BPI-9016M / Betta Pharma - LARVOL DELTA

Safety, efficacy and pharmacokinetics of BPI-9016M in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic non-small-cell lung cancer: a phase Ib study. (PubMed, BMC Cancer) - P1 | "BPI-9016M showed manageable safety profile in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic NSCLC, but showed limited efficacy."

Journal • Metastases • P1 data • PK/PD data • Hematological Disorders • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thrombocytopenia • MET

Radiosensitizing effect of c-Met kinase inhibitor BPI-9016M in esophageal squamous cell carcinoma cells in vitro and in vivo. (PubMed, Ann Transl Med) - "The radiosensitizing effects of BPI-9016M were due to increased apoptosis, such as the up-regulation of cleaved-caspase 3 and 9, down-regulation of mutant P53 and Bcl-2, the decreased of phosphorylation of ATR and ATM, and the inhibition of γ-H2AX accumulation in vitro and in vivo. These findings indicated that BPI-9016M exerts a radiosensitizing effect and enhances apoptosis by inhibiting homologous recombination DNA repair in irradiated ESCC cells."

IO biomarker • Journal • Preclinical • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • BCL2 • CASP3 • CASP9 • CHEK1 • CHEK2 • HGF • HRD • MET • TP53

BPI-9016M, a novel c-Met inhibitor, in pretreated advanced solid tumor: Results from a first-in-human, phase I, dose-escalation study. (ASCO 2018) - P1,P1/2; "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)."

P1 data • Non Small Cell Lung Cancer

BPI-9016M, a novel c-Met inhibitor, in pretreated advanced solid tumor: results from a first-in-human, phase 1, dose-escalation study (ESMO 2018) - P1, P1/2; "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)."

P1 data • Non Small Cell Lung Cancer

BPI-9016M, a Novel c-Met Inhibitor, in Pretreated Advanced Solid Tumor: Results from a First-In-Human, Phase 1, Dose-Escalation Study (IASLC-WCLC 2018) - P1, P1/2; "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). "

P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic Cancer

Safety and Pharmacokinetics of BPI-9016M in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=20; Completed; Sponsor: Betta Pharmaceuticals Co., Ltd.; Recruiting ➔ Completed; N=30 ➔ 20

Clinical • Enrollment change • Trial completion • Oncology • Solid Tumor

Safety, Efficacy and Pharmacokinetic of BPI-9016M in Patients With c-Met- Dysregulated Advanced NSCLC (clinicaltrials.gov) - P1; N=80; Recruiting; Sponsor: Betta Pharmaceuticals Co., Ltd.; Completed ➔ Recruiting; Trial completion date: Dec 2018 ➔ Nov 2024; Trial primary completion date: Dec 2018 ➔ Nov 2024

Clinical • Enrollment open • Trial completion date • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • MET

First-in-human phase I study of BPI-9016M, a dual MET/Axl inhibitor, in patients with non-small cell lung cancer. (PubMed, J Hematol Oncol) - P1; "BPI-9016M showed favorable safety and pharmacokinetic profiles, and no DLT was observed at doses up to 800 mg once daily. The promising antitumor activity in Chinese NSCLC patients supports further development of this tyrosine kinase inhibitor."

Clinical • Journal • P1 data

BPI-9016M, a c-Met inhibitor, suppresses tumor cell growth, migration and invasion of lung adenocarcinoma via miR203-DKK1. (PubMed, Theranostics) - "Furthermore, we observed significantly enhanced tumor cell growth inhibition upon combining BPI-9016M treatment with miR203 mimics or DKK1 siRNA. Our data indicated that BPI-9016M is an effective agent against lung adenocarcinoma, particularly in tumors with c-Met activation, and likely functions through upregulation of miR203 leading to reduced DKK1 expression."

Journal

Safety, Efficacy and Pharmacokinetic of BPI-9016M in Patients With c-Met- Dysregulated Advanced NSCLC (clinicaltrials.gov) - P1; N=77; Completed; Sponsor: Betta Pharmaceuticals Co., Ltd.; Recruiting ➔ Completed; Phase classification: P1/2 ➔ P1; N=50 ➔ 77

Clinical • Enrollment change • Phase classification • Trial completion