Drug intelligence / Profile preview

INV-9956 + dexamethasone + fludrocortisone acetate

Development stage
Phase 2
Lead developer
Ionova Life Science
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination regimen used in clinical trials for advanced metastatic castration-resistant prostate cancer (mCRPC). It consists of INV-9956, an orally available, selective, and potent inhibitor of the cholesterol side chain cleavage enzyme (Cyp11A1), co-administered with dexamethasone (a synthetic glucocorticoid) and fludrocortisone acetate (a synthetic mineralocorticoid). INV-9956 potently inhibits the biosynthesis of pregnenolone and other androgens in adrenocortical cells, targeting androgen biosynthesis critical for prostate cancer progression, especially in drug-resistant settings. The inclusion of dexamethasone and fludrocortisone acetate serves as corticosteroid replacement therapy to mitigate adrenal insufficiency and potential adrenal toxicity from Cyp11A1 inhibition. The regimen is in Phase 1/2 trials for mCRPC and developed by Ionova Life Science. Fludrocortisone acetate is supplied as Florinef and is primarily used to replace aldosterone and manage various forms of adrenal insufficiency, with both mineralocorticoid and glucocorticoid actions[1][2][3][4][5][6][7][8][9].

Other names
fludrocortisone acetatedexamethasone
02

Targets

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

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