Ibandronic acid
(Synonyms: 伊班膦酸) 目录号 : GC36287
Ibandronic acid是高效含氮双磷酸盐，可作用于骨质疏松。
Cas No.:114084-78-5
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
Ibandronic acid is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.Target: OthersIbandronate (1.25-2 μM) significantly reduces endothelial cell growth, while ibandronate (2 μM) also significantly reduces capillary-like tube formation and increases apoptosis of endothelial cells. Ibandronate (< 100 μM) dose-dependently increases VEGF expression in endothelial cells [1]. Ibandronate (< 100 μM) inhibits growth of both prostate cancer cell lines (LNCaP and PC-3) in a dose dependent manner [2].Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly reduces the risk of new morphometric vertebral fractures by 62% and 50% (p = 0.0006), respectively, in osteoporotic women after 3 years' treatment. Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly and progressively increases BMD of lumbar spine by 6.5% and 5.7%, respectively, in osteoporotic women after 3 years' treatment [3]. Ibandronate (< 125 mg/kg s.c.) results in a dose dependent increase in bone mineral density (BMD), trabecular bone volume and trabecular number, load to failure (Fmax), and yield load in long bones and vertebrae in ovariectomized rats, and increased trabecular separation in ovariectomized rats is fully prevented by all doses [4].
[1]. Morgan, C., S. Jeremiah, and J. Wagstaff, Metronomic administration of ibandronate and its anti-angiogenic effects in vitro. Microvasc Res, 2009. 78(3): p. 453-8. [2]. Epplen, R., et al., Differential effects of ibandronate, docetaxel and farnesol treatment alone and in combination on the growth of prostate cancer cell lines. Acta Oncol, 2011. 50(1): p. 127-33. [3]. Chesnut, I.C., et al., Effects of oral ibandronate administered daily or intermittently on fracture risk in postmenopausal osteoporosis. J Bone Miner Res, 2004. 19(8): p. 1241-9. [4]. Bauss, F., et al., Effects of treatment with ibandronate on bone mass, architecture, biomechanical properties, and bone concentration of ibandronate in ovariectomized aged rats. J Rheumatol, 2002. 29(10): p. 2200-8.
| Cas No. | 114084-78-5 | SDF | |
| 别名 | 伊班膦酸 | ||
| Canonical SMILES | OC(P(O)(O)=O)(P(O)(O)=O)CCN(C)CCCCC | ||
| 分子式 | C9H23NO7P2 | 分子量 | 319.23 |
| 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 | 3.1325 mL | 15.6627 mL | 31.3254 mL |
| 5 mM | 0.6265 mL | 3.1325 mL | 6.2651 mL |
| 10 mM | 0.3133 mL | 1.5663 mL | 3.1325 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。
Ibandronic acid: a review of its use in the treatment of bone metastases of breast cancer
Drugs 2006;66(5):711-28.PMID:16620148DOI:10.2165/00003495-200666050-00011.
Ibandronic acid (Bondronat) is a potent, new-generation, nitrogen-containing bisphosphonate, available in both intravenous and oral formulations, which effectively inhibits osteoclast-mediated bone resorption. In clinical trials, the two formulations were equally effective in preventing skeletal-related events and improving quality of life in patients with bone metastases of breast cancer. Both intravenous and oral Ibandronic acid reduced metastatic bone pain scores below baseline levels for up to 2 years. Oral Ibandronic acid is administered as a single 50 mg tablet taken once daily. It suppressed bone resorption in breast cancer patients with bone metastases to an extent similar to that observed with intravenous zoledronic acid. Both intravenous and oral Ibandronic acid were well tolerated with no evidence of renal toxicity. Ibandronic acid is therefore a valuable addition to the bisphosphonates used in the treatment of bone metastases of breast cancer, offering high potency and the convenience of oral administration, combined with the absence of renal toxicity.
Osteoporosis treatment: why Ibandronic acid?
Expert Opin Pharmacother 2013 Jul;14(10):1371-81.PMID:23650954DOI:10.1517/14656566.2013.795949.
Introduction: In this article, we have summarized the specific evidence on Ibandronic acid (or ibandronate) efficacy, tolerability, and feasibility acquired from trials and clinical use. Areas covered: This critical review focuses on evidence from randomized controlled clinical trials, meta-analyses, surrogate markers, bridging trials, long-term extension studies, observational studies, clinical experiences in osteoporosis in addition to postmenopausal treatment adherence in clinical practice, and safety profile of Ibandronic acid. Expert opinion: Pivotal studies on Ibandronic acid efficacy in terms of antifracture effects on nonvertebral fractures had some intrinsic limitations. However, a large body of indirect evidence suggests that ibandronate has significantly sustained vertebral and nonvertebral antifracture efficacies in women with postmenopausal osteoporosis, in comparison to those observed with other nitrogen-containing bisphosphonates. Discrepancies in efficacy between the available bisphosphonate regimens appear to be a function of dose rather than to inherent differences in their respective therapeutic potential. Drugs or treatment regimens that minimize the risk of osteoporotic fractures and make the treatment of osteoporosis more convenient and suitable for patients are preferred: Ibandronic acid marketed at oral doses of 150 mg once monthly and 3 mg quarterly as intravenous injection has these characteristics. The safety profile of Ibandronic acid treatment appears to be good overall and in some cases better than that of other nitrogen-containing bisphosphonates.
Oral Ibandronic acid
IDrugs 2005 Feb;8(2):155-69.PMID:15696417doi
Roche Holdings AG is developing an oral formulation of the bisphosphonate derivative Ibandronic acid as a potential treatment for metastatic bone disease in breast cancer patients; it was filed for this indication in October 2002. Roche and its Japanese subsidiary Chugai Pharmaceutical Co Ltd, in collaboration with GlaxoSmithKline plc, have also developed the formulation for the treatment of osteoporosis.
Zoledronic acid is more efficient than Ibandronic acid in the treatment of symptomatic bone marrow lesions of the knee
Knee Surg Sports Traumatol Arthrosc 2020 Feb;28(2):408-417.PMID:31273410DOI:10.1007/s00167-019-05598-w.
Purpose: The purpose of this study was to determine the efficacy and tolerability of different antiresorptive therapeutic regimens for treating symptomatic bone marrow lesions (BML) of the knee. Methods: Patient records of 34 patients with radiologically diagnosed, painful BML of the knee treated with either a bisphosphonate (zoledronic, ibandronic, or alendronic acid) or with a human monoclonal antibody (denosumab) were retrospectively evaluated. Response to treatment was assessed, as change in patient-reported pain, by evaluation of BML expansion on MRI using the Whole-Organ Magnetic Resonance Imaging Score (WORMS), and by laboratory analysis of bone turnover markers: C-terminal cross-linking telopeptide (CTx) and procollagen type 1 amino-terminal propeptide (P1NP). Tolerability was evaluated by documentation of adverse reactions. Results: Zoledronic acid was more or at least equally effective as the other treatment regimens with response to treatment in 11 of 12 patients (92%). The highest rate of adverse events was noted in 4 of 12 patients (33%) treated with zoledronic acid. CTx and WORMS differentiated well between responders and non-responders, whereas P1NP failed to do so. Changes in pain correlated moderately with change in WORMS (r = - 0.32), weakly with change in CTx (r = - 0.07), and not at all with change in P1NP. Conclusion: Zoledronic acid appeared to be more effective than other antiresorptive medications-at the cost of more frequent adverse events. While radiological and laboratory evaluation methods may allow for objective treatment monitoring, they appear to capture different dimensions than patient-reported pain. Level of evidence: III.
Oral Ibandronic acid versus intravenous zoledronic acid in treatment of bone metastases from breast cancer: a randomised, open label, non-inferiority phase 3 trial
Lancet Oncol 2014 Jan;15(1):114-22.PMID:24332514DOI:10.1016/S1470-2045(13)70539-4.
Background: Bisphosphonates are routinely used in the treatment of metastatic bone disease from breast cancer to reduce pain and bone destruction. Zoledronic acid given by intravenous infusion has been widely used, but places a substantial logistical burden on both patient and hospital. As a result, the use of oral Ibandronic acid has increased, despite the absence of comparative data. In the ZICE trial, we compared oral Ibandronic acid with intravenous zoledronic acid for the treatment of metastatic breast cancer to bone. Methods: This phase 3, open-label, parallel group active-controlled, multicentre, randomised, non-inferiority phase 3 study was done in 99 UK hospitals. Eligibility criteria included at least one radiologically confirmed bone metastasis from a histologically confirmed breast cancer. Patients with ECOG performance status 0 to 2 and clinical decision to treat with bisphosphonates within 3 months of randomisation were randomly assigned to receive 96 weeks of treatment with either intravenous zoledronic acid at 4 mg every 3-4 weeks or oral Ibandronic acid 50 mg daily. Randomisation (1:1) was done via a central computerised system within stratified block sizes of four. Randomisation was stratified on whether patients had current or planned treatment with chemotherapy; current or planned treatment with hormone therapy; and whether they had a previous skeletal-related event within the last 3 months or had planned radiotherapy treatment to the bone or planned orthopaedic surgery due to bone metastases. The primary non-inferiority endpoint was the frequency and timing of skeletal-related events over 96 weeks, analysed using a per-protocol analysis. All active (non-withdrawn) patients have now reached the 96-week timepoint and the trial is now in long-term follow-up. The trial is registered with ClinicalTrials.gov, number NCT00326820. Findings: Between Jan 13, 2006, and Oct 4, 2010, 705 patients were randomly assigned to receive Ibandronic acid and 699 to receive zoledronic acid; three patients withdrew immediately after randomisation. The per-protocol analysis included 654 patients in the Ibandronic acid group and 672 in the zoledronic acid group. Annual rates of skeletal-related events were 0·499 (95% CI 0·454-0·549) with Ibandronic acid and 0·435 (0·393-0·480) with zoledronic acid; the rate ratio for skeletal-related events was 1·148 (95% CI 0·967-1·362). The upper CI was greater than the margin of non-inferiority of 1·08; therefore, we could not reject the null hypothesis that Ibandronic acid was inferior to zoledronic acid. More patients in the zoledronic acid group had renal toxic effects than in the Ibandronic acid group (226 [32%] of 697 vs 172 [24%] of 704) but rates of osteonecrosis of the jaw were low in both groups (nine [1%] of 697 vs five [<1%] of 704). The most common grade 3 or 4 adverse events were fatigue (97 [14%] of 697 patients allocated zoledronic acid vs 98 [14%] of 704 allocated Ibandronic acid), increased bone pain (91 [corrected] [13%] vs 85 [corrected] [12%]), joint pain (41 [corrected] [6%] vs 38 [5%]), infection (31 [5%] vs 23 [corrected] [3%]), and nausea or vomiting (38 [5%] vs 41 [6%]). Interpretation: Our results suggest that zoledronic acid is preferable to Ibandronic acid in preventing skeletal-related events caused by bone metastases. However, both drugs have acceptable side-effect profiles and the oral formulation is more convenient, and could still be considered if the patient has a strong preference or if difficulties occur with intravenous infusions. Funding: Roche Products Ltd (educational grant), supported by National Institute for Health Research Cancer Network, following endorsement by Cancer Research UK (CRUKE/04/022).