Depending on the severity, dose modifications or cessation may be required.

Warnings and Precautions

If interstitial lung disease (ILD) is identified, stop taking the medication immediately.

QT Prolongation: Exercise caution in patients with a history of heart problems; routinely check ECGs.

Cardiomyopathy: Prior to and during treatment, keep an eye on the ejection fraction.

Hepatotoxicity: Regular evaluations of liver function are recommended.

Fetal Risk: During and after therapy, effective contraception is required because osimertinib may harm the fetus.

Drug Interactions

Because osimertinib is metabolized by CYP3A enzymes, its efficacy or toxicity may change if it is used concurrently with potent CYP3A inducers or inhibitors, such as ketoconazole.

Clinical Effectiveness

Important studies like FLAURA and AURA3 showed that osimertinib significantly improved survival compared to conventional EGFR TKIs. Osimertinib demonstrated a median progression-free survival of 18.9 months in the FLAURA study, while typical EGFR TKIs demonstrated a median progression-free survival of 10.2 months. Osimertinib’s place as a second-line treatment was cemented when the AURA3 study demonstrated benefits in patients with the T790M resistant mutation.

Keeping and Managing

Store in original container below 30°C (86°F).

Defend against light and moisture.

Keep out of children’s reach.

Conclusion

The 40 mg and 80 mg tablets of osimertinib (Tagrisso) are a major improvement in the treatment of non-small cell lung cancer with an EGFR mutation. It is the recommended option for both first-line and follow-up therapy because to its capacity to overcome resistance mutations, enter the central nervous system, and produce long-lasting effects with a controllable safety profile. Tagrisso continues to be a key component in the battle against targeted lung cancer as research advances.

Order Now At Mdx Pharma bd….

To order from MDX Pharma BD, visit their website at https://mdxpharmabd.com, where you can browse products and place orders online. For inquiries or orders via email, contact emedicarepharma@gmail.com. Alternatively, call (+88) 01929123476. Their address is 29, Abdullahpur, Uttara, Dhaka-1230, Bangladesh.

1. What is Osimertinib (Tagrisso) used for?
Osimertinib is a targeted therapy used to treat non-small cell lung cancer (NSCLC) that has specific mutations in the EGFR gene. It is often prescribed when the cancer has metastasized or returned after previous EGFR therapy.

2. Osimertinib: How does it work?
The T790M resistant mutation is one of the mutant EGFR proteins that are blocked by osimertinib, a third-generation EGFR-TKI (tyrosine kinase inhibitor). This aids in reducing or halting the spread of cancerous cells.

3. What is the typical Osimertinib dosage?
80 mg once daily, with or without food, is the recommended dosage. Patients who have specific adverse effects or problems with organ function may occasionally be administered 40 mg per day.

4. Is Osimertinib safe to take while pregnant or nursing?
Osimertinib may be harmful to the fetus. During treatment and for at least six weeks following the last dose, women should take an effective form of birth control. It is not advised to breastfeed.

5. How is Osimertinib supplied and stored?
Osimertinib comes in 40 mg and 80 mg tablets. Store it at room temperature, away from heat and moisture. Keep out of reach of children.