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2-methylene-19-nor-(20S)-1alpha-hydroxy-bishomopregnacalciferol

Development stage
Preclinical
Lead developer
University of Wisconsin-Madison
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intraperitoneal, Topical, Transdermal, Parenteral, Rectal
01

Overview

2-methylene-19-nor-(20S)-1alpha-hydroxy-bishomopregnacalciferol (2MbisP) is a synthetic vitamin D analog developed by the University of Wisconsin-Madison through the Wisconsin Alumni Research Foundation (WARF). It is characterized by a modified side chain and the absence of the C19 methylene group. 2MbisP acts as a potent agonist of the vitamin D receptor (VDR) but is distinguished by its uniquely low calcemic activity; it exhibits minimal intestinal calcium transport activity and very low bone calcium mobilization. This profile makes it a promising therapeutic candidate for secondary hyperparathyroidism and renal osteodystrophy, as it can suppress parathyroid hormone (PTH) levels without the significant risk of hypercalcemia or hyperphosphatemia. Beyond mineral metabolism, 2MbisP has demonstrated anti-proliferative and pro-differentiation effects in various cancer cell lines, including myeloid leukemia and breast cancer, and has shown potential in treating autoimmune disorders like multiple sclerosis and type 1 diabetes, as well as skin diseases such as psoriasis.

Other names
2-methylene-19-nor-(20S)-1α-hydroxy-bishomopregnacalciferol2-methylene-19-nor-20(S)-1α-hydroxy-bishomopregnacalciferol
02

Targets

VDR (Vitamin D receptor)

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