Drug intelligence / Profile preview

inecalcitol

Development stage
Phase 2
Lead developer
Theramex
Modality
Small Molecules
Administration
Oral
01

Overview

Inecalcitol is a synthetic analog of calcitriol (the active form of vitamin D3) and acts as a potent agonist of the vitamin D3 receptor (VDR). By binding to and activating VDR, inecalcitol modulates VDR-mediated gene expression pathways. This activation leads to enhanced cellular differentiation, induction of tumor cell apoptosis, inhibition of tumor cell growth, and modulation of genes involved in cancer progression. Inecalcitol has demonstrated greater potency than calcitriol for inhibiting cancer cell proliferation while causing significantly less hypercalcemia. It is being investigated primarily for its antineoplastic activity against cancers such as prostate cancer and acute myeloid leukemia[1][2][3][5][6][8]. The drug was developed using synthetic chemistry methods.

Other names
(7E)-19-nor-9,10-seco-14beta-cholesta-5,7-dien-23-yne-1alpha,3beta,25-triolinecalcitol [INN]163217–09–2
02

Targets

VDR (Vitamin D receptor)

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