Drug intelligence / Profile preview

inlexisertib

Development stage
Phase 2
Lead developer
Deciphera Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Inlexisertib is an orally bioavailable, selective small molecule inhibitor of the serine/threonine-protein kinases **ULK1** and **ULK2**, developed for the potential treatment of various cancers. It inhibits autophagosome formation by suppressing phosphorylation of ULK1/2 substrates such as ATG13, thereby blocking autophagy. This mechanism is particularly relevant in tumors, such as mutant RAS cancers, that depend on autophagy for survival and drug resistance. Inlexisertib is in clinical development, investigated both as monotherapy and in combination with other targeted anticancer agents such as trametinib, binimetinib, sotorasib, and ripretinib for a range of solid tumors, including gastrointestinal stromal tumors and KRAS mutant cancers[1][2][3][5][7][9].

Other names
inlexisertib [INN]2543673-19-2
02

Targets

ULK2 (Unc-51-like kinase 2)

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