Product Name: Tasso 80mg

Generic Name: Osimertinib 80mg

Pack Size: 30 Tablets

Company Name: Jenphar Bangladesh.

Origin: Bangladesh

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Indications

Tasso is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test. Tasso is indicated for the treatment of patients with metastatic EGFR T790M mutation-positive NSCLC, as detected by an FDA-approved test, whose disease has progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy.

Pharmacology

Osimertinib is kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. In cultured cells and animal tumor implantation models, Osimertinib exhibited anti-tumor activity against NSCLC lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletion, and exon 19 deletion) and, to a lesser extent, wild-type EGFR amplifications. Two pharmacologically-active metabolites (AZ7550 and AZ5104 circulating at approximately 10% of the parent) with similar inhibitory profiles to Osimertinib have been identified in the plasma after oral administration of Osimertinib. AZ7550 showed a similar potency to Osimertinib, while AZ5104 showed greater potency against exon 19 deletion and T790M mutants (approximately 8-fold) and wild- type (approximately 15-fold) EGFR. In vitro, Osimertinib also inhibited the activity of HER2, HER3, HER4, ACK1, and BLK at clinically relevant concentrations.

The area under the plasma concentration-time curve (AUC) and maximal plasma concentration (C max ) of Osimertinib increased dose proportionally over 20 to 240 mg dose range (i.e., 0.25 to 3 times the recommended dosage) after oral administration and exhibited linear pharmacokinetics (PK). Administration of Osimertinib orally once daily resulted in approximately 3-fold accumulation withsteady state exposures achieved after 15 days of dosing. At steady state, the C max to C min (minimal concentration) ratio was 1.6-fold.

Absorption: The median time to C max of Osimertinib was 6 hours (range 3-24 hours). Following administration of a 20 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 Osimertinib were compared to that under fasting conditions.

Distribution: The mean volume of distribution at steady-state (Vss/F) of Osimertinib was 986 L. Plasma protein binding of Osimertinib was 95%.

Elimination: Osimertinib plasma concentrations decreased with time and a population estimated mean half-life of Osimertinib was 48 hours, and oral clearance (CL/F) was 14.2 (L/h).

Metabolism: The main metabolic pathways of Osimertinib were oxidation (predominantly CYP3A) and dealkylation in vitro. Two pharmacologically active metabolites (AZ7550 and AZ5104) have been identified in the plasma after Osimertinib oral administration. The geometric mean exposure (AUC) of each metabolite (AZ5104 and AZ7550) was approximately 10% of the exposure of Osimertinib at steady-state.

Excretion: Osimertinib is primarily eliminated in the feces (68%) and to a lesser extent in the urine (14%). Unchanged Osimertinib accounted for approximately 2% of the elimination