Potent Preclinical Antitumor Activity Demonstrated by Janpix’s Selective STAT3 & STAT5 Monovalent Degraders to be presented at the Virtual Annual Meetings of the European Hematology Association and American Association for Cancer Research (Part II)
June 15, 2020 08:00 ET | Source: Janpix Inc.
CAMBRIDGE, Mass., June 15, 2020 (GLOBE NEWSWIRE) — Janpix Inc., a biotechnology company developing monovalent small molecule protein degraders as novel therapeutics, today announced the company will present preclinical data showing the characterization of novel, highly selective and potent monovalent degraders of STAT3 & STAT5 proteins. This is the first time that a monovalent small molecule has been shown to degrade both, STAT3 and STAT5. These compounds show activity across multiple hematologic malignancies including acute myelogenous leukemia (AML) and T-cell prolymphocytic leukemia (T-PLL). Data will be shared in poster presentations during the 2020 European Hematology Association Virtual Meeting starting on Monday, June 15th, and the 2020 American Association for Cancer Research Virtual Annual Meeting II starting on Monday, June 22th.
STAT3 and STAT5, are transcription factors whose aberrant activation leads to the expression of genes associated with tumor cell proliferation, survival and drug resistance. Both proteins individually are attractive targets in cancer and their combined targeting could be synergistic as well as lower the likelihood of drug resistance formation. This development opens up interesting therapeutic avenues for hematologic and solid tumors through the modulation of these largely intractable proteins.
Highlights of the presentations include:
- Rapid, potent, and highly selective degradation of STAT3 & STAT5 in leukemic cells upon treatment with JPX-1188.
- Sustained (> 72h) STAT3 & STAT5 degradation of greater than 90% achieved with only 2 hours of exposure to JPX-1188, leading to repression of downstream signaling and induction of apoptotic cell death.
- Significant tumor regression in a systemic AML mouse model with no overt toxicity upon dosing of STAT3/5 degraders.
“As Janpix advances our STAT3/5 degraders towards the clinic, we continue to expand our understanding of the biological impact of dual STAT3/5 degradation,” said Patrick Gunning, CSO of Janpix Inc. “Our data also highlight the potential for STAT3/5 degraders to treat a broader set of leukemia patients, as most leukemic primary patient samples tested responded to our compounds. We plan to select a lead compound for IND-enabling studies later in 2020.”
About Janpix, Inc.:
Janpix Inc was launched in 2017 following seed financing by medicxi. The Company’s aim is to advance the discovery and clinical development of selective STAT monovalent degraders based on new structural insights and chemistry developed by Prof Patrick Gunning, a Canada Research Chair in Medicinal Chemistry and co-founder. Janpix has identified small molecule degraders of STAT3 and STAT5 that show therapeutic potential in a number of hematological and solid tumors. Janpix is focused on advancing pre-clinical programs into the clinic for these difficult to treat and refractory indications. For more information visit www.janpixbio.com
Ryo Imai Burns McClellan