A METHOD OF EXTENDING THE DOSE RANGE OF VITAMIN D COMPOUNDS

• Main Author: SHEVDE, NIRUPAMA, K
• Format: Patent
• Language: English; Spanish
• Published: 27.05.2005
• Edition: 7
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

Inhibitors of bone calcium resorption are administered to allow high doses of vitamine D compounds or mimetics to be given the intent of treating non-calcium related diseases such as cancer, psoriasis, and autoimmune disease without the dangers of calcification of kidney, heart, and aorta. Inhibitors of bone calcium resorption include the bis-phosphonates, OPG or the soluble RANKL receptor known as sRANK, and function to block the availabilite of calcium from bone thereby preventing hypercalcemia and the resulting calcification of soft tissues. Thus, high doses of 1alpha,25-dihydroxyvitamin D3 (1,25-(OH)2D3), its analogs, prodrugs, or mimetics can be utilized with minimal risk to a patient. Specifically, alendronate is shown to block the bone calcium mobilization activity of both 1,25-(OH)2D3 and its very potent analog, 2-methylene-19-nor(20S)-1alpha,25 dihydroxyvitamin D3. Se administran inhibidores de resorcion de calcio de huesos, para permitir que altas dosis de compuestos de vitamina D o mimeticos sean suministradas con la intencion de tratar enfermedades no relacionadas con calcio tales con cancer, psoriasis, y enfermedad autoinmune sin el peligro de calcificacion de rinones, corazon y aorta. Inhibidores de resorcion de calcio en huesos incluyen los bis-fosfonatos, OPG o el receptor RANKL soluble conocido como sRANK, y funcionan para bloquear la disponibilidad de calcio de hueso, de esta manera evitando hipercalcemia y la calsificacion resultante de tejidos blandos. De esta manera, altas dosis de 1 alfa, 25-dihidroxivitamina D3 (1,25-(OH)2D3), sus analogos, prodrogas, o mimeticos pueden ser utilizadas con riesgo minimo para un paciente. Especificamente, se ilustra que alendronato bloquea la actividada de movilizacion de calcio en huesos de ambos 1,25-(OH)2D3 y su analogo muy potente, 2-metilen-19-nor(20S)-1 alfa, 25 dihidroxivitamina D3.