Drug intelligence / Profile preview

zavondemstat

Development stage
Phase 1
Lead developer
Tachyon Therapeutics
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Zavondemstat is a first-in-class, selective small molecule inhibitor of the histone lysine demethylase KDM4 family (also known as JMJD2). It acts as an epigenetic modulator by inhibiting KDM4 isoforms A-D, with reported IC50 values around 80 nM. Zavondemstat has demonstrated robust anti-proliferative and antitumor activity in preclinical models across various solid tumors and hematological malignancies. Its mechanism involves altering histone methylation states, particularly at H3K9 and H3K36, thereby affecting gene expression relevant to cancer cell proliferation. The drug is being developed primarily for oncology indications, including advanced solid tumors and hematological cancers[1][2][3][5][9].

Other names
zavondemstat [INN]TACH101TACH-101TACH 101QC8222 free baseQC-8222 free baseQC 8222 free base(R)-3-(((7-(4-Isopropylphenyl)(methyl)amino)chroman-4-yl)methyl)aminoisonicotinic acid
02

Targets

KDM4BKDM4A (Lysine-specific demethylase 4A)KDM4D (Lysine-specific demethylase 4D)KDM4C (Lysine-specific demethylase 4C)

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