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LY3039478 + prednisone
- Development stage
- Phase 1
- Lead developer
- Eli Lilly
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
LY3039478 + prednisone is a combination therapy consisting of **crenigacestat (LY3039478)**, an orally bioavailable small molecule inhibitor of the Notch signaling pathway, and **prednisone**, a synthetic glucocorticoid corticosteroid. Crenigacestat (LY3039478) inhibits the γ-secretase enzyme, thereby blocking the cleavage and activation of Notch receptors (Notch1-4), which are implicated in the proliferation and survival of various malignancies. Prednisone is used here primarily to reduce gastrointestinal toxicities associated with Notch inhibition without significantly affecting the pharmacokinetics of crenigacestat. This combination has been investigated in advanced or metastatic cancer patients to determine safety, maximum tolerated dose, pharmacokinetic interactions, and preliminary antitumor activity[1][3][7].
- Other names
- crenigacestat + prednisone
02
Targets
GSEC (Gamma-Secretase Complex)GR (Glucocorticoid receptor)NOTCH (Neurogenic locus notch homolog protein 3)
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