DONNA J. GLOVER, M.D.; LESLIE SHAW, Ph.D.; JOHN H. GLICK, M.D.; EDUARDO SLATOPOLSKY, M.D.; CLARE WEILER, R.N.; MAURICE ATTIE, M.D.; STANLEY GOLDFARB, M.D.
The chemoprotective and hypocalcemic agent WR-2721, S-2-(3-aminopropylamino) ethyl-phosphorothioic acid, inhibits parathyroid hormone secretion in vivo and in vitro. We report the first clinical use of WR-2721 in refractory hypercalcemia secondary to parathyroid cancer. After several days of saline diuresis the patient received WR-2721, 740 mg/m2 over 15 minutes, resulting in a fall in serum calcium from 11.76 to 9.06 mg/dL within 24 hours. Serum parathyroid hormone levels decreased from 675 to 140 µLeq/mL 2 hours after the infusion was complete. When hypercalcemia recurred the patient was retreated with differing doses and infusion rates to determine the optimal method of drug administration to provide a satisfactory hypocalcemic response without adverse effects. In this patient, WR-2721 in intravenous boluses of 150 mg/m2 was effective without adverse effects. Using high-pressure liquid chromatography with electrochemical detection, plasma pharmacokinetic studies showed that WR-2721 's distribution half-life is 0.55 minutes.
GLOVER DJ, SHAW L, GLICK JH, SLATOPOLSKY E, WEILER C, ATTIE M, et al. Treatment of Hypercalcemia in Parathyroid Cancer with WR-2721,5-2(3aminopropylamino) Ethyl-Phosphorothioic Acid. Ann Intern Med. ;103:55–57. doi: 10.7326/0003-4819-103-1-55
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Published: Ann Intern Med. 1985;103(1):55-57.
Endocrine and Metabolism, Fluid and Electrolyte Disorders, Nephrology.
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