Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
The New England Journal of Medicine publishes the primary CAHtalyst™ Adult Phase 3 study results of Crinecerfont for the treatment of congenital adrenal hyperplasia (CAH). Classic congenital adrenal hyperplasia (CAH) due to 21-hydroxylase deficiency (21OHD) is a rare genetic disorder, affected by a lack of cortisol and/or aldosterone. Corticotropin-releasing factor type 1 receptor (CRF1) antagonism is shown to clinically decrease ACTH production and adrenal androgen levels.
Neurocrine's Crinecerfont is an investigational, selective CRF1 antagonist being developed to reduce and control excess adrenocorticotropic hormone (ACTH) and adrenal androgens. The phase 3 study meets primary and important key secondary endpoints, including a significant reduction in androstenedione levels and lowering glucocorticoid dosing.
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