- Molecular NameTiludronate
- SynonymAcide tiludronique [INN-French]; Acido tiludronico [INN-Spanish]; Acidum tiludronicum [INN-Latin]; Tiludronate disodium; Tiludronic acid; Tiludronic Acid Disodium Salt
- Weight318.61
- Drugbank_IDDB01133
- ACS_NO89987-06-4
- Show 2D model
- LogP (experiment)0.549
- LogP (predicted, AB/LogP v2.0)-1.57
- pka<1.5, 2.27, 6.31, 10.6
- LogD (pH=7, predicted)-7.37
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)0.5
- LogSw (predicted, AB/LogsW2.0)2.34
- Sw (mg/ml) (predicted, ACD/Labs)3.5
- No.of HBond Donors4
- No.of HBond Acceptors6
- No.of Rotatable Bonds4
- TPSA159.98
- StatusFDA approved
- AdministrationN/A
- PharmacologyA bisphosphonate.
- Absorption_value6.0
- Absorption (description)The mean oral bioavailability in healthy male subjects is 6% after an oral dose equivalent to 400 mg tiludronic acid administered after an overnight fast and 4 hours before a standard breakfast. In single-dose studies, bioavailability was reduced by 90% when an oral dose equivalent to 400 mg tiludronic acid was administered with, or 2 hours after, a standard breakfast compared to the same dose administered after an overnight fast and 4 hours before a standard breakfast.
- Caco_2N/A
- Bioavailability6.0
- Protein binding90.0
- Volume of distribution (VD)30 to 60 L
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIn vitro, tiludronic acid is not metabolized in human liver microsomes and hepatocytes. There is no evidence that tiludronate is metabolized in humans.
- Half life40~150 h
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityBased on the known action of tiludronate, hypocalcemia is a potential consequence of overdose. In one patient with hypercalcemia of malignancy, intravenous administration of high doses (800 mg/day total dose, 6 mg/kg/day for 2 days) was associated with acute renal failure and death.
- LD50 (rat)N/A
- LD50 (mouse)N/A