Searchable abstracts of presentations at key conferences in endocrinology

ea0086p344 | Neuroendocrinology and Pituitary | SFEBES2022

CRN04894: an oral, nonpeptide adrenocorticotropic hormone (ACTH) receptor antagonist decreases basal and stimulated cortisol secretion in healthy volunteers

Trainer Peter , Ferrara-Cook Christine , Ayala Alejandro , Luo Rosa , Miller Stephanie , Wang Yang , Hernandez-Illas Martha , Scott Struthers R. , Betz Stephen , Krasner Alan

CRN04894 is a potent, orally bioavailable nonpeptide that is a highly selective antagonist for melanocortin type 2 receptor (MC2R). This receptor is found exclusively in the adrenal cortex and is the primary mediator of adrenal activation. We report results from a randomized, double-blinded, placebo-controlled (6 active:3 placebo/cohort), multiple ascending dose (40, 60, and 80 mg) study in health volunteers evaluating safety, pharmacokinetics, and pharmacodynamics of oral, on...

ea0070oc6.1 | Hot Topics (including COVID-19 | ECE2020

Effects of nonpeptide orally bioavailable ACTH antagonists on adrenal gland size and function in rats

Markison Stacy , Fowler Melissa , Athanacio Jon , Kredel Taylor , Antwan Agnes , Johns Michael , Tsivkovski Oleg , Cruz Shirley , Luo Rosa , Reinhart Greg , Kusnetzow Ana , Madan Ajay , Betz Stephen , Struthers R Scott

Cushing’s disease (CD) and Ectopic ACTH syndrome (EAS) stem from excess circulating adrenocorticotropic hormone (ACTH) and resulting hypercortisolemia. In CD, excess ACTH is secreted from pituitary tumors, whereas excess ACTH in EAS arises from nonpituitary tumors. ACTH acts on the adrenal melanocortin type 2 (MC2) receptor to control the synthesis and secretion of adrenal hormones, including the stress hormone cortisol (corticosterone in rats) which accounts for the com...