OSIMERITINIB [Tagrisso] - Tagrisso 40mg



A Tagrisso 40mg tablet is containing an active substance known as Osimeritinib, which is formerly known as Mereletinib. Tagrisso 40mg is considered as third generation medicine, which is available in tablet form. Tagrisso 40mg is an inevitable, selectively deviated epidermal growth factor receptor prohibitor, containing anti-cancer activity. The pharmacological category of Tagrisso 40mg is tyrosine kinase prohibitor.

     Tagrisso 40mg


A Tagrisso 40mg tablet is widely indicated as first line therapy for advanced non-small cell lung cancer with EGFR mutation positive patients. Tagrisso 40mg is also used for the treatment of patients affected with advanced EGFR T792M mutation positive NSCLC, disease has advanced on or after the tyrosine kinase inhibitor treatment.

                                                               Tagrisso 40mg


Osimeritinib is similar in action when compared to other tyrosine kinase inhibitor drugs. Osimeritinib, Tagrisso 40mg tablet is named tyrosine kinase inhibitor of epidermal development factor receptor which is available on the surface of tumor cells Osimeritinib is non-reversibly converge with mutant type of EGFR at 9 folds than wild sort
Forbids EGFR sharpening changes exon 19 Del and L858R Prompts denies transformed EGFR with T790M opposition transformation. At last, bring down action against wild kind EGFR

                                                            Tagrisso 40mg


Absorption :High plasma concentration time of Osimeritinib reaches within 6 hours
Distribution :
Volume of distribution 918L
Human Plasma protein bound to Osimeritinib is 95%
Metabolism :
The metabolism of Osimeritinib is occurs via oxidation.
The Two pharmacologically active metabolite of Osimeritinib are AZ7550 & AZ5104
Excretion :
The mean terminal half-life period 48 hours
Clearance value 14.3L/hr
68% of metabolite is excreted in feces; 14% through urine

2% of unchanged form of drug is eliminated

                                                Tagrisso 40mg


The recommended dosage of  the tablets are, 80mg tablet should be taken as a single dose. Tagrisso 40mg tablet should be administered with or without food.If patient felt difficult to swallow the Tagrisso 40mg tablets as such, must disperse the tablet in 60ml of noncarbonated water and drink the solution immediately.
Tagrisso 40mg tablet do not break, crush or chew.
Interrupt the treatment during the conditions like;
Interstitial lung disease
QT prolongation
Symptomatic congestive heart failure
In pain management
Grade III or severe: discontinue the Tagrisso 40mg tablet for 3 weeks
Grade 0 to II: follow at 80mg or 40mg as a single dose
If no development in 3 weeks: Discontinue the therapy.
While co administration of Tagrisso 40mg with CYP3A4 inducers, the dosage of Tagrisso 40mg should be increased to 160mg as a single dose and followed by 80mg for 3 weeks after discontinuation of strong CYP3A4 inducers.

                                                                Tagrisso 40mg


Interstitial lung disease:
To avoid this problem, withheld or stop the Tagrisso 40mg tablets.
check the manifestation of keratitis regularly and provide supportive measures
Embryo fetal toxicity:
Tagrisso 40mg tablet required in pregnancy period causes fetal damage.
QTc extension:
Do not concurrent use of Tagrisso 40mg with drug prolong the QTc
Periodic cardiac monitoring is assessed; in this condition stop the therapy.

                                                               Tagrisso 40mg


The most common adverse effects occurred during the therapy; Cardiomyopathy, QT prolongation, Interstitial lung disease, Keratitis.
Other common side effect :
Diarrhea or constipation, Hyperglycemia, Hypomagnesemia, Hyponatremia, Elevation of AST & ALT, Stomatitis, Nausea, Vomiting, Rash, Nail toxicity, Pruritus, Dry skin, Headache, Cough, Dyspnea, Fatigue, Pyrexia, Loss of appetite, Respiratory tract infection, Lymphopenia, Thrombocytopenia, Anemia, Neutropenia.


Pregnancy category of Osimeritinib is not designate While using Tagrisso 40mg tablet causes possible for fetal harm


Milk feeding should not be taken during lactation period.


The Tagrisso 40mg tablet is, stored at 25°C.
Keep the tablet carton from moisture, heat and light.


In case of missed dose, do not take the missed dose and follow the regular dosing schedule.


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