Drug intelligence / Profile preview

lerociclib + letrozole or fulvestrant

Development stage
Unknown
Lead developer
Genor Biopharma
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Lerociclib is a novel, oral, small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), developed for continuous daily dosing. It is being investigated in combination with endocrine therapies such as letrozole (an aromatase inhibitor) or fulvestrant (an estrogen receptor antagonist) for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. In phase III clinical trials, lerociclib combined with either letrozole or fulvestrant has demonstrated significant improvement in progression-free survival and a favorable safety profile compared to placebo plus endocrine therapy[1][2]. The drug is positioned as a first-line option for HR+/HER2- advanced breast cancer, including patients who have relapsed or progressed on prior endocrine therapy.

02

Targets

CYP19A1 (Aromatase)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)

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