Drug intelligence / Profile preview

dalotuzumab + MK-0752

Development stage
Unknown
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

**dalotuzumab + MK-0752** is an investigational combination therapy composed of dalotuzumab, a humanized monoclonal antibody targeting insulin-like growth factor 1 receptor (IGF-1R), and MK-0752, an oral, small-molecule gamma secretase inhibitor that blocks Notch receptor activation. The combination has been studied in early-phase clinical trials for advanced malignancies, including metastatic or recurrent platinum-resistant ovarian cancer, fallopian tube cancer, primary peritoneal cancer, and metastatic/recurrent wild-type KRAS colorectal cancer. Dalotuzumab acts by inhibiting signaling through IGF-1R, thus suppressing cancer cell proliferation and survival. MK-0752 inhibits gamma secretase, an intramembrane protease essential for Notch receptor activation, thereby blocking Notch signaling pathways involved in cancer cell maintenance and resistance. The combination aims to target both IGF and Notch pathways to enhance anti-tumor activity[1][3].

02

Targets

IGF-1R (Insulin-like growth factor 1 receptor)GSEC (Gamma-Secretase Complex)

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