Drug intelligence / Profile preview

KTX-120

Development stage
Preclinical
Lead developer
Kymera Therapeutics
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

KTX-120 is a novel IRAKIMiD development candidate, a heterobifunctional small molecule designed to induce the selective degradation of both Interleukin-1 receptor-associated kinase 4 (IRAK4) and the immunomodulatory drug (IMiD) substrates Ikaros (IKZF1) and Aiolos (IKZF3). Developed by Kymera Therapeutics, KTX-120 utilizes an IMiD-based cereblon binder to co-opt the ubiquitin-proteasome system for targeted protein degradation. This dual-targeting approach is intended to provide synergistic antitumor activity in MYD88-mutant B-cell malignancies, such as diffuse large B-cell lymphoma (DLBCL), by addressing both the myddosome signaling pathway and essential transcription factors. Preclinical studies have shown that KTX-120 induces rapid cell death and significant tumor regressions in MYD88-mutant cell-derived and patient-derived xenograft models, with the potential for intermittent oral or intravenous dosing.

Other names
IRAKIMiD
02

Targets

IKZF1 (Ikaros family zinc finger protein 1)IKZF3 (Zinc finger protein Aiolos)IRAK4 (Interleukin-1 receptor associated kinase 4)CRBN (Cereblon)

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