Drug intelligence / Profile preview

dalpiciclib + letrozole

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Dalpiciclib + letrozole is an oral combination therapy used primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Dalpiciclib is a novel, selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor that blocks cell cycle progression by inhibiting phosphorylation of the retinoblastoma protein, thereby preventing cellular proliferation in cancer cells dependent on this pathway[2][3][4]. Letrozole is a third-generation nonsteroidal aromatase inhibitor that suppresses estrogen production by inhibiting the aromatase enzyme (CYP19A1), which converts androgens to estrogens; this reduction in estrogen levels slows or stops the growth of estrogen-dependent breast tumors[6][7]. The combination has demonstrated significant clinical benefit as first-line therapy for HR+/HER2- advanced breast cancer, improving progression-free survival and objective response rates compared to endocrine therapy alone[5]. Dalpiciclib was developed by Jiangsu Hengrui Pharmaceuticals.

Other names
dalpiciclib + letrozole/anastrozole
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)CYP19A1 (Aromatase)

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