Drug intelligence / Profile preview

AUR1545

Development stage
Unknown
Lead developer
Auron Therapeutics
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Classical Binding Small Molecules → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

AUR1545 is a potent and selective small molecule degrader of the histone acetyltransferases KAT2A (lysine acetyltransferase 2A) and KAT2B (lysine acetyltransferase 2B). Developed by Auron Therapeutics, it was designed to target epigenetic regulators that are hijacked in cancer cells to maintain a highly plastic and proliferative state. By inducing rapid and selective degradation of KAT2A/B, AUR1545 inhibits tumor growth and promotes differentiation in preclinical models of acute myeloid leukemia (AML), small cell lung cancer (SCLC), and neuroendocrine tumors. The compound demonstrates high selectivity, picomolar potency for its targets, oral bioavailability, and significant anti-proliferative effects in vivo[1][3][4][5].

02

Targets

KAT2BKAT2A (Lysine acetyltransferase 2A)

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