Drug intelligence / Profile preview

RO4929097 + exemestane

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

Overview

RO4929097 + exemestane is an investigational combination therapy consisting of RO4929097, a potent and selective small molecule inhibitor of gamma-secretase, and exemestane, an aromatase inhibitor. - **RO4929097** inhibits the gamma-secretase enzyme, thereby blocking Notch signaling—a pathway implicated in tumor cell growth and survival. It has demonstrated cytostatic effects in preclinical models and early clinical trials for various advanced solid tumors[1][2][3][5]. - **Exemestane** is a steroidal aromatase inhibitor that suppresses estrogen synthesis by irreversibly binding to the aromatase enzyme, commonly used in hormone receptor-positive breast cancer. The combination aims to target both the Notch signaling pathway (via RO4929097) and estrogen-driven tumor growth (via exemestane), potentially providing synergistic antitumor activity. This approach has been explored primarily in clinical research settings for advanced or refractory cancers.

02

Targets

CYP19A1 (Aromatase)GSEC (Gamma-Secretase Complex)NOTCH (Neurogenic locus notch homolog protein 3)

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