Drug intelligence / Profile preview

dalpiciclib + letrozole (Hengrui Therapeutics)

Development stage
Phase 4
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Dalpiciclib + letrozole is a combination therapy consisting of dalpiciclib (marketed as Darsilide), a selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), and letrozole, a non-steroidal aromatase inhibitor. Dalpiciclib, developed by Jiangsu Hengrui Pharmaceuticals, works by blocking the cell cycle progression from G1 to S phase, thereby inhibiting tumor cell proliferation. Letrozole reduces estrogen levels by inhibiting the aromatase enzyme, which is crucial for the growth of hormone receptor-positive (HR+) breast cancer cells. This combination is primarily investigated for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer, as well as in neoadjuvant settings for HR-positive, HER2-positive breast cancer when combined with anti-HER2 therapies like trastuzumab and pertuzumab.

Brand names
Darsilide
Other names
Dalcilibdalpiciclibletrozole
02

Targets

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

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