MOA

TAGRISSO: 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*
Potently† inhibits both EGFRm and EGFR T790M1-3*
Potently† inhibits both EGFRm and EGFR T790M1-3
Minimal activity against wild-type EGFR1*
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 barrier4
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See how TAGRISSO selectively targets both EGFR sensitising and resistance mutations1

View TAGRISSO Mechanism of Action

References: 1. AstraZeneca Pharmaceuticals. TAGRISSO® (osimertinib). Summary of Product Characteristics, 2021. 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(9):1046-1061. 3. Ramalingam SS, Yang JC, Lee CK, et al. Osimertinib as first-line treatment of EGFR mutation–positive advanced non–small-cell lung cancer. J Clin Oncol. 2018;36(9):841-849. 4. Varrone A, Varnäs K, Jucaite A, et al. A PET study in healthy subjects of brain exposure of 11C-labelled osimertinib – a drug intended for treatment of brain metastases in non-small cell lung cancer. J Cereb Blood Flow Metab. 2020;40(4):799-807.

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