Introduction for Osimert 80 mg (Osimertinib): 

Each tablet of Osimert 80 mg contains Osimertinib 80 mg. Osimertinib 80 is a protein kinase inhibitor used to treat non-small cell lung cancer. Adult individuals with specific EGFR mutations are treated with it . Osimert 80 is used for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors include epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. Osimertinib is also used to treat patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, and whose disease has progressed during or after EGFR tyrosine kinase inhibitor (TKI) treatment.

Pharmacology:

Osimert 80 mg is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to specific mutant forms of EGFR (T790M, L858R, and exon 19 deletion) found in non-small cell lung cancer (NSCLC) tumors after therapy with first-line EGFR-TKIs. As a third-generation tyrosine kinase inhibitor, Osimert 80 mg targets the gate-keeper T790M mutation, which increases ATP binding activity to EGFR and leads to a poor prognosis in late-stage illness. Furthermore, Osimert 80 mg has been demonstrated to protect wild-type EGFR during therapy, lowering non-specific binding and minimizing toxicity.

The area under the plasma concentration-time curve and maximal plasma concentration (C max) of Osimertinib 80 mg increased dose proportionately over the 20 to 240 mg dose range (i.e., 0.25 to 3 times the recommended dosage) following oral administration, and the pharmacokinetics were linear. Osimert 80 mg was administered orally once daily, resulting in roughly 3-fold accumulation and steady-state exposures after 15 days of treatment. At steady state, the C max to C min (lowest concentration) ratio was 1.6 times.
The median time to C max for Osimert 80 mg (Osimertinib) was 6 hours (range 3-24 hours). Following the administration of 20 mg Osimert 80 mg (Osimertinib) tablets with a high-fat, high-calorie meal (containing approximately 58 grams of fat and 1000 calories), the C max and AUC of Osimert 80 mg (Osimertinib) were compared to those obtained when fasting.

Osimert 80 mg (Osimertinib) had a mean steady-state distribution volume (Vss/F) of 986 L. Osimert 80 mg (Osimertinib) has a plasma protein binding rate of 95%.
Osimert 80 mg (Osimertinib) plasma concentrations dropped over time, with a population-estimated mean half-life of 48 hours and oral clearance (CL/F) of 14.2 L/hour.In vitro, the primary metabolic routes of Osimert 80 mg (Osimertinib) were oxidation (mostly CYP3A) and dealkylation. Following oral treatment of Osimert 80 mg (Osimertinib), two pharmacologically active metabolites (AZ7550 and AZ5104) were detected in the plasma. The geometric mean exposure (AUC) of each metabolite (AZ5104 and AZ7550) was roughly 10% of Osimertinib 80 mg’s exposure at steady-state. Osimert 80 mg (Osimertinib) is mostly removed through feces (68%) and  to a lesser extent through urine (14%).

Dosage & Administration:

The recommended dose of Osimert 80 mg  is 80 mg once daily until disease progression or intolerable toxicity. Osimertinib 80 can be taken with or without food, but it is best to take it at the same time every day to maximize its advantages.

Administration of Osimert 80 mg:

Dissolve the tablet with 60 ml of non-carbonated water only. Stir until the tablet is divided into small bits (it will not entirely dissolve), then consume immediately. During preparation, avoid crushing, heating, and ultrasonicating.

Interaction:

Strong CYP3A4 inducer: If co-administration of Osimert 80 mg (Osimertinib) with strong CYP3A inducers is necessary, increase the dose to 160 mg daily. Resume Osimertinib 80 mg 3 weeks after stopping the strong CYP3A4 inducer.

Side Effects:

The most common (>20%) adverse effects reported in Osimert 80 mg treated individuals were diarrhea (42%), rash (41%), dry skin (31%), and nail toxicity (25%). The most common side effects resulting in dosage reductions or suspensions were electrocardiogram QTc prolongation (2.2%) and neutropenia (1.9%). Pneumonia and pulmonary embolism were among the serious adverse responses recorded in 2% or more patients.

Pregnancy and Lactation:
Osimert 80 mg when given to a pregnant patient, it may harm the developing fetus. Administration of Osimert 80 mg (Osimertinib) to pregnant rats resulted in similar exposures to embryonic death, lower fetal growth, and neonatal mortality. Osimertinib 80 mg is not recommended during pregnancy or for women of reproductive potential who do not use contraception.

There is no information available regarding Osimertinib 80 mg’s presence in human milk, how it affects breastfed infants.

Storage Conditions:
Osimert 80 mg should be kept between 20°C and 25°C at room temperature. When a medication is no longer needed or has expired, dispose of it safely. Keep Osimert 80 mg and all medicines out of the reach of children.

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