生物活性

• 描述PI3Kδ and PI3Kγ are the two isoforms of PI3K involved in the proliferation, development, maintenance, and transformation of immune cells. Tenalisib is a potent, small molecular inhibitor of both PI3Kδ and PI3Kγ with IC₅₀ values of 24.5 and 33.2 nM, respectively. Tenalisib at 2–7 μM resulted in a dose-dependent inhibition (>50%) in the growth of immortalized B-cell lymphoma cells (Raji, TOLEDO, KG-1, JEKO, REC-1). It demonstrated a potent inhibitory effect in the viability of DLBCL cell lines OCI-LY-1 and OCI-LY-10 (>50% inhibition at 0.1–0.7 μM). Also, tenalisib inhibited the production of pAKT in OCI-LY-1 and OCI-LY-10 cells with EC50 values of 6 and 70 nM, respectively. Treatment with 4 µM tenalisib led to increased cell death in patient-derived primary cells. Moreover, tenalisib at 5 µM significantly inhibited spheroid formation in PEO4, OVCAR-5 and CAOV-2 cells. In vivo, tenalisib markedly reduced tumor associated macrophages and angiogenesis, and also displayed synergy with checkpoint inhibition in syngeneic mouse models.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03471351	Classical Hodgkin Lymphoma	Phase 1 Phase 2	Recruiting	December 2019	United States, Illinois ... more >> University of Chicago Recruiting Chicago, Illinois, United States, 60637 Contact: Justin Kline, MD          United States, Michigan Rhizen Pharmaceuticals investigational trial site; Karmanos Cancer Institute, Recruiting Detroit, Michigan, United States, 48201 Contact: Radhakrishnan Ramchandren, MD    313-576-8739    clinicaltrials@rhizen.com    United States, Washington University of Washington Recruiting Seattle, Washington, United States, 98109 Contact: Ryan Lynch, MD Collapse <<
  NCT03770000	T Cell Lymphoma	Phase 1 Phase 2	Not yet recruiting	November 2020	United States, Texas ... more >> The University of Texas MD Anderson Cancer Center, Not yet recruiting Houston, Texas, United States, 77030 Contact: Swaminathan P Iyer, MD          The University of Texas MD Anderson Cancer Center, Not yet recruiting Houston, Texas, United States, 77030 Contact: Auris Huen, MD Collapse <<
  NCT03711604	Hematological Malignancies	Phase 1 Phase 2	Recruiting	December 2020	United States, Colorado ... more >> Division of Hematology, University of Colorado, Recruiting Denver, Colorado, United States, 80045 Contact: Brad Haverkos, MD, MPH, MS Collapse <<

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