MOA

TAGRISSO: Uniquely designed to potently and selectively inhibit EGFR sensitising and resistance mutations1,2

TAGRISSO is a third-generation, irreversible EGFR TKI designed to1,2

  • Inhibit EGFR sensitising mutations (EGFRm, commonly exon 19 deletion and L858R)1,2*
  • Inhibit the emergence of the EGFR T790M resistance mutation2,3
  • Have minimal activity against wild-type EGFR1,2*
Potently† inhibits both EGFRm and EGFR T790M1-3
Potently† inhibits both EGFRm and EGFR T790M1-3
Minimal activity against wild-type EGFR1,2
Minimal activity against wild-type EGFR1,2
Potently† inhibits both EGFRm and EGFR T790M1-3

  • *

  • As demonstrated in preclinical in vitro studies.

  • †

  • Refers to potency of inhibition at the receptor level.

In addition, TAGRISSO crosses the intact blood-brain barrier1,4
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See how TAGRISSO selectively targets both EGFR sensitising and resistance mutations1

TAGRISSO Mechanism of Action

References:
1. TAGRISSO [package insert]. Wilmington, DE: AstraZeneca Pharmaceuticals LP; 2018. 2. Cross DAE, Ashton SE, Ghiorghiu S, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014;4:1046-1061. 3. Ramalingam SS, Yang JCH, Lee CK, et al. Osimertinib as first-line treatment of EGFR mutation-positive advanced non–small-cell lung cancer. J Clin Oncol. 2017;35:1-11. doi:10.1200/JCO.2017.74.7576. 4. Varrone A, Varnas 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. Presented at: American Association for Cancer Research Meeting; April 14-18; Chicago, IL.