Clinical trial NCT00692640 (phase 1, status: completed)
Conditions: cancer, non-small cell lung cancer
ICD codes: C05.2, C10.0, C16.0, C16.4, C17.0, C17.1, C17.2, C78.00, C78.01, C78.02, D14.30, D14.31, D14.32, C34.2
Drugs: xl147 (sar245408), erlotinib
SMILES: COC1=CC=C(Cl)C(NC2=C(NS(=O)(=O)C3=CC(NC(=O)C(C)(C)N)=CC=C3)N=C3C=CC=CC3=N2)=C1, COCCOC1=CC2=C(C=C1OCCOC)C(NC1=CC(=CC=C1)C#C)=NC=N2
Eligibility criteria:

        Inclusion Criteria:

          -  Subjects accrue to one of two phases:

               -  in the Dose Escalation Phase, the subject has a histologically confirmed solid
                  tumor that is metastatic or unresectable and is no longer responding to therapies
                  known to prolong survival or to other standard therapies, or has disease for
                  which no standard therapy exists or for which monotherapy with erlotinib is
                  considered standard therapy.

               -  in the Cohort Expansion Phase, the subject has advanced or metastatic NSCLC that
                  is no longer responding to therapies known to prolong survival or to other
                  standard therapies and which:

                    1. has been previously or currently treated with erlotinib or gefitinib or

                    2. with the agreement of the sponsor, has been previously or is currently
                       treated with other EGFR/VEGFR tyrosine kinase inhibitors

          -  The subject has measurable or non-measurable lesions by the Response Evaluation
             Criteria in Solid Tumor (RECIST) criteria.

          -  At least 10 unstained slides of tumor tissue, archival or fresh, or paraffin block or
             a fresh tumor biopsy are identified and designated for central laboratory analysis.

          -  The subject has an Eastern Cooperative Oncology Group (ECOG) performance status ≤ 2.

          -  The subject has adequate organ and marrow function.

          -  The subject has a fasting plasma glucose ≤ 120 mg/dL at screening.

          -  The subject is ≥ 18 years old.

          -  The subject is capable of understanding and complying with the protocol requirements
             and has signed the informed consent document.

          -  Sexually active subjects (male and female) must use accepted methods of contraception
             during the course of the study and for at least 3 months after the last dose of
             protocol drug(s).

          -  Female subjects of childbearing potential must have a negative pregnancy test at
             screening.

        Exclusion Criteria:

          -  The subject has previously been treated with a selective PI3K inhibitor.

          -  The subject has received:

               -  cytotoxic chemotherapy (including investigational cytotoxic agents) or biologic
                  agents (antibodies, immune modulators, cytokines) within 3 weeks or has received
                  nitrosoureas or mitomycin C within 6 weeks before the scheduled first dose of
                  XL147

               -  a small-molecule kinase inhibitor (including investigational small molecule
                  kinase inhibitors) excluding small-molecule inhibitors of EGFR or non-cytotoxic
                  hormonal agent within 14 days of the scheduled first dose of XL147

               -  other investigational therapy (ie, not specified in exclusion criterion) within
                  28 days of the first scheduled dose of XL147

          -  The subject has not recovered from toxicity due to prior therapy to baseline or Common
             Terminology Criteria for Adverse Events (CTCAE) Grade 1 or less (except alopecia).

          -  The subject has a diagnosis of uncontrolled diabetes mellitus.

          -  The subject is currently receiving anticoagulation with therapeutic doses of warfarin
             (low-dose warfarin ≤ 1mg/day, heparin, and low-molecular weight heparins are
             permitted).

          -  The subject is taking oral corticosteroids chronically.

          -  The subject has prothrombin time/International Normalized Ratio and/or partial
             thromboplastin time test results at screening that are above 1.3x the laboratory upper
             limit of normal.

          -  The subject has uncontrolled intercurrent illness including but not limited to an
             active infection or hypertension that would limit compliance with study requirements.

          -  The subject has had congestive heart failure, unstable angina, a myocardial
             infarction, or a stroke within 3 months of entering the study.

          -  The subject has a baseline corrected QT interval (QTc) ≥ 460 ms.

          -  The subject has psychiatric illness/social situation(s) that would limit compliance
             with study requirements.

          -  The subject is known to be positive for the human immunodeficiency virus.

          -  The subject has a previously identified allergy or hypersensitivity to components of
             the XL147 formulation.

          -  The subject is pregnant or breastfeeding.

          -  The subject is unable or unwilling to abide by the study protocol or cooperate fully
             with the investigator or designee.