Last reviewed 2026-04-22 · How we verify

AZD9291 Dosing

AZD9291 is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, while sparing wild-type EGFR.

AZD9291 is a third-generation EGFR tyrosine kinase inhibitor that irreversibly binds to and inhibits mutant EGFR, including T790M resistance mutations, while sparing wild-type EGFR. Used for Non-small cell lung cancer with EGFR T790M mutation after progression on first- or second-generation EGFR inhibitors, EGFR-mutant non-small cell lung cancer (first-line treatment).

At a glance

Mechanism of action

AZD9291 (osimertinib) covalently binds to cysteine-797 in the ATP-binding pocket of mutant EGFR, providing sustained inhibition of oncogenic signaling. It is specifically designed to overcome resistance conferred by the T790M mutation that emerges during treatment with first- and second-generation EGFR inhibitors. The drug's selectivity for mutant over wild-type EGFR reduces toxicity to normal tissues.

Approved indications

• Non-small cell lung cancer with EGFR T790M mutation after progression on first- or second-generation EGFR inhibitors
• EGFR-mutant non-small cell lung cancer (first-line treatment)

Common side effects

• Diarrhea
• Rash
• Nausea
• Vomiting
• Stomatitis
• Decreased appetite
• Fatigue
• QT prolongation

Key clinical trials

• Prospective Non-Interventional Study Comparing Osimertinib +/- Chemotherapy for EGFR-Mutated NSCLC Patients
• An Open-Label, Single-Arm, Dose-Escalation Phase I Study Evaluating the Safety, Tolerability, and Preliminary Efficacy of EDB-102 in Patients With EGFR L858R-Mutant, Third-Generation TKI-Resistant Advanced Non-Small Cell Lung Cancer With Liver Metastases (PHASE1)
• A Study of Amivantamab and Lazertinib in Combination With Platinum-Based Chemotherapy Compared With Platinum-Based Chemotherapy in Patients With Epidermal Growth Factor Receptor (EGFR)-Mutated Locally Advanced or Metastatic Non- Small Cell Lung Cancer After Osimertinib Failure (PHASE3)
• AZD9291 in Combination With Ascending Doses of Novel Therapeutics (PHASE1)
• A Study to Evaluate ANS014004 in Combination With EGFR-TKI in Non-Small Cell Lung Cancer (PHASE1, PHASE2)
• Study to Assess the Effect of AZD9291 on the Blood Levels of Simvastatin in Patients With EGFRm+ NSCLC (PHASE1)
• Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of AZD9291, in Patients With EGFR Positive Non-small Cell Lung Cancer. Patients Will be Chosen From Those Who Have Already Been Prescribed an EGFR TKI Medicine (Such as Iressa or Tarceva) (PHASE1)
• A Study Evaluating the Safety, Pharmacokinetics (PK), and Preliminary Efficacy of ABBV-399 in Participants With Advanced Solid Tumors (PHASE1)

Primary sources

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