Composition : Osimeritinib
Strength availability : 40mg
Pack : 30 tablets in a carton
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A Tagrisso 40 mg 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 40 mg is an inevitable, selectively deviated epidermal growth factor receptor prohibitor, containing anti-cancer activity.
The pharmacological category of Tagrisso 40mgis tyrosine kinase prohibitor.
A Tagrisso 40mg (osimertinib) tablet is widely indicated as first line therapy for advanced non-small cell lung cancer with EGFR mutation positive patients.
Tagrisso 40mgi s 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.
The usual prescribed dosage of Tagrisso 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 40mgtablets as such, must disperse the tablet in 60ml of noncarbonated water and drink the solution immediately.
Tagrisso tablet do not break, crush or chew.
Discontinue the therapy during the conditions like :
Interstitial lung disease
Symptomatic congestive heart failure
In pain management
Grade III or severe: Withheld 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 40mgwith CYP3A4 inducers, the dosage of Tagrisso 40mgshould be increased to 160mg as a single dose and followed by 80mg for 3 weeks after discontinuation of strong CYP3A4 inducers.
Peak plasma concentration time of osimertinib reaches within 6 hours
Distribution:Volume of distribution 918L
Plasma protein bound to Osimeritinib is 95%
The metabolism of Osimeritinib is occurs through 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
Osimeritinib is similar in action when compared to other tyrosine kinase inhibitor drugs.
Osimeritinib 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
Some of the adverse effects occur during the therapy :
Interstitial lung disease: To avoid this problem, withheld or discontinue the Tagrisso 40mg tablets.
QTc extension: Avoid concurrent use of Tagrisso 40mg with drug prolong the QTc
Cardiomyopathy: Periodic cardiac monitoring is assessed; in this condition discontinue the therapy.
Keratitis: Monitor the manifestation of keratitis frequently and provide supportive measures
Embryo fetal toxicity: Tagrisso 40mgtablet used in pregnancy period causes fetal damage.
Tagrisso 40mg tablets combines with strong CYP3A4 inducers causes reducing the exposure of Osimeritinib, this may leads to reduce the efficacy of Tagrisso.
Avoid the concomitant use of strong CYP3A4 inducers with Tagrisso 40mgtablets.
Tagrisso 40mg tablet combined with BCRP substrates may causes increasing the exposure of BCRP substrates. Thus results as increasing the adverse effects related to BCRP substrates
Avoid concomitant use of Tagrisso 40mg tablets with drug which induce the QT prolongation. In this case patients should be undergone periodic ECG monitoring.
No contraindication occurred during the therapy
In some patient’s anaphylactic reaction may occur due to patients may contraindicated to the ingredient of the product
Tagrisso 40mg is a chemo medicine, in case of missed dose occurred skip the missed dose and follow the regular dosing schedule.
Common side effects :
Fatigue; Lymphocytopenia (Low White Blood Cells); Low Sodium; Shortness of breath; Musculoskeletal Pain; Decreased Appetite; Cough
Less common side effects :
Constipation; Increased serum creatinine; Colitis; Low potassium; Low magnesium; High calcium; Vomiting; Weakness; Diarrhea; High potassium; Low calcium; Swelling; Fever; Rash; Abdominal pain; Increased serum AST; Thrombocytopenia; Increased serum alkaline phosphatase; Chest pain; Weight loss.This are the tagrisso side effects.