Drug intelligence / Profile preview

raloxifene + alendronate

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Raloxifene + alendronate is a combination therapy used in the management of postmenopausal osteoporosis. Raloxifene is a selective estrogen receptor modulator (SERM) that acts as an estrogen agonist on bone, increasing bone mineral density (BMD) and reducing bone turnover by modulating gene expression through the estrogen receptor. Alendronate is a bisphosphonate that inhibits osteoclast-mediated bone resorption, also leading to increased BMD and reduced fracture risk. The combination has been shown to produce additive effects on BMD at the lumbar spine and femoral neck compared to either agent alone, though evidence for reduction in fracture risk beyond monotherapy remains insufficient[1][2][3][4]. Both drugs act via distinct mechanisms: raloxifene through selective modulation of the estrogen receptor, and alendronate through inhibition of osteoclast activity.

02

Targets

FDPS (Farnesyl pyrophosphate synthase)ESR2 (ERβ)ESR1 (ERα)

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