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 per investigator assessment
* Patients who are either Hepatitis B surface antigen (HBsAg) positive or hepatitis B virus (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: (For all patients unless otherwise specified)

* Patients with a history or presence of interstitial lung disease (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
* 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 gastrointestinal (GI) function or GI disease that may significantly alter the absorption of EGF816
* 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.