Drug intelligence / Profile preview

IK-595

Development stage
Unknown
Lead developer
ImageneBio
Modality
Small Molecules
Administration
Oral
01

Overview

IK-595 is an orally bioavailable small molecule described as a MEK/RAF molecular glue and dual kinase inhibitor with potential antineoplastic activity. It is designed to trap MEK and RAF in an inactive complex, thereby more completely inhibiting RAS pathway signaling than existing inhibitors. This mechanism prevents CRAF-mediated bypass and reactivation of the pathway, which are common resistance mechanisms to first-generation MEK inhibitors. Preclinical studies have shown robust antitumor activity in models harboring KRAS, NRAS, non-V600E BRAF mutations, and CRAF amplification. The drug is being developed by Ikena Oncology for use as monotherapy or potentially in combination with other targeted therapies for patients with advanced solid tumors characterized by RAS or RAF alterations[1][2][4][5][6].

02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RAF1 (c-Raf-1 (Y340D/Y341D))BRAF (B-Raf proto-oncogene, serine/threonine kinase)

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