2025 Spring International Convention of
The Pharmaceutical Society of Korea

PSK

2025 Spring
International Convention of PSK

04.21(MON) - 04.22(TUE)
D+25

Abstracts

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P4-5

Novel orally available HPK1 inhibitor enhanced in vitro immune response and exhibited in vivo anti-tumor efficacy

 

  • Min Jeong Ahn1,2, Eun Hye Kim1, Yunha Choi1,3, Pilho Kim1, Chong Hak Chae1, Sun Young Rha4,5,6,7, Jung Hyu Shin8, Chan Woo Kim8, Sang Woo Kim9, Seong Hwan Kim*1,2
  • 1Therapeutics & Biotechnology Division, Korea Research Institute of Chemical Technology, Daejeon, Korea
  • 2Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon, Korea
  • 3Department of Medicinal Chemistry and Pharmacology, University of Science and Technology, Daejeon, Korea
  • 4Song-dang Institute for Cancer Research, Yonsei University College of Medicine, Seoul, Korea
  • 5Department of Medicine, Yonsei University College of Medicine, Seoul, Korea
  • 6Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul, Korea
  • 7Division of Medical Oncology, Department of Internal Medicine, Yonsei Cancer Center, Yonsei University Health System, Seoul, Korea
  • 8Cancer Immunotherapy Evaluation Team, Non-Clinical Evaluation Center (NCEC), OSONG Medical Innovation Foundation (KBIOHealth), Cheongju, Korea
  • 9MDBiopharm, Seoul, Korea

Hematopoietic progenitor kinase 1 (HPK1) is a kinase that negatively regulates T-cell signaling by phosphorylating SLP-76, a critical mediator of T-cell receptor activation. In recent data, the genetic ablation or the pharmacological inhibition of HPK1 kinase activity has been shown to improve immune response to cancers. Here, we present KHK-6 as an HPK1 compound that enhances T-cell activation in vitro. Furthermore, we demonstrated that MD302, optimized from KHK-6, shows potent antitumor efficacy both in vitro and in the CT26 syngeneic mouse model with good pharmacokinetic properties. In the humanized mouse model, the combination of MD302 with Nivolumab (PD-L1 inhibitor) more potently inhibited tumor growth with statistical significance. The safety of the orally bioavailable MD302 in the ongoing toxicological studies could be a druggable target for immunomodulatory immunotherapy. 

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TODAY 2025. 05. 17

2025 Spring Convention

D+25

Conference infomation

Conference Schedule
Apr. 21(Mon) ~ 22(Tue), 2025
Conference Venue
Daegu Exhibition & Convention Center (EXCO) 10 Exco-ro, Buk-gu, Daegu, Republic of Korea
Location
Early Registration Period
Feb. 24(Mon) ~ Apr. 14(Mon), 2025
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Abstract Submission Period
Feb. 24(Mon) ~ Apr. 3(Thu), 2025
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