Drug intelligence / Profile preview

ACE-232 + dexamethasone + fludrocortisone

Development stage
Unknown
Lead developer
Acerand Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

**ACE-232 + dexamethasone + fludrocortisone** is an investigational oral combination therapy evaluated in clinical trials for metastatic castration-resistant prostate cancer (mCRPC). ACE-232 is a highly potent and selective small-molecule inhibitor of the enzyme CYP11A1, which plays a critical role in steroid hormone biosynthesis, including androgen production[1][3][5]. Dexamethasone is a synthetic glucocorticoid used as an anti-inflammatory and immunosuppressant, and fludrocortisone is a synthetic corticosteroid with mineralocorticoid properties used to manage adrenal insufficiency. The combination aims to suppress androgen and steroid hormone synthesis through CYP11A1 inhibition (ACE-232), while dexamethasone and fludrocortisone compensate for secondary corticosteroid deficiencies and help mitigate toxicity from steroid depletion[5]. This regimen is currently under Phase 1 clinical testing. It is designed to address androgen-dependent and androgen-refractory prostate cancers, especially in patients resistant to androgen receptor pathway inhibitors such as enzalutamide and abiraterone[1][3][5]. Development and clinical trials are led by Acerand Therapeutics[1][3][8].

02

Targets

GR (Glucocorticoid receptor)MR (Mineralocorticoid receptor)SMO (Smoothened)CYP11A1 (Cholesterol side chain cleavage enzyme)

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