Minodronic acid
(Synonyms: 1-羟基-2-(咪唑并[1,2-A]吡啶-3-基)乙烷-1,1-双膦酸,YM-529) 目录号 : GC36613
Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. Minodronic acid is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain.
Cas No.:180064-38-4
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
Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. Minodronic acid is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain.
| Cas No. | 180064-38-4 | SDF | |
| 别名 | 1-羟基-2-(咪唑并[1,2-A]吡啶-3-基)乙烷-1,1-双膦酸,YM-529 | ||
| Canonical SMILES | OC(P(O)(O)=O)(P(O)(O)=O)CC1=CN=C2C=CC=CN21 | ||
| 分子式 | C9H12N2O7P2 | 分子量 | 322.15 |
| 溶解度 | Water: 5 mg/mL (15.52 mM and warming); DMSO: < 1 mg/mL (insoluble or slightly soluble) | 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 | 3.1041 mL | 15.5207 mL | 31.0414 mL |
| 5 mM | 0.6208 mL | 3.1041 mL | 6.2083 mL |
| 10 mM | 0.3104 mL | 1.5521 mL | 3.1041 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。
A review of Minodronic acid hydrate for the treatment of osteoporosis
Clin Interv Aging 2013;8:185-9.PMID:23440003DOI:10.2147/CIA.S23927.
Minodronic acid hydrate was the first bisphosphonate developed and approved for osteoporosis treatment in Japan. With regard to inhibition of bone resorption, Minodronic acid hydrate is 1000 times more effective than etidronic acid and 10-100 times more effective than alendronic acid. Clinical trials conducted to date have focused on postmenopausal female patients suffering from primary osteoporosis. In these trials, 1 mg of oral Minodronic acid hydrate was administrated once daily, and a significant increase was observed in lumbar-spine and hip-joint bone density 1-2 years after administration. All markers of bone metabolism urinary collagen type 1 cross-linked N-telopeptide, urinary free deoxypyridinoline, serum bone alkaline phosphatase, and serum osteocalcin were decreased. The incidence rate of new vertebral and nonvertebral fractures was also decreased. Therefore, effectiveness in fracture prevention was confirmed. A form of Minodronic acid (50 mg) requiring once-monthly administration has been developed and is currently being used clinically. A comparative study between this new formulation and once-daily Minodronic acid (1 mg) showed no significant differences between the two formulations in terms of improvement rates in lumbar-spine and hip-joint bone density, changes in bone metabolism markers, or incidence of side effects. This indicates the noninferiority of the monthly formulation. Side effects such as osteonecrosis of the jaw or atypical femoral fractures were not reported with other bisphosphonates, although it is believed that these side effects may emerge as future studies continue to be conducted. On the basis of studies conducted to date, Minodronic acid hydrate is considered effective for improving bone density and preventing fractures. We anticipate further investigations in the future.
Efficacy of Minodronic acid for the prevention of osteoporosis in premenopausal women with gynaecologic disease who undergo bilateral oophorectomy: a single-centre, non-randomised controlled, experimental study
J Obstet Gynaecol 2022 Nov;42(8):3591-3599.PMID:36200398DOI:10.1080/01443615.2022.2130202.
We evaluated the efficacy of Minodronic acid for osteoporosis prevention after bilateral oophorectomy for gynaecologic disease in premenopausal women. Bone mineral density (BMD) and young adult mean (YAM) data from the lumbar vertebrae and femur and bone alkaline phosphatase (BAP)/tartrate-resistant acid phosphatase 5 b (TRACP 5 b) data were obtained for 101 patients. The primary endpoint was the efficacy of Minodronic acid for osteoporosis prevention. Fifty-five and 31 patients were assigned to medication and no medication groups, respectively. The decrease in BMD and YAM and the increase in BAP/TRACP-5b were significantly more suppressed in the medication group. There were no significant between-group differences in age at oophorectomy, cancer type, body mass index (BMI), and adjuvant therapy. There were no adverse events due to Minodronic acid. Minodronic acid may prevent osteoporosis after oophorectomy in premenopausal women with gynaecologic disease, independent of age at oophorectomy, cancer type, BMI, or adjuvant therapy. Impact statementWhat is already known on this subject? Although the current strategy for osteoporosis prevention after premenopausal bilateral oophorectomy (b-OVX) is hormone therapy (HT), there is no consensus on the treatment duration or adverse events.What do the results of this study add? Therefore, we planned a prospective study to evaluate the efficacy of prophylactic treatment for osteoporosis after b-OVX in premenopausal women with gynaecologic disease using Minodronic acid, an oral bisphosphonate, which have a strong evidence of the treatment for osteoporosis. The result showed Minodronic acid significantly suppressed the decrease in bone mineral density (BMD) and young adult mean (YAM) and the increase in bone alkaline phosphatase (BAP)/tartrate-resistant acid phosphatase 5b (TRACP 5b). Minodronic acid may prevent osteoporosis after oophorectomy in premenopausal women with gynaecologic disease, independent of age at oophorectomy, cancer type, BMI, or adjuvant therapy.What are the implications of these findings for clinical practice and/or further research? Minodronic acid treatment for osteoporosis prevention after premenopausal b-OVX may be effective as a therapeutic agent after the cessation of HT, or alternative for patients who are contraindicated for HT in breast cancer and thrombosis and should be administered with caution with a history of uterine or ovarian cancer.
Minodronic acid suppresses gonadotropin-releasing hormone agonist-induced bone remodeling biomarkers: a retrospective pilot study
Gynecol Endocrinol 2016;32(3):250-2.PMID:26503621DOI:10.3109/09513590.2015.1112783.
Background: Estrogen deprivation therapy for myoma/adenomyosis decreases bone mineral density and can only be applied in the short term, as temporizing measures in the premenopausal woman. Objective: To examine the effects of bisphosphonate Minodronic acid on markers of bone turnover over a 6-month period in women receiving gonadotropin-releasing hormone agonist (GnRHa). Methods: We retrospectively analyzed the medical records of 19 premenopausal patients with myoma/adenomyosis, who received GnRHa (leuprolide acetate, 1.88 mg/month or buserelin acetate, 900 µg/day) for 6 months from January 2014 to December 2014. Eight patients concomitantly received Minodronic acid 50 mg every month during GnRHa therapy, and 11 treated with GnRHa alone. To compare these data in a case-controlled study, we analyzed an age-matched group of seven (premature or natural) menopausal women treated with Minodronic acid. The primary outcome was percent changes in bone turnover markers in urine at 6 months. Results: In menopausal women group, Minodronic acid (50 mg once-monthly) for 6 months decreased urinary deoxypyridinoline (DPD) and cross-linked N-telopeptides of type 1 collagen (NTX). Women receiving a GnRHa had a significant increase in urinary DPD and TNX at 6 months while Minodronic acid during GnRHa therapy improved urinary levels of DPD and NTX to near baseline. Conclusion: Minodronic acid treatment appears to be promising in women with secondary bone loss receiving GnRHa treatment.
[Minodronic acid hydrate as a new therapeutic agent for osteoporosis]
Clin Calcium 2005 Jan;15(1):9-14.PMID:15632466doi
Minodronic acid hydrate is one of the new-generation bisphosphonates containing nitrogen. The drug has an inhibitory effect on bone resorption by suppressing the osteoclastic function. Minodronic acid hydrate is being developed as a therapeutic drug of osteoporosis. In non-clinical study, the inhibitory effect of Minodronic acid hydrate on the decrease in the bone mineral density and on the reduction in the bone intensity in ovariectomized rat osteoporosis models. The results of the clinical studies conducted so far showed that Minodronic acid hydrate administered once daily for 36 weeks increases the bone mineral density of lumbar spine (L2-4BMD) significantly compared to the placebo group. It was speculated that Minodronic acid hydrate has an increasing effect on the bone mineral density that is at least equivalent to that of alendronate and risedronate. It was also expected that the incidence of digestive diseases with Minodronic acid hydrate is lower than that with the existing bisphosphonates. At the moment, the Phase III study is being conducted. We expect that Minodronic acid hydrate is used for a number of patients with osteoporosis as a potent and safe domestic bisphosphonate in the near future.
Minodronic acid induces morphological changes in osteoclasts at bone resorption sites and reaches a level required for antagonism of purinergic P2X2/3 receptors
J Bone Miner Metab 2018 Jan;36(1):54-63.PMID:28243795DOI:10.1007/s00774-017-0814-y.
Minodronic acid is an aminobisphosphonate that is an antagonist of purinergic P2X2/3 receptors involved in pain. The aim of this study was to investigate the action and distribution of Minodronic acid and the potential for P2X2/3 receptor antagonism based on the estimated concentration of Minodronic acid. Microlocalization of radiolabeled Minodronic acid was examined in the femur of neonatal rats. The bone-binding characteristics of Minodronic acid and morphological changes in osteoclasts were analyzed in vitro. The Minodronic acid concentration around bone resorption lacunae was predicted based on bone binding and the shape of lacunae. In microautoradiography, radioactive silver grains were abundant in bone-attached osteoclasts and were detected in calcified and ossification zones and in the cytoplasm of osteoclasts but not in the hypertrophic cartilage zone. In an osteoclast culture with 1 µM Minodronic acid, 65% of Minodronic acid was bound to bone, and C-terminal cross-linking telopeptide release was inhibited by 96%. Cultured osteoclasts without Minodronic acid treatment formed ruffled borders and bone resorption lacunae and had rich cytoplasm, whereas those treated with 1 µM Minodronic acid were not multinucleated, stained densely with toluidine blue, and were detached from the bone surface. In the 1 µM culture, the estimated Minodronic acid concentration in resorption lacunae was 880 µM, which is higher than the IC50 for Minodronic acid antagonism of P2X2/3 receptors. Thus, inhibition of P2X2/3 receptors around osteoclasts may contribute to the analgesic effect of Minodronic acid.