Tiludronic acid is a bisphosphonate used for the treatment of Paget's disease of bone. Tiludronate, or (4-chlorophenyl)thio-methylene-1,1-bisphosphonate, is a first generation bisphosphonate similar to etidronic acid and clodronic acid.
- Mechanism
- Curator reviewed · 10 references
Bisphosphonates are taken into the bone where they bind to hydroxyapatite. Bone resorption by osteoclasts causes local acidification, releasing the bisphosphonate, which is taken into the osteoclast by fluid-phase endocytosis. Endocytic vesicles become acidified, releasing bisphosphonates into the cytosol of osteoclasts where they act.
Osteoclasts mediate resorption of bone. When osteoclasts bind to bone they form podosomes, ring structures of F-actin. Tiludronate inhibits protein-tyrosine-phosphatase, which increases tyrosine phosphorylation, and disrupts podosome formation. Tiludronic acid also inhibits V-ATPases in the osteoclast, though the exact subunits are unknown, preventing F-actin from forming podosomes. Disruption of the podosomes causes osteoclasts to detach from bones, preventing bone resorption.
- Primary indication
- Tiludronic acid is indicated to treat Paget's disease of bone in patients with serum alkaline phosphatase levels ≥2 times the upper limit of normal, with symptoms, or with risk of future complications.Curator reviewed · 3 structured indications
- Formula / weight
- C7H9ClO6P2S · 318.608 g/mol (avg)
- First approval
- United States, 1997
- Also known as
- Tiludronate
- Code names
- SR-41319
Resolves to
DKJJVAGXPKPDRL-UHFFFAOYSA-NSMILESOP(O)(=O)C(SC1=CC=C(Cl)C=C1)P(O)(O)=OWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Tiludronic acid, and which of those have an active Phase 3 trial?
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