HOUSTON, TX, USA I April 10, 2021 I Tachyon Therapeutics, Inc. (“Tachyon” or “the Company”), a research and development biotechnology company, today announced a presentation of data of the Company’s novel compound, TACH101, at the American Association for Cancer Research (“AACR”) Annual Meeting. TACH101, Tachyon’s lead product candidate, is a first-in-class, highly-selective inhibitor of KDM4 histone demethylase. AACR is being held virtually from April 10-15 and May 17-21, 2021.

“We are excited to be presenting for the first time data on TACH101, a novel first-in-class inhibitor of KDM4,” stated Frank Perabo, MD, PhD, CEO of Tachyon Therapeutics. “KDM4 is an important epigenetic regulator of processes responsible for genomic instability, replicative immortality, evasion of apoptosis, deficiency in DNA repair and ability to metastasize across multiple tumor types. Extensive preclinical work shows compelling data for TACH101 to have broad potential in cancer treatment. To date, no small molecule inhibitor of KDM4 has reached clinical stage development, thus Tachyon would be the first to investigate this mechanistic pathway in a clinical trial.”

Highlights from the AACR presentation are summarized below:

  • TACH101 was broadly effective in the majority of 300 cancer cell lines screened.
  • TACH101 treatment induced cell cycle arrest in a dose-dependent manner, increasing the proportion of cells in S-phase by up to 3.2-fold after 72 hours of treatment.
  • TACH101 was potent in inducing apoptosis in human colorectal, esophageal, and triple negative breast cancer cell lines; the half maximal effective concentrations (EC50s) were in the nanomolar levels (ranging from 33 – 92 nM).
  • In vivo, TACH101 demonstrated effective tumor control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.
  • TACH101-treated tumors showed a significant reduction in the population of cancer stem cells by 4.4-fold.
  • Pharmacokinetic studies showed TACH101 exhibited low clearance, moderate volume of distribution, and good oral bioavailability in mouse, rat, and dog, and had little or no inhibitory effects on CYP enzyme activities.

“Changes in epigenetic regulation are present in all human cancers and act as the control center for a variety of cancer pathways,” states Mike Clarke, MD PhD, one of the Founders of Tachyon Therapeutics. “TACH101 is able to halt cancer progression by blocking KDM4 which participates in a majority of these pathways. Being able to reverse these alterations at the core level has far-reaching implications for cancer prevention and treatment and we are looking forward to further explore the full potential of this drug candidate.”

The poster presentation titled, “TACH101, a First-in-Class Pan-Inhibitor of KDM4 Histone Lysine Demethylases,” is available for viewing on the AACR Annual Meeting website at https://www.abstractsonline.com/pp8/#!/9325/presentation/3226.

About Tachyon Therapeutics Inc.

Tachyon Therapeutics, Inc. is an R&D focused biotechnology company advancing novel, first-in-class therapeutics for the treatment of advanced cancers. Tachyon operates with a dedicated internal core development team and a virtual external network of expertise to achieve one goal – advance our program with speed and innovation, without compromising the quality or integrity of our science. For more information, please visit www.tachyontx.com.

SOURCE: Tachyon Therapeutics