CRENESSITY inhibits ACTH secretion at the source1
Watch the video to learn more about how CRENESSITY works in the CRF pathway.
CRF has been identified as a primary regulator of the HPA axis, including production of adrenal cortisol, aldosterone, and androgens.2,3
CRENESSITY is a potent and selective CRF1 receptor antagonist.1,4,5 By selectively blocking CRF binding to CRF1 receptors in the pituitary gland, CRENESSITY1:
- Directly reduces ACTH
- Reduces downstream production of androgens
CRENESSITY improves androgen control and allows for GC dose reductions, enabling a transformational approach to managing CAH.1
ACTH=adrenocorticotropic hormone; CRF=corticotropin-releasing factor; CRF1=corticotropin-releasing factor type 1; GC=glucocorticoid; HPA=hypothalamic-pituitary-adrenal; MOA=mechanism of action; MOD=mechanism of disease.
REFERENCES
- Crenessity. Package insert. Neurocrine Biosciences, Inc.
- Schröder MAM, Claahsen-van der Grinten HL. Novel treatments for congenital adrenal hyperplasia. Rev Endocr Metab Disord. 2022;23(3):631-645. doi:10.1007/s11154-022-09717-w
- Mallappa A, Merke DP. Management challenges and therapeutic advances in congenital adrenal hyperplasia. Nat Rev. 2022;18(6):337-352. doi:10.1038/s41574-022-00655-w
- Gully D, Geslin M, Serva L, et al. 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A): a potent and selective corticotrophin-releasing factor(1) receptor antagonist. I. Biochemical and pharmacological characterization. J Pharmacol Exp Ther. 2002;301(1):322-332. doi:10.1124/jpet.301.1.322
- Fleck BA, Hoare SR, Pick RR, Bradbury MJ, Grigoriadis DE. Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor. J Pharmacol Exp Ther. 2012;341(2):518-531. doi:10.1124/jpet.111.188714