TIGER-1: Safety and Efficacy Study of Rociletinib (CO-1686) or Erlotinib in Patients With EGFR-mutant/Metastatic NSCLC Who Have Not Had Any Previous EGFR Directed Therapy

Inclusion Criteria:

1. Histologically or cytologically confirmed metastatic or unresectable locallyadvanced/metastatic NSCLC

2. Documented evidence of a tumor with activating EGFR mutations by local testing.Patients with exon 20 insertions are not eligible with the exception of patients withdocumented evidence of the exon 20 insertion A763_Y764insFQEA in the EGFR gene

3. Have undergone a biopsy or surgical resection of either primary or metastatic tumortissue within 60 days of the first day of study treatment, C1D1, and have tissueavailable to send to sponsor laboratories or are able to undergo a biopsy duringscreening and provide tissue to sponsor laboratories

4. Measureable disease according to RECIST Version 1.1

5. Life expectancy of at least 3 months

6. ECOG (Eastern Cooperative Oncology Group) performance status of 0 to 1

7. Minimum age 18 years (in certain territories, the minimum age requirement may behigher (e.g. 20 years in Japan and Taiwan)

8. Adequate hematological and biological function, confirmed by defined laboratory values

9. Written consent on an IRB/IEC-approved Informed Consent Form (ICF) prior to anystudy-specific evaluation

Exclusion Criteria:

1. Documented evidence of an exon 20 insertion activating mutation other thanA763_Y764insFQEA in the EGFR gene

2. Prior treatment with cytotoxic chemotherapy for advanced NSCLC; neoadjuvant/adjuvantchemotherapy is permitted if at least 6 months has elapsed between the end ofchemotherapy and randomization

3. Active second malignancy; i.e., patient known to have potentially fatal cancer presentfor which he/she may be (but not necessarily) currently receiving treatment

4. Patients with a history of malignancy that has been completely treated, and currentlywith no evidence of that cancer, are permitted to enroll in the trial provided allchemotherapy was completed > 6 months prior and/or bone marrow transplant > 2 yearsprior to first day of study treatment

5. Known pre-existing interstitial lung disease

6. Brain metastases

7. Treatment with prohibited medications less than or equal to 14 days prior to first dayof study treatment

8. Patients who are currently receiving treatment with any medications that have thepotential to prolong the QT interval if that treatment cannot be either discontinuedor switched to a different medication prior to administration of study drug

9. Prior treatment with EGFR TKIs (e.g. erlotinib, gefitinib, neratinib, afatinib,AZD9291, or dacomitinib), rociletinib or other drugs that target mutant EGFR

10. Clinically significant abnormal 12-lead ECG, QT interval corrected using Fridericia'smethod (QTCF) > 450 ms

11. Inability to measure QT interval on ECG

12. Personal or family history of long QT syndrome

13. Implantable pacemaker or implantable cardioverter defibrillator

14. Resting bradycardia < 55 beats/min

15. Non-study related surgical procedures less than or equal to 7 days prior toadministration of study drug. In all cases, the patient must be sufficiently recoveredand stable before treatment administration.

16. Females who are pregnant or breastfeeding

17. Refusal to use adequate contraception for fertile patients (females and males) for 12weeks after the last dose of rociletinib and 2 weeks after the last dose of erlotinib

18. Presence of any serious or unstable concomitant systemic disorder incompatible withthe clinical study

19. Any other reason the investigator considers the patient should not participate in thestudy