Drug intelligence / Profile preview

MK-0752 + letrozole

Development stage
Phase 4
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-0752 + letrozole is an investigational combination therapy evaluated for the treatment of early-stage, estrogen receptor (ER)-positive breast cancer. MK-0752 is a small molecule gamma-secretase inhibitor that targets the Notch signaling pathway, which plays a role in tumor cell survival and resistance to endocrine therapies. Letrozole is an aromatase inhibitor used as standard hormonal therapy for ER-positive breast cancer by reducing estrogen production. The rationale behind this combination is that inhibition of the Notch pathway by MK-0752 may help overcome or delay resistance to endocrine therapy such as letrozole. Clinical studies have focused on assessing safety, tolerability, and preliminary efficacy of this combination in patients with early-stage ER-positive breast cancer prior to surgery[1][5][8].

02

Targets

CYP19A1 (Aromatase)GSEC (Gamma-Secretase Complex)

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