tiludronic acid

Ligand id: 7604

Name: tiludronic acid

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 4
Rotatable bonds 4
Topological polar surface area 159.98
Molecular weight 317.93
XLogP -0.7
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Tiludronic acid is a bisphosphonate used to treat Paget's disease of bone, a disease caused by abnormal bone turnover, including excessive resorption and subsequent disorganised bone remodelling. There is no information regarding approval of this drug on either the US FDA or EMA websites. Individual national approval agencies may have granted marketing authorisation for this drug. In some countries only veterinary use is authorised.
Mechanism Of Action and Pharmacodynamic Effects
Bisphosphonates bind to hydroxyapatite in calcified bone matrix and inhibit the activity of enzymes that utilize pyrophosphate. Non-nitrogenous bisphosphonates such as tiludronic acid are metabolised in osteoclasts to compounds that form non-functional ATP molecules. This non-functional ATP then competes with active ATP in energy metabolism within the cell. The effect is reduced energy metabolism which drives the osteoclasts into apoptotic cell death. The net drug-induced effect is inhibition of osteoclast-driven bone resorption [1].