For the treatment of metastatic EGFRm NSCLC

TAGRISSO is designed to potently and selectively inhibit EGFR sensitizing and resistance mutations1-4

TAGRISSO is a third-generation, irreversible EGFR TKI designed to2-4

  • Inhibit EGFR sensitizing mutations—exon 19 del and L858R
  • Inhibit mutated EGFR with the T790M resistance mutation
  • Have lower activity against wild-type EGFR
Mechanism of action (MOA) of TAGRISSO Mechanism of action (MOA) of TAGRISSO

TAGRISSO crossed the blood-brain barrier (BBB) in preclinical models1,5,6

In a study, TAGRISSO crossed the BBB in healthy humans7*

*Study Description: Eight (8) male healthy volunteers (age 52±8 years) were examined for ~90 minutes with PET imaging after single intravenous microdose (1.2 mcg; range 1.1-1.4 mcg) of 11C-labeled TAGRISSO. Concentrations of 11C-labeled TAGRISSO were also measured in arterial and venous blood and plasma. Brain MRI was acquired and used for co-registration of PET data and automatic delineation of regions of interest in the brain. PK parameters Cmax (brain), Tmax (brain) and AUC0–90 min brain/blood ratio were calculated. Safety and tolerability monitoring included recording of AEs, vital signs, ECG.7

Learn more about the mechanism of action for TAGRISSO

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NCCN Guidelines® recommend that every effort should be made to establish a patient's genetic alteration status (EGFR, ALK, ROS1, BRAF) and PD-L1 status prior to treatment initiation8

Click here for information about testing for EGFRm in newly diagnosed patients with metastatic NSCLC.
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References: 1. TAGRISSO [package insert]. Wilmington, DE: AstraZeneca Pharmaceuticals LP; 2018. 2. Soria JC, Ohe Y, Vansteenkiste J, et al. Osimertinib in untreated EGFR-mutated advanced non-small-cell lung cancer. N Engl J Med. 2018;378(2):113-125. 3. Cross DA, Ashton SE, Ghiorghiu S, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014;4(9):1046-1061. 4. Finlay MR, Anderton M, Ashton S, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014;57(20):8249-8267. 5. Ballard P, Yates JW, Yang Z, et al. Preclinical comparison of osimertinib with other EGFR-TKIs in EGFR-mutant NSCLC brain metastases models, and early evidence of clinical brain metastases activity. Clin Cancer Res. 2016;22(20):5130-5140. 6. Colclough N, Ballard P, Barton P, et al. Preclinical comparison of the blood brain barrier (BBB) permeability of osimertinib (AZD9291) with other irreversible next generation EGFR TKIs. Eur J Cancer. 2016;69:S28. 7. Varrone A, Varnäs K, Jucaite A, et al. Osimertinib displays high brain exposure in healthy subjects with intact blood-brain barrier: a micro-dose positron emission tomography (PET) study with 11C-labelled osimertinib. Poster presented at: 2018 AACR meeting; April 14-18, 2018; Chicago, IL. 8. Referenced with permission from the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for NSCLC V.5.2018. © National Comprehensive Cancer Network, Inc. 2018. All rights reserved. Accessed June 29, 2018. To view the most recent and complete version of the guideline, go online to NCCN.org. NCCN makes no warranties of any kind whatsoever regarding their content, use or application and disclaims any responsibility for their application or use in any way.

Important Safety Information Expand

  • There are no contraindications for TAGRISSO

  • Interstitial lung disease (ILD)/pneumonitis occurred in 3.9% of the 1142 TAGRISSO-treated patients; 0.4% of cases were fatal. Withhold TAGRISSO and promptly investigate for ILD in patients who present with worsening of respiratory symptoms which may be indicative of ILD (eg, dyspnea, cough and fever). Permanently discontinue TAGRISSO if ILD is confirmed

  • Heart rate-corrected QT (QTc) interval prolongation occurred in TAGRISSO-treated patients. Of the 1142 TAGRISSO-treated patients in clinical trials, 0.9% were found to have a QTc > 500 msec, and 3.6% of patients had an increase from baseline QTc > 60 msec. No QTc-related arrhythmias were reported. Conduct periodic monitoring with ECGs and electrolytes in patients with congenital long QTc syndrome, congestive heart failure, electrolyte abnormalities, or those who are taking medications known to prolong the QTc interval. Permanently discontinue TAGRISSO in patients who develop QTc interval prolongation with signs/symptoms of life-threatening arrhythmia

  • Cardiomyopathy occurred in 2.6% of the 1142 TAGRISSO-treated patients; 0.1% of cardiomyopathy cases were fatal. A decline in left ventricular ejection fraction (LVEF) ≥10% from baseline and to <50% LVEF occurred in 3.9% of 908 patients who had baseline and at least one follow-up LVEF assessment. Conduct cardiac monitoring, including assessment of LVEF at baseline and during treatment, in patients with cardiac risk factors. Assess LVEF in patients who develop relevant cardiac signs or symptoms during treatment. For symptomatic congestive heart failure, permanently discontinue TAGRISSO

  • Keratitis was reported in 0.7% of 1142 patients treated with TAGRISSO in clinical trials. Promptly refer patients with signs and symptoms suggestive of keratitis (such as eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain and/or red eye) to an ophthalmologist

  • Verify pregnancy status of females of reproductive potential prior to initiating TAGRISSO. Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with TAGRISSO and for 6 weeks after the final dose. Advise males with female partners of reproductive potential to use effective contraception for 4 months after the final dose

  • Most common adverse reactions (≥20%) were diarrhea, rash, dry skin, nail toxicity, stomatitis, fatigue and decreased appetite

Indications

  • TAGRISSO 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

  • TAGRISSO 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


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