Department of Medical & Surgical Sciences, University of Padua, School of Medicine, via Giustiniani 2, 35128 Padova, Italy.
Med Chem. 2012 Jul;8(4):556-63. doi: 10.2174/157340612801216355.
Hypercalcemia is a relatively frequent alteration, mostly associated to primary hyperparathyroidism (PHPT) and malignancy-associated hypercalcemia (MAH). Treatment first includes rehydration and loop diuretics, as general measures. Bisphosphonates are considered the drugs of choice due to their long-term management. Calcitonin is preferable in the short-term control of severe hypercalcemia. The antireabsorptive action of bisphosphonates has been considered the most effective in the disorders characterized by an excessive bone resorption. Zoledronate is superior to both clodronate or pamidronate in the treatment of MAH. Calcimimetic agents has been recently introduced to control hypercalcemia in selected cases of PHPT. They are used when surgery is not possible or patients do not meet surgical criteria. Malignancy- associate hypercalcemia is broadly divided into two categories: humoral MAH and osteolytic MAH. The first concerns the paraneoplastic release of humoral factors, mainly parathyroid hormone-related peptide (PTHrP). Recently a humanized monoclonal antibody against human PTHrP has been generated and is still under evaluation. The receptor activator of nuclear factor-κ ligand (RANKL) has a critical role in the etiology of malignancy skeletal complications. The fully humanized anti-RANKL antibody (denosumab) would seem to be even more effective than bisphosphonates to suppress bone resorption, as shown in preliminary results .
高钙血症是一种相对常见的改变,主要与原发性甲状旁腺功能亢进症(PHPT)和恶性肿瘤相关的高钙血症(MAH)有关。治疗首先包括补液和袢利尿剂等一般措施。双膦酸盐由于其长期管理而被认为是首选药物。降钙素在短期控制严重高钙血症方面更具优势。双膦酸盐的抗吸收作用被认为在以过度骨吸收为特征的疾病中最有效。唑来膦酸在 MAH 的治疗中优于氯屈膦酸或帕米膦酸。钙敏感受体激动剂最近被引入用于控制选定 PHPT 病例的高钙血症。当手术不可行或患者不符合手术标准时使用。恶性肿瘤相关的高钙血症广泛分为两类:体液性 MAH 和溶骨性 MAH。第一种涉及副肿瘤性释放体液因子,主要是甲状旁腺激素相关肽(PTHrP)。最近,一种针对人 PTHrP 的人源化单克隆抗体已被开发出来,并仍在评估中。核因子-κ 配体受体激活剂(RANKL)在恶性肿瘤骨骼并发症的发病机制中起着关键作用。全人源抗 RANKL 抗体(地舒单抗)似乎比双膦酸盐更能有效抑制骨吸收,初步结果显示。