Drug intelligence / Profile preview

alendronate + placebo

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Alendronate is a nitrogen-containing bisphosphonate that serves as a potent inhibitor of osteoclast-mediated bone resorption. In the specific context of the Phase 3 clinical trial conducted by Columbia University (NCT00000412), alendronate (10 mg/day) was administered in combination with a placebo matching calcitriol to evaluate its efficacy in preventing the rapid bone loss typically observed in patients following cardiac transplantation. The drug works by binding to hydroxyapatite crystals on bone surfaces; during bone resorption, it is taken up by osteoclasts where it inhibits farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. This inhibition disrupts the prenylation of small GTP-binding proteins, leading to osteoclast apoptosis and a subsequent reduction in bone turnover. The study demonstrated that alendronate is effective in maintaining bone mineral density in the lumbar spine and hip in heart transplant recipients, who are at high risk for osteoporosis due to mandatory glucocorticoid therapy.

Brand names
Fosamax
Other names
alendronate sodium
02

Targets

FDPS (Farnesyl pyrophosphate synthase)

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