Sevelamer
(Synonyms: 司维拉姆) 目录号 : GC37630
Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
Cas No.:52757-95-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
Sevelamer is as effective as CaCO3 in reducing serum phosphorus, calcium-phosphorus product, and attenuating secondary hyperparathyroidism in nephrectomized rats (U) fed high phosphorus (HP) diet. Sevelamer results in markedly lower calcium deposition in the myocardium and aorta compared to control rats. [1] Sevelamer suppresses calcification of the aorta media, and also the osteoid volume, fibrosis volume, and porosity ratio of femurs in chronic renal failure rats. [2] Sevelamer results in a significantly lower degree of atherosclerosis and vascular calcification in uremic mice when compared with uremic control mice. Sevelamer exerts an effect on both intima and media calcification in uremic mice. [3] Sevelamer treatment controlled serum P independent of increases in serum Ca, thus reducing serum calcium-phosphate product and further deterioration of renal function, as indicated by the highest creatinine clearances in uremic rats. Sevelamer is as effective as CaCO3 in the control of high-P-induced SH, as shown by similar serum PTH levels, parathyroid (PT) gland weight, and markers of PT hyperplasia. Sevelamer causes a dramatic reduction of renal Ca deposition compared with both uremic + high-P diet (U-HP) and the U-HP+CaCO3 diet. [4] Sevelamer hydrochloride results in a fall in urine pH, as well as an increase in urinary ammonium and calcium excretion consistent with an increase in net acid excretion in animal model. [5]
[1] Cozzolino M, et al. Kidney Int, 2003, 64(5), 1653-1661. [2] Katsumata K, et al. Kidney Int, 2003, 64(2), 441-450. [3] Phan O, et al. Circulation, 2005, 112(18), 2875-2882.
| Cas No. | 52757-95-6 | SDF | |
| 别名 | 司维拉姆 | ||
| Canonical SMILES | NCC(CC(CC)CNCC(O)CNCC(C)CC(CC)CN)CC.[m].[c].[b].[a] | ||
| 分子式 | C20H46N4O | 分子量 | 358.61 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7885 mL | 13.9427 mL | 27.8854 mL |
| 5 mM | 0.5577 mL | 2.7885 mL | 5.5771 mL |
| 10 mM | 0.2789 mL | 1.3943 mL | 2.7885 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Sevelamer carbonate
Ann Pharmacother 2010 Jan;44(1):127-34.PMID:19955298DOI:10.1345/aph.1M291.
Objective: To review the pharmacology, pharmacokinetics, clinical efficacy, safety data, and place in therapy of Sevelamer carbonate for the treatment of hyperphosphatemia in patients with chronic kidney disease (CKD). Data sources: A literature search of MEDLINE and MEDLINE In-Process & Other Non-Indexed Citations Databases (1966-August 2009) was conducted using the key words chronic kidney disease, hyperphosphatemia, and Sevelamer carbonate. All published articles regarding Sevelamer carbonate were included. References of selected articles, data from multiple presentations, and abstract publications were reviewed. Study selection and data extraction: Available English-language data from reviews, abstracts, presentations, and clinical trials of Sevelamer carbonate in humans were reviewed; relevant clinical data were selected and included. Data synthesis: Sevelamer carbonate is approved to control serum phosphorus levels and treat hyperphosphatemia in patients with CKD who are on dialysis. In clinical trials, Sevelamer carbonate has been shown to lower serum phosphorus levels and calcium-phosphorus product to a similar extent as Sevelamer hydrochloride. Significantly fewer patients receiving treatment with Sevelamer carbonate were likely to report any gastrointestinal adverse event compared with those on Sevelamer hydrochloride treatment. Further, Sevelamer carbonate is associated with significant effects on decreasing low-density lipoprotein cholesterol levels and may cause less metabolic acidosis than Sevelamer hydrochloride. Additionally, Sevelamer hydrochloride was removed from the market in October 2009; Sevelamer carbonate is now the only available formulation. Conclusions: Sevelamer carbonate is a treatment option for hyperphosphatemia in patients with CKD who are on dialysis. Clinical data indicate that Sevelamer carbonate effectively lowers serum phosphorus levels while having minimal effect on serum calcium or serum chloride levels. The role of Sevelamer carbonate in the treatment of hyperphosphatemia relative to other phosphate-binding drugs, including calcium salts and lanthanum, has not yet been established.
Sevelamer
Nephron Clin Pract 2003;94(3):c53-8.PMID:12902631DOI:10.1159/000072021.
Hyperphosphataemia in patients with chronic renal failure has traditionally been treated with calcium- and aluminium-containing phosphate binders. This article briefly discusses the rationale and complications of these treatments and reviews Sevelamer that is a novel non-calcium-, non-aluminium-containing phosphate binder and the evidence to support its use in clinical practice.
Sevelamer Versus Calcium-Based Binders for Treatment of Hyperphosphatemia in CKD: A Meta-Analysis of Randomized Controlled Trials
Clin J Am Soc Nephrol 2016 Feb 5;11(2):232-44.PMID:26668024DOI:10.2215/CJN.06800615.
Background and objectives: People with CKD stages 3-5 and on dialysis (5D) have dramatically increased mortality, which has been associated with hyperphosphatemia in many studies. Oral phosphate binders are commonly prescribed to lower serum phosphate. We conducted an updated meta-analysis of the noncalcium-based binder (non-CBB) Sevelamer versus CBBs in CKD stages 3-5D. Design, setting, participants, & measurements: Randomized, controlled trials comparing Sevelamer with CBBs were identified through MEDLINE and the Cochrane Central Register of Controlled Trials. Patient-level outcomes included all-cause mortality, cardiovascular events and mortality, hospitalization, and adverse effects. Intermediate outcomes included vascular calcification and bone changes. Biochemical outcomes included serum phosphate, calcium, parathyroid hormone, lipids, and hypercalcemia. We conducted and reported this review according to Cochrane guidelines. Results: We included 25 studies to March 31, 2015 with 4770 participants (88% on hemodialysis). Patients receiving Sevelamer had lower all-cause mortality (risk ratio [RR], 0.54; 95% confidence interval [95% CI], 0.32 to 0.93), no statistically significant difference in cardiovascular mortality (n=2712; RR, 0.33; 95% CI, 0.07 to 1.64), and an increase in combined gastrointestinal events of borderline statistical significance (n=384; RR, 1.42; 95% CI, 0.97 to 2.08). For biochemical outcomes, patients receiving Sevelamer had lower total serum cholesterol (mean difference [MD], -20.2 mg/dl; 95% CI, -25.9 to -14.5 mg/dl), LDL-cholesterol (MD, -21.6 mg/dl; 95% CI, -27.9 to -15.4 mg/dl), and calcium (MD, -0.4 mg/dl; 95% CI, -0.6 to -0.2 mg/dl) and a reduced risk of hypercalcemia (RR, 0.30; 95% CI, 0.19 to 0.48). End of treatment intact parathyroid hormone was significantly higher for Sevelamer (MD, 32.9 pg/ml; 95% CI, 0.1 to 65.7 pg/ml). Serum phosphate values showed no significant differences. Conclusions: Patients with CKD stages 3-5D using Sevelamer have lower all-cause mortality compared with those using CBBs. Because of a lack of placebo-controlled studies, questions remain regarding phosphate binder benefits for patients with CKD stages 3-5 and not on dialysis.
Sevelamer carbonate: a review in hyperphosphataemia in adults with chronic kidney disease
Drugs 2014 May;74(7):771-92.PMID:24811546DOI:10.1007/s40265-014-0215-7.
Sevelamer carbonate (Renvela(®)), a buffered form of Sevelamer hydrochloride (Renagel(®)), is an orally administered non-absorbed phosphate-binding anion exchange resin used in the treatment of hyperphosphataemia in chronic kidney disease (CKD). In the EU, Sevelamer carbonate is approved in adult CKD patients who require dialysis and in those who do not require dialysis with serum phosphate levels ≥ 1.78 mmol/L, whereas in the USA Sevelamer carbonate is approved in adult CKD patients who require dialysis. Sevelamer carbonate and Sevelamer hydrochloride achieved similar reductions in serum phosphate levels in randomized comparative trials in patients with CKD receiving haemodialysis; Sevelamer carbonate also reduced serum phosphate levels in noncomparative studies in CKD patients not requiring dialysis. The most common adverse events with Sevelamer carbonate are gastrointestinal in nature. Sevelamer has pleiotropic effects, such as improving the serum lipid profile and attenuating endothelial and cardiovascular risk factors in CKD. All formulations of Sevelamer have markedly higher acquisition costs than calcium-based phosphate binders. Cost-effectiveness analyses focusing specifically on Sevelamer carbonate have not been conducted, and those based on clinical trial data with Sevelamer hydrochloride have provided both favourable and unfavourable results compared with calcium-based phosphate binders, reflecting heterogeneity between modelled analyses in terms of data sources, assumptions, comparators, geographical regions, type of costs included and other factors. Although well-designed studies evaluating the impact of phosphate binders on hard clinical endpoints appear to be warranted, Sevelamer carbonate may be particularly useful for the treatment of patients at risk of metabolic acidosis (offering advantages over Sevelamer hydrochloride in this regard) and for individuals requiring treatment with a phosphate binding agent that does not contain aluminium or calcium.
Pi-induced in-situ aggregation of Sevelamer nanoparticles for vascular embolization
Nanotechnology 2022 Jun 9;33(35).PMID:35616242DOI:10.1088/1361-6528/ac738b.
Decades have witnessed rapid progress of polymeric materials for vascular embolic or chemoembolic applications. Commercially available polymeric embolics range from gelatin foam to synthetic polymers such as poly(vinyl alcohol). Current systems under investigation include tunable, bioresorbable microspheres composed of chitosan or poly(ethylene glycol) derivatives,in situgelling liquid embolics with improved safety profiles, and radiopaque embolics that are trackablein vivo. In this paper, we proposed a concept of 'responsive embolization'. Sevelamer, clinically proved as an inorganic phosphate binder, was ground into nanoparticles. Sevelamer nanoparticle is highly mobile and capable of swelling and aggregating in the presence of endogenous inorganic phosphate, thereby effectively occluding blood flow in the vessel as it was administered as an embolic agent for interventional therapy. Moreover, citrated Sevelamer nanoparticles delayed the aggregation, preferable to penetrate deeply into the capillary system. On the rabbit VX2 liver cancer model, both Sevelamer particles aggregates occlude the tumor feeding artery, but backflow was found for the pristine one, thereby citrate passivation of Sevelamer nanoparticles endows it have potential from 'bench to bedside' as a new type of vascular embolic.