Drug intelligence / Profile preview

ORG2058

Development stage
Unknown
Lead developer
Organon
Modality
Small Molecules
Administration
In Vitro
01

Overview

ORG2058 is a synthetic **progestin of the 19-norprogesterone group** that was developed as a research tool and never marketed. It has **very high affinity for the progesterone receptor** (about 775% that of natural progesterone), shows negligible affinity for the estrogen and glucocorticoid receptors, and has slightly lower mineralocorticoid receptor affinity than progesterone. ORG2058 has been extensively used in scientific research to study progesterone receptor function, hormone-dependent cancer cell proliferation, and modulation of gene expression such as BRCA1. Its mechanism involves acting as a potent **orthosteric agonist of the progesterone receptor**, thereby mediating downstream effects on cell proliferation, gene expression (e.g., BRCA1 induction), and metabolic pathways. The compound has also served as a pharmacological tool to dissect progestogenic activities in in vitro and in vivo systems[1][2][3][5][6][7][8][11][13][15].

Other names
16α-ethyl-21-hydroxy-19-norprogesterone
02

Targets

ER (Estrogen receptor)mPRα (Membrane progesterone receptor alpha)PR (Progesterone receptor)

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