A Phase I/II, Multicenter, Open-label Study of EGFRmut-TKI EGF816, Administered Orally in Adult Patients With EGFRmut Solid Malignancies

Inclusion Criteria: (For all patients unless otherwise specified)

- Histologically or cytologically confirmed locally advanced (stage IIIB not amenable to
definitive multi-modality therapy including surgery) or metastatic (stage IV) EGFR
mutant NSCLC.

- Patients with controlled brain metastases

- ECOG performance status: Phase I part: 0, 1, or 2; Phase II part: 0 or 1

- Presence of at least one measurable lesion according to RECIST 1.1

- Patients who are either HBsAg positive or HBV-DNA positive must be willing and able to
take antiviral therapy 1-2 weeks prior to 1st dose of EGF816 treatment and continue on
antiviral therapy for at least 4 weeks after the last dose of EGF816

- Patients must have negative hepatitis C antibody (HCV-Ab) or positive HCV-Ab but
undetectable level of HCV-RNA. Note: patients with detectable HCV-RNA are not eligible
for the study.

- For Phase I: patients must have failed no more than 3 lines of any systemic
antineoplastic therapy for advanced NSCLC, including EGFR-TKI

- For Phase II: patients must be naïve from any systemic antineoplastic therapy in the
advanced setting. Patients who have failed no more than 1 cycle of systemic
antineoplastic therapy in the advanced setting are allowed.

Exclusion criteria: (Applies to all patients unless otherwise specified)

- Patients with a history or presence of ILD or interstitial pneumonitis, including
clinically significant radiation pneumonitis (i.e. affecting activities of daily
living or requiring therapeutic intervention)

- Presence or history of another malignancy

- Undergone a bone marrow or solid organ transplant

- Known history of human immunodeficiency virus (HIV) seropositivity (HIV testing is not
mandatory)

- Patients receiving concomitant immunosuppressive agents or chronic corticosteroids use
at the time of study entry except for control of brain metastases, topical
applications, inhaled sprays, eye drops or local injections

- Patients with clinically significant, uncontrolled heart disease

- Any prior therapies ≤ 4 weeks prior to the first dose of study treatment

- Patients who are receiving treatment with medications that are known to be strong
inhibitors or inducers of CYP3A4/5 and cannot be discontinued 1 week prior to the
start of EGF816 treatment and for the duration of the study.

- Patients who have impairment of GI function or GI disease that may significantly alter
the absorption of EGF816 (e.g., ulcerative diseases, uncontrolled nausea, vomiting,
diarrhea, or malabsorption syndrome)

- Patients who are receiving treatment with any enzyme-inducing anticonvulsant that
cannot be discontinued at least 1 week before first dose of study treatment, and for
the duration of the study

- Women of child-bearing potential, defined as all women physiologically capable of
becoming pregnant, unless they are using highly effective methods of contraception

- Sexually active males unless they use a condom during intercourse while taking drug
and for 3 months after stopping treatment Other protocol-defined inclusion and
exclusion criteria may apply.