Drug intelligence / Profile preview

abemaciclib + abiraterone acetate + prednisolone

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

**Abemaciclib + abiraterone acetate + prednisolone** is an investigational oral combination regimen studied in patients with metastatic castration-resistant prostate cancer (mCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC). - **Abemaciclib** is a selective, oral inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), blocking phosphorylation of the retinoblastoma protein and resulting in cell cycle arrest in the G1 phase. - **Abiraterone acetate** is an oral prodrug of abiraterone, an inhibitor of the enzyme CYP17A1 (17α-hydroxylase/C17,20-lyase), reducing androgen production from testicular, adrenal, and prostate tumor tissue. - **Prednisolone** is a synthetic glucocorticoid used to prevent mineralocorticoid excess due to abiraterone-induced CYP17A1 inhibition. The combination aims to simultaneously inhibit androgen signaling and cell cycle progression in prostate cancer cells. Clinical development has tested this combination primarily in the first-line treatment of mCRPC and mHSPC[4][3][5].

Other names
abemaciclib + abiraterone acetate + prednisone
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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