Osicent Osimertinib 80 mg Tablet

Osicent 80 MG (Osimertinib)

Osimertinib

Price: $100.00

Osimertinib is a third-generation, irreversible, EGFR-TKI, which approved treatment option (80 mg once daily) for patients with EGFRm advanced NSCLC and for patients with T790M-positive NSCLC after disease progression on EGFR-TKIs. Although osimertinib use substrate for the permeability glycoprotein and breast cancer resistance protein efflux transporters. The permeability of osimertinib sufficient to overcome this efflux. Preclinical evidence in nonhuman primates shows that osimertinib has greater penetration of the blood-brain barrier and higher brain exposure compared with other EGFR-TKIs.

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Description

Osicent (Osimertinib) is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) at approximately 9-fold smaller concentrations than wild-type. In cultured cells and animal tumor implantation models, osimertinib showed anti-tumor activity against non-small cell lung cancer (NSCLC) lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletions, and exon 19 deletions) and, to a lesser extent, wild-type EGFR amplifications.

Indication

Osimertinib is a kinase inhibitor indicate for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detect an FDA-approved test, who progress on or after EGFR tyrosine kinase inhibitor therapy.

Interstitial Lung Disease (ILD)/Pneumonitis: Occurs in 3.3% of patients. It permanently discontinued in patients diagnosed with ILD/Pneumonitis.

QTc Interval Prolongation: Electrocardiograms and electrolytes should monitored in patients who have a history or predisposition for QTc prolongation. Those who are taking medications that are known to prolong the QTc interval. It should withheld then restarted at a reduced dose or permanently discontinued.

Cardiomyopathy: Occurred in 1.4% of patients. Left ventricular ejection fraction (LVEF) should assessed before treatment and then every 3 months thereafter.

 

Side Effects

The most common (>20%) adverse reactions (all grades) observed in Osimertinib-treated patients were Diarrhoea (42%), rash (41%), dry skin (31%), and nail toxicity (25%). The most frequent adverse reactions that led to dose reductions or interruptions were: electrocardiogram QTc prolonged (2.2%) and neutropenia (1.9%). Serious adverse reactions reported in 2% or more patients were pneumonia and pulmonary embolus.

 

Drug Interaction

Strong CYP3A Inhibitors Concomitant administration of Osimertinib should avoided with strong CYP3A inhibitors.  Including macrolide antibiotics (e.g., telithromycin), antifungals (e.g., itraconazole), antivirals (e.g., ritonavir), nefazodone, as concomitant use of strong CYP3A inhibitors may increase Osimertinib plasma concentrations. If no other alternative exists, patients should monitored more closely for adverse reactions.

 

Strong CYP3A Inducers

Concomitant administration of Osimertinib should avoided with strong CYP3A inducers (e.g., phenytoin, rifampicin, carbamazepine, St. John’s Wort) as strong CYP3A inducers may decrease Osimertinib plasma concentrations.

 

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