Drug intelligence / Profile preview

orteronel + LHRH agonist

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

Orteronel (TAK-700) is a selective, non-steroidal inhibitor of the enzyme CYP17A1, specifically targeting its 17,20 lyase activity. This enzyme is crucial for androgen synthesis in the testes, adrenal glands, and prostate cancer cells. By inhibiting 17,20 lyase, orteronel reduces androgen production more selectively than other agents that also inhibit 17α-hydroxylase. The combination with an LHRH (luteinizing hormone-releasing hormone) agonist further suppresses testicular androgen production by downregulating gonadotropin release from the pituitary gland. This dual approach aims to achieve more complete androgen deprivation than standard therapies alone and is under investigation primarily for advanced or high-risk prostate cancer[1][2][4][6].

Other names
steroid 17alpha-monooxygenase TAK-700steroid17alpha-monooxygenase TAK-700steroid-17alpha-monooxygenase TAK-700selective 17,20 lyase inhibitor + LHRH agonist
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GnRHR (Gonadotropin-releasing hormone receptor)

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