Drug intelligence / Profile preview

tibremciclib + fulvestrant

Development stage
Unknown
Lead developer
Betta Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Tibremciclib (BPI-16350) is a novel, potent, and selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), structurally similar to abemaciclib but with less inhibition of CDK9. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and accelerates the degradation of the estrogen receptor. The combination is being developed for hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer in patients who have progressed on prior endocrine therapy. Clinical studies have shown promising antitumor activity with an objective response rate exceeding 50% in this population[1][3][4][6].

Other names
BPI-16350 + fulvestranttibremciclib + fulvestrant
02

Targets

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

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