On January 20, 2022 Tachyon Therapeutics, Inc. ("Tachyon" or "the Company"), a private biotechnology company creating novel therapeutics to unlock new pathways to treat advanced cancers, reported the presentation of data from its TACH101 program in a virtual poster presentation at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Gastrointestinal Cancer Symposium being held from January 20-22, 2022 (Press release, Tachyon Therapeutics, 20 20, 2022, View Source [SID1234605673]).

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The data demonstrate the potent anti-cancer activity of TACH101, a first-in-class small molecule inhibitor of KDM4 histone demethylase, in preclinical models of gastrointestinal (GI) cancers. KDM4 is a novel target for cancer therapy, playing an important role in the self-renewal of cancer stem cells and regulating epigenetic processes. Overexpression of KDM4 can lead to inhibition of apoptosis, genetic instability, uncontrolled gene expression and cell proliferation, and metastasis. The Company plans to initiate a first-in-human Phase 1 clinical trial in the first half of 2022.

"These preclinical data for TACH101 highlight its potent anti-tumor activity in gastric, esophageal, and colorectal xenograft models and provide support for KDM4 as an important new target for cancer therapy," said Frank Perabo, MD, PhD, CEO of Tachyon Therapeutics. "There is a significant unmet need for new therapeutic options for patients with GI cancers, and we are excited about advancing TACH101 into a first-in-human clinical trial and develop it as a potential new treatment for GI cancers."

Highlights from the ASCO (Free ASCO Whitepaper)-GI poster presentation (Abstract #132) are summarized below:

TACH101 showed potent anti-proliferative activity in GI cancer cell lines and organoid models with IC50 as low as 0.001 µM.
Further evaluation in a panel of colorectal cancer (CRC) patient-derived xenograft (PDX) and organoid models showed a strong correlation of TACH101 sensitivity with MSI-H status (IC50 ranging from 0.001 – 0.270 µM).
TACH101 induced apoptosis in human CRC (HT-29) and esophageal (KYSE-150) cancer cell lines with EC50s of 0.033 μM and 0.092 μM, respectively.
In vivo, TACH101 triggered effective tumor control (≥70%) in xenograft models of CRC (SU60), esophageal (KYSE-150) and gastric (GXA-3036) cancers.
TACH101 treatment caused 86% repression of PNUTS mRNA (a direct target of KDM4) as well as a 51% increase in H3K9me3 (a mark of repressed transcription).
The virtual poster presentation titled, "TACH101, a First-in-Class KDM4 Inhibitor for Treatment of Gastrointestinal Cancers," is available for on-demand viewing beginning at 9 am EST on January 20 by conference attendees on the ASCO (Free ASCO Whitepaper)-GI conference website at View Source