Drug intelligence / Profile preview

LSZ102 + ribociclib

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

Overview

LSZ102 + ribociclib is a combination therapy consisting of LSZ102, an investigational oral selective estrogen receptor degrader (SERD), and ribociclib (Kisqali), a CDK4/6 inhibitor. This combination has been studied for the treatment of estrogen receptor-positive (ER+) breast cancer. In clinical trials, the combination demonstrated promising clinical activity with a manageable safety profile in heavily pretreated patients with ER+ breast cancer who had progressed after prior endocrine therapy. The combination works through dual mechanisms: LSZ102 degrades estrogen receptors while ribociclib blocks CDK4/6 proteins that help cancer cells grow and divide.

02

Targets

CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)

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