4929. Incadronic Acid

Nomenclature

CAS number: 124351-85-5
[(Cycloheptylamino)methylene]bisphosphonic acid.
C8H19NO6P2; mol wt 287.19.
C 33.46%, H 6.67%, N 4.88%, O 33.43%, P 21.57%.

Description and references

Bisphosphonate antiresorptive agent. Prepn: Y. Isomura et al., EP 325482; eidem, US 4970335 (1989, 1990 both to Yamanouchi); M. Takeuchi et al., Chem. Pharm. Bull. 41, 688 (1993). HPLC determn in plasma, urine and bone: T. Usui et al., J. Chromatogr. 584, 213 (1992). Effect on bone mineral density in dogs: H. Motoie et al., J. Bone Miner. Res. 10, 910 (1995). Toxicology: A. Okazaki et al., J. Toxicol. Sci. 20, Suppl. 1, 15 (1995). Clinical pharmacokinetics: T. Usui et al., Int. J. Clin. Pharmacol. Ther. 35, 239 (1997). Clinical evaluation in hypercalcemia of malignancy: S. Fukumoto et al., J. Clin. Endocrinol. Metab. 79, 165 (1994).

Chemical structure

Properties

Crystals from methanol-water, mp 232-233°.

Derivative

Disodium salt.

Nomenclature

CAS number: 138330-18-4
Cimadronate sodium; incadronate sodium; YM-175; Bisphonal (Yamanouchi).
C8H17NNa2O6P2; mol wt 331.15.
C 29.02%, H 5.17%, N 4.23%, Na 13.88%, O 28.99%, P 18.71%.

Properties

Occurs as the monohydrate. White, odorless crystalline powder. Easily sol in water. LD50 in male, female rats (mg/kg): 23, 21 i.v. (Okazaki).

Therapeutic Category

Bone resorption inhibitor.

Keywords

Antiosteoporotic; Bone Resorption Inhibitor