Drug intelligence / Profile preview

bisphosphonates + eldecalcitol

Development stage
Unknown
Lead developer
Chugai Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of bisphosphonates and eldecalcitol, used primarily for the treatment of osteoporosis. Bisphosphonates are anti-resorptive agents that bind to bone mineral (hydroxyapatite) and inhibit osteoclast-mediated bone resorption by inducing osteoclast apoptosis. Nitrogen-containing bisphosphonates specifically inhibit farnesyl pyrophosphate synthase in the mevalonate pathway, disrupting protein prenylation essential for osteoclast function[6][7]. Eldecalcitol is an active vitamin D analog that binds to the vitamin D receptor (VDR), modulating calcium absorption in the intestine and reducing bone resorption by acting on osteoblasts and osteoclast precursors[9]. Clinical studies show that combining eldecalcitol with bisphosphonates results in greater increases in bone mineral density (BMD) at lumbar spine, femoral neck, and hip compared to either agent alone or other vitamin D analogs plus bisphosphonate[2][3][4][5][8]. This combination is particularly effective for patients with osteoporosis who have suboptimal response to monotherapy.

02

Targets

FDPS (Farnesyl pyrophosphate synthase)VDR (Vitamin D receptor)

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