On April 10, 2021 Tachyon Therapeutics, Inc. ("Tachyon" or "the Company"), a research and development biotechnology company, reported a presentation of data of the Company’s novel compound, TACH101, at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) ("AACR") Annual Meeting (Press release, Tachyon Therapeutics, APR 10, 2021, View Source [SID1234577858]). TACH101, Tachyon’s lead product candidate, is a first-in-class, highly-selective inhibitor of KDM4 histone demethylase . AACR (Free AACR Whitepaper) is being held virtually from April 10-15 and May 17-21, 2021.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

"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 (Free AACR Whitepaper) 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 (Free AACR Whitepaper) Annual Meeting website at View Source!/9325/presentation/3226.