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  P1.01 - Advanced NSCLC (Not CME Accredited Session) (ID 933)

  • Event: WCLC 2018
  • Type: Poster Viewing in the Exhibit Hall
  • Track:
  • Presentations: 1
  • Moderators:
  • Coordinates: 9/24/2018, 16:45 - 18:00, Exhibit Hall

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    P1.01-37 - BPI-9016M, a Novel c-Met Inhibitor, in Pretreated Advanced Solid Tumor: Results from a First-In-Human, Phase 1, Dose-Escalation Study (ID 12317)

    16:45 - 18:00  |  Author(s): Lieming Ding
    • Abstract
    • Slides

    Background
    

    BPI-9016M (Betta Pharmaceuticals Co, Ltd, Hangzhou, China) is a potent targeted therapy that inhibits MET and Axl. This first-in-human study is to assess the safety, tolerability, and pharmacokinetics (PK) of BPI-9016M in patients with advanced solid tumor, and to determine the maximum tolerated dose (MTD) and recommended phase 2 dose (RP2D) for the phase Ib/II study.

    a9ded1e5ce5d75814730bb4caaf49419 Method
    

    Eligible patients were enrolled into sequential dose-escalating cohorts from 100 mg to 1000 mg given orally once per day continually following the conventional 3+3 design. The primary endpoint was safety and tolerability. MTD was defined as the highest dose level resulting in <1 of 3 dose limiting toxicities (DLTs). Blood levels of BPI-9016M were evaluated after single and multiple administration (NCT02478866).

    4c3880bb027f159e801041b1021e88e8 Result
    

    Twenty patients were enrolled and treated in 6 of 7 predefined dose cohorts (100 mg n=4, 200 mg n=3, 300 mg n=3, 450 mg n=4, 600 mg n=3, 800 mg n=3), dose escalation stopped at 800 mg due to saturation. All had stage IV non-small cell lung cancer (NSCLC) progressed on previous systemic therapy (including previous EGFR TKI in 16 patients). BPI-9016M was well-tolerated in all dose cohorts without DLT. The incidence of overall and grade 3/4 TRAEs was 85% and 45%, respectively. Common TRAEs included elevated ALT (45%), constipation (30%), elevated bilirubin (25%), and oral paresthesia (25%). Tumor response was seen in 1 patients in the 800 mg dose cohort. Systemic exposure to BPI-9016M (maximum plasma concentration and AUC) increased with increasing dose. Mean time to maximum plasma concentration and half-life were 2 to 5.33 hours and 8.09 to 22.3 hours, respectively. Two metabolites (M1, M2-2) were detected.

    8eea62084ca7e541d918e823422bd82e Conclusion
    

    BPI-9016M was well tolerated in patients with advanced solid tumor. A phase Ib study is ongoing to investigate the safety and activity of BPI-9016M in patients with c-Met-dysregulated advanced NSCLC (NCT02929290).

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