Drug intelligence / Profile preview

GDC-0810 + palbociclib

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

Overview

GDC-0810 + palbociclib is an investigational **combination therapy** for advanced or metastatic estrogen receptor positive, HER2 negative breast cancer. GDC-0810 (also known as ARN-810) is an oral, non-steroidal **selective estrogen receptor degrader (SERD)** that induces degradation of the estrogen receptor and blocks its signaling. Palbociclib is an oral **cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor** that prevents cell cycle progression by inhibiting phosphorylation of retinoblastoma protein. The combination was studied to assess safety, pharmacokinetics, and preliminary anti-tumor activity, typically in postmenopausal women or those rendered postmenopausal by ovarian suppression. Clinical trials found the combination to be generally safe and tolerable, with a safety profile consistent with other endocrine therapies in both monotherapy and combination settings[1][3][5][7].

Other names
ARN-810 + palbociclibGDC-0810 + IBRANCE
02

Targets

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

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