Osimatab 80 MG (Osimertinib) Tablet

Introduction

Osimatab 80 mg (Osimertinib) Tablet is a groundbreaking third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) designed to treat non-small cell lung cancer (NSCLC) harboring specific EGFR mutations, including T790M, L858R, and exon 19 deletions. Manufactured by Eskayef Pharmaceuticals Ltd., a WHO-GMP-certified leader in oncology innovation, and supplied globally by Onco Solution, this targeted therapy addresses both primary sensitizing EGFR mutations and the T790M resistance mutation, which often develops after first-line EGFR-TKI therapy. Osimatab 80 mg (Osimertinib) Tablet offers a dual advantage: potent antitumor activity and reduced toxicity to healthy cells due to its selective binding to mutant EGFR isoforms. With proven efficacy in delaying disease progression and improving survival outcomes, it has become a cornerstone in the management of advanced or metastatic EGFR-mutant NSCLC.

Key Benefits & Mechanism of Action

Osimatab 80 mg (Osimertinib) Tablet works through irreversible inhibition of mutant EGFR, offering precision therapy for NSCLC:

Targeted Binding: Binds irreversibly to EGFR mutations (T790M, L858R, exon 19 deletions) at concentrations 9-fold lower than wild-type EGFR, minimizing damage to normal cells.
Overcoming Resistance: Effectively targets the T790M mutation, a common resistance mechanism to first-generation EGFR TKIs like gefitinib or erlotinib.
Active Metabolites: Generates two pharmacologically active metabolites—AZ7550 (similar potency) and AZ5104 (8-15x greater potency against mutants and wild-type EGFR)—enhancing therapeutic efficacy.
Broad Kinase Inhibition: Also inhibits HER2, HER3, HER4, ACK1, and BLK kinases at clinically relevant concentrations, broadening its antitumor effects.

Indications

Osimatab 80 mg (Osimertinib) Tablet is approved for:

Second-Line Therapy: Treatment of T790M-positive NSCLC in patients progressing after prior EGFR-TKI therapy.
First-Line Therapy: Initial treatment for EGFR exon 19 deletion or L858R mutation-positive metastatic NSCLC.
CNS Metastases: Reduces the risk and progression of brain metastases due to its ability to cross the blood-brain barrier.

Dosage & Administration

Recommended Dose: 80 mg once daily, taken orally with or without food.

Administration: Swallow the tablet whole with water; do not crush or split.
Missed Dose: Take as soon as remembered unless the next dose is due within 12 hours.
Dose Adjustments:
- Severe Adverse Reactions: Reduce to 40 mg daily for ILD, QTc prolongation, or cardiomyopathy.
- Hepatic/Renal Impairment: No initial adjustment required, but monitor closely.

Pharmacokinetics

Absorption: Peak plasma concentration achieved within 6 hours; bioavailability unaffected by food.
Metabolism: Primarily metabolized by CYP3A4 enzymes, with contributions from CYP3A5.
Excretion: 68% via feces, 14% via urine; elimination half-life of 48 hours.
Protein Binding: 95% bound to plasma proteins, primarily albumin.

Side Effects

Common Reactions (≥20%):

Dermatologic: Rash, dry skin, paronychia.
Gastrointestinal: Diarrhea, nausea, decreased appetite.
Constitutional: Fatigue, musculoskeletal pain.

Serious Adverse Reactions:

Interstitial Lung Disease (ILD): Occurs in ~3.3% of patients; discontinue immediately if confirmed.
QTc Prolongation: Monitor ECG and electrolytes in patients with cardiac risk factors.
Cardiomyopathy: Assess LVEF before treatment and periodically thereafter.

Contraindications

Hypersensitivity to osimertinib or any tablet component.
Concurrent use with strong CYP3A4 inducers (e.g., rifampicin, carbamazepine).

Drug Interactions

CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir): Increase osimertinib exposure by 2.1-fold; monitor for toxicity.

CYP3A4 Inducers (e.g., phenytoin, St. John’s wort): Reduce osimertinib efficacy by 78%; avoid concomitant use.
Gastric Acid Reducers: PPIs or H2 blockers may reduce absorption; administer 2 hours before or 10 hours after antacids.

Warnings & Precautions

ILD/Pneumonitis: Permanently discontinue if confirmed; symptoms include dyspnea, cough, and hypoxia.
Cardiac Monitoring: Perform ECGs and electrolyte assessments in patients with congenital long QT syndrome or taking QTc-prolonging drugs.
Embryo-Fetal Toxicity: Can cause fetal harm; advise contraception during treatment and for 6 weeks post-therapy.
Hepatotoxicity: Monitor liver enzymes every 2 weeks for 3 months, then monthly.

Overdose Management

No specific antidote exists. Management includes:

Symptomatic Care: Anti-diarrheals, hydration, and electrolyte correction.
ECG Monitoring: For QTc prolongation or arrhythmias.
Hemodialysis: Ineffective due to high protein binding.

Storage & Handling

Temperature: Store below 30°C in original blister packaging.
Protection: Keep away from moisture, light, and children.

Manufacturer & Supplier

Eskayef Pharmaceuticals Ltd.: A pioneer in oncology since 1990, Eskayef combines cutting-edge technology with WHO-GMP-certified manufacturing to ensure global quality standards. Their facilities in Bangladesh serve over 40 countries.
Onco Solution: A trusted global supplier, Onco Solution bridges gaps in cancer care by delivering Osimatab 80 mg (Osimertinib) Tablet to hospitals and clinics in 50+ countries. For bulk orders or clinical support, visit www.oncosolution.com.

Conclusion

Osimatab 80 mg (Osimertinib) Tablet represents a paradigm shift in the treatment of EGFR-mutant NSCLC, offering hope to patients with resistant or advanced disease. Its ability to selectively target T790M, L858R, and exon 19 deletion mutations while sparing wild-type EGFR underscores its precision and safety. Backed by robust clinical trials like AURA3 and FLAURA, this therapy has redefined first- and second-line treatment protocols, significantly improving progression-free survival and quality of life. Trust Eskayef Pharmaceuticals Ltd. for uncompromised manufacturing excellence and Onco Solution for seamless global distribution. For orders or clinical inquiries, contact Onco Solution to access this life-saving therapy.