Drug intelligence / Profile preview

Orteronel + prednisone

Development stage
Discontinued
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Orteronel + prednisone is a combination therapy investigated primarily for the treatment of metastatic castration-resistant prostate cancer. Orteronel (TAK-700) is a novel small molecule inhibitor that selectively targets the 17,20 lyase activity of the enzyme Cytochrome P450 17A1 (CYP17A1). This inhibition reduces androgen synthesis in the testes, adrenal glands and prostate cancer cells—lowering circulating androgen levels and suppressing tumor growth in androgen-dependent cancers. Prednisone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties; it acts as an agonist at the glucocorticoid receptor to reduce inflammation and modulate immune responses. In clinical studies for prostate cancer, orteronel was administered together with low-dose prednisone to mitigate mineralocorticoid excess side effects associated with CYP17A1 inhibition[6][4][5].

02

Targets

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

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