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abiraterone acetate + prednisone + exemestane

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Abiraterone acetate + prednisone + exemestane is a combination therapy investigated primarily for the treatment of estrogen receptor-positive (ER+) metastatic breast cancer in postmenopausal women who have progressed after nonsteroidal aromatase inhibitor therapy. Abiraterone acetate is a prodrug of abiraterone, an oral small molecule that inhibits androgen biosynthesis by blocking the enzyme cytochrome P450 17A1 (CYP17A1), thereby reducing androgen and cortisol production. Prednisone is co-administered as glucocorticoid replacement to mitigate mineralocorticoid excess caused by CYP17A1 inhibition. Exemestane is an irreversible steroidal aromatase inhibitor that suppresses estrogen synthesis. The rationale for this combination is to achieve dual suppression of both androgen and estrogen signaling pathways, which may contribute to resistance in ER+ metastatic breast cancer[1][3][4]. This regimen has also been studied in clinical trials but did not show improved outcomes compared with exemestane alone in this setting[1][3].

Brand names
Yonsa
02

Targets

CYP19A1 (Aromatase)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)

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