2222344-98-9

Usage

Uses

Used in Pharmaceutical Industry:
(8R,9S,10R,11S,13S,14S,17S)-17-(3,3-dimethylbut-1-yn-1-yl)-17-hydroxy-11-(4-(isopropyl(methyl)amino)phenyl)-13-methyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one is used as a potential hormone receptor modulator or inhibitor for the development of new drugs targeting steroid-related conditions.
Used in Research and Development:
(8R,9S,10R,11S,13S,14S,17S)-17-(3,3-dimethylbut-1-yn-1-yl)-17-hydroxy-11-(4-(isopropyl(methyl)amino)phenyl)-13-methyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one is used as a research tool for studying the interactions of steroidal compounds with enzymes and proteins involved in steroid metabolism and signaling pathways, which can contribute to the understanding of various diseases and the development of targeted therapies.

Upstream product

• 39931-89-0 (5R,10R,13S,17S)-13-methyl-1,2,4,6,7,8,12,13,14,15,16,17-dodecahydrospiro[5,10-epoxycyclopenta[a]phenanthrene-3,2'-[1,3]dioxolan]-17-ol 
• 39931-88-9 (5'R,10'R,13'S)-13'-methyl-1',2',6',7',8',12',13',14',15',16'-decahydro-17'H-spiro[1,3-dioxolane-2,3'-[5,10]epoxycyclopenta[a]phenanthren]-17'-one 
• 5571-36-8 ethylene deltenone 
• 61684-98-8 4-(N-isopropyl-N-methylamino)phenyl bromide 

Relevant academic research and scientific papers

SOLID FORMS AND FORMULATIONS COMPRISING A GLUCOCORTICOID RECEPTOR ANTAGONIST AND USES THEREOF

The present invention relates generally to formulations and methods for treating cancer. Provided herein are formulations comprising substituted steroidal derivatives. The subject formulations are useful for the treatment of cancer.

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101)

The glucocorticoid receptor (GR) has been linked to therapy resistance across a wide range of cancer types. Preclinical data suggest that antagonists of this nuclear receptor may enhance the activity of anticancer therapy. The first-generation GR antagonist mifepristone is currently undergoing clinical evaluation in various oncology settings. Structure-based modification of mifepristone led to the discovery of ORIC-101 (28), a highly potent steroidal GR antagonist with reduced androgen receptor (AR) agonistic activity amenable for dosing in androgen receptor positive tumors and with improved CYP2C8 and CYP2C9 inhibition profile to minimize drug-drug interaction potential. Unlike mifepristone, 28 could be codosed with chemotherapeutic agents readily metabolized by CYP2C8 such as paclitaxel. Furthermore, 28 demonstrated in vivo antitumor activity by enhancing response to chemotherapy in the GR+ OVCAR5 ovarian cancer xenograft model. Clinical evaluation of safety and therapeutic potential of 28 is underway.

INHIBITORS OF GLUCOCORTICOID RECEPTOR

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.