阿仑膦酸钠/胆骨化醇(Alendronate Sodium/Cholecalciferol) - 药物靶点：VDR_在研适应症：骨质疏松症，绝经期后骨质疏松_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Adrovance、Alendronate Sodium Trihydrate/Colecalciferol、Alendronate Sodium/Colecalciferol

+ [10]

靶点

VDR

作用方式

激动剂、抑制剂

作用机制

VDR激动剂(维生素D受体激动剂)、破骨细胞抑制剂

治疗领域

内分泌与代谢疾病皮肤和肌肉骨骼疾病

在研适应症

骨质疏松症绝经期后骨质疏松

非在研适应症

维生素D缺乏症

原研机构

Merck Sharp & Dohme Corp.

在研机构

Organon NV

Organon & Co.Merck Sharp & Dohme Farmaceutica Ltda.

+ [1]

非在研机构

Merck Sharp & Dohme Corp.

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (2005-04-07),

绝经期后骨质疏松骨质疏松症

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C31H63NNaO11P2

InChIKeyZBOIUMYEYAMMKJ-FYLNQELCSA-N

CAS号871265-92-8

关联

14

项与阿仑膦酸钠/胆骨化醇相关的临床试验

CTR20241313

/ Completed临床1期

阿仑膦酸钠维D3片（Ⅱ）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、四周期、完全重复交叉生物等效性试验

按有关药代动力学试验的规定，选择杭州默沙东制药有限公司为生产商的阿仑膦酸钠维D3片（Ⅱ）（商品名：福美加®；规格：每片含阿仑膦酸钠70mg（以阿仑膦酸计）与维生素D3 5600IU（相当于140μg））为参比制剂，对南京九霄药业有限公司持有的受试制剂阿仑膦酸钠维D3片（Ⅱ）（规格：每片含阿仑膦酸钠70mg（以阿仑膦酸计）与维生素D3 5600IU（相当于140μg））进行空腹口服生物等效性试验，比较两种制剂在中国健康志愿者体内的血药浓度经时过程，估算相应的药代动力学参数。同时观察健康受试者口服受试制剂和参比制剂后的安全性。

开始日期2024-05-28

申办/合作机构

南京九霄药业有限公司

EUCTR2019-003101-97-ES

/ Unknown status临床4期IIT

An unicentric, open, randomized and crossover clinical trial to evaluate vitamin D supplementation effect of colecalciferol versus calcidiol in mineral metabolism in hemodialisis patients.

开始日期2020-02-18

申办/合作机构-

NCT02132026

/ Completed临床2期IIT

SALTIRE II: Bisphosphonates and RANKL Inhibition in Aortic Stenosis

Aortic stenosis is a condition whereby one of the heart valves (aortic valve) becomes narrowed, due to calcium deposition, over time. This can lead to chest pain, heart failure and sudden death. It is the commonest valve disease requiring surgery in the developed world and as the population becomes increasingly older, it is predicted that the prevalence of aortic stenosis will double in the next 20 years. Currently the only treatment is replacement of the aortic valve. Whilst this is excellent treatment, not everyone is suitable for it.
The primary objective of our study is to determine whether 2 drugs used in the treatment of osteoporosis (a condition of bone thinning) can halt/retard the progression of aortic stenosis. This is on the basis that studies have suggested that altered regulation of calcium metabolism may be an important mechanism perpetuating the disease. Both drugs work by reducing calcium release into the bloodstream from bones and therefore calcification of the aortic valve.
150 patients will therefore be randomly allocated to either of the trial drugs which are denosumab,the bisphosphonate (alendronic acid), or a placebo.
Positron Emission Tomography (PET) scanning is a technique where biochemically active molecules are injected and are taken up at sites of ongoing calcification activity where they emit radiation and can be detected by the PET scanner. We have previously shown that this technique can demonstrate areas of newly developing calcification on an aortic valve.
We therefore propose that patients receiving bisphosphonates or denosumab will have reduced evidence of active calcification and slower progression of their disease at two years as assessed by Echocardiography (ultrasound) and a change in their calcium score (quantity of calcium on the aortic valve measured using Computed Tomography [CT] ).
The data from this study will then be used to design a larger trial.

开始日期2014-11-12

申办/合作机构

The University of Edinburgh

[+2]

100 项与阿仑膦酸钠/胆骨化醇相关的临床结果

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100 项与阿仑膦酸钠/胆骨化醇相关的转化医学

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100 项与阿仑膦酸钠/胆骨化醇相关的专利（医药）

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57

项与阿仑膦酸钠/胆骨化醇相关的文献（医药）

2025-02-01·World Allergy Organization Journal

Desensitization to colecalciferol in 18 patients with immediate hypersensitivity reactions

Article

作者: Tepetam, Fatma Merve ; Can, Ali ; Özden, Şeyma ; Şaylan, Bengü ; Atik, Özge

IntroductionHypersensitivity reactions (HSRs) to colecalciferol (vitamin D) have been rarely reported and the mechanism is unknown. As an alternative treatment was not recommended for vitamin D deficiency, a desensitization protocol with colecalciferol can be performed. We found that there is no standard desensitization protocol for vitamin D. In this study, we aimed to investigate clinical features and skin test results of patients with HSRs to the vitamin D and effectiveness of the 6-step desensitization protocol in which we applied oral drops of colecalciferol.MethodThis retrospective cross-sectional study included 18 patients with a history of HSRs to oral vitamin D supplements and patients who were planned to receive oral vitamin D replacement. Before desensitization, some of the patients underwent skin tests (skin prick test and intradermal test) with colecalciferol, and the results were recorded. Skin tests were not performed in patients with a history of drug use (antihistamine, systemic steroid, omalizumab, etc.) that affected the results of skin tests. All patients were applied an one bag 6-step desensitization protocol with colecalciferol. Vitamin D3 solution was administered totally 30 drop (4000 IU)/day (1 drop:133.33 IU of 3333 IU/mL) dose of colecalciferol (Devit-3®, DEVA-Türkiye, 15 mL/50,000 IU, 1 mL = 25 drop) at 15-minutes intervals without premedication.ResultsThe patient group consisted of 16 female subjects (89%); the mean age was 46 ± 12 years. When the patients were evaluated in terms of the risk of hypersensitivity reactions according to their clinical history, 5 patients had a history of anaphylaxis with vitamin D preparations (colecalciferol oral drop, n = 3; colecalciferol capsule, n = 2), and 13 patients had a history of HSRs other than anaphylaxis with isolated cutaneous reactions (pruritus, flushing, urticaria and angioedema) (n = 11, colecalciferol oral drop; n = 2, colecalciferol capsule). Skin prick test (SPT) and intradermal test (IDT) were performed on 9 patients. SPTs and IDTs were negative in all patients. Urticaria occur during desensitization in only one patient but vitamin D replacement was performed within the following 48-72 h after HSRs. All other patients tolerated 30 drop (4000 IU) and have continued to take same dose every day for the last 6 weeks with no adverse reactions.ConclusionDesensitization with oral vitamin D preparations has a crucial role for patients who can not receive vitamin D supplements by other ways. Vitamin D drop forms, which are better absorbed than capsule forms which contains the lowest units per/mL without the need to dilute the preparation, not contain any additives with HSRs potential such as gelatin and peanut oil are good option. Our 6-step desensitization protocol with oral drop of colecalciferol is a reliable protocol in patients with a history of vitamin D HSRs.

2024-07-01·Heliyon

Repurposing anti-osteoporosis drugs for autoimmune diseases: A two-sample Mendelian randomization study

Article

作者: Luo, Zongping ; Huang, Xuerong ; Huang, Xiaoxiong ; Cheng, Qi ; Zhang, Qin ; Xiang, Pan ; Yang, Chengyuan ; Shen, Ruoyi

BackgroundDespite the increasing availability of therapeutic drugs for autoimmune diseases, many patients still struggle to achieve their treatment goals. Our aim was to identify whether drugs originally used to treat bone density could be applied to the treatment of autoimmune diseases through Mendelian randomization (MR).MethodsUsing summary statistics from genome-wide association studies, we used a two-sample MR design to estimate the correlation between autoimmune diseases and BMD-related drug targets. Data from the DrugBank and ChEMBL databases were used to identify the drug targets of anti-osteoporosis medications. The Wald ratio test or inverse-variance weighting method was used to assess the impact of genetic variation in drug target(s) on autoimmune disease therapy.ResultsThrough our analysis, we discovered a negative correlation between genetic variability in a specific gene (ESR1) in raloxifene/colecalciferol and various autoimmune disorders such as ankylosing spondylitis, endometriosis, IgA nephropathy, rheumatoid arthritis, sarcoidosis, systemic lupus erythematosus, and type 1 diabetes.ConclusionThese results indicate a possible link between genetic differences in the drug targeting ESR1 and susceptibility to autoimmune disorders. Hence, our study offers significant support for the possible use of drugs targeting ESR1 for the management of autoimmune disorders. MR and drug repurposing are utilized to investigate the relationship between autoimmune diseases and bone mineral density, with a focus on ESR1.

2024-04-01·Hospital Pharmacy

One Year Evaluation of Pharmacist Medication Charting Service in a Principal Referral Women and Newborn Hospital

Article

作者: Mukadam, Nabeelah ; Petrovski, Michael ; Teoh, Stephanie

Background: Accuracy of medication charts on admission to hospital has previously shown that inadvertent omission of therapy was the most common discrepancy, accounting for 40% to 60% of errors. Partnered Pharmacist Medication Charting (PPMC) has shown to reduce medicationrelated problems. Objective: The aim of this study was to evaluate the implementation of Pharmacist Medication Charting (PMC), a derivative of PPMC, in a maternity and gynecological hospital. The occurrence of medication omission identified by the pharmacists was assessed and the pharmacist interventions involving PMC analyzed. Methods: The pharmacist interventions documented from 1st July 2022 to 30th June, 2023 were evaluated using PowerBI for data and trends on the Medication-Related Problems (MRPs) identified, occurrence of PMC, common medications charted by the pharmacists and the pharmacist recommendation and action following the identification of MRPs. Results: A total of 4898 pharmacy interventions was documented in the 12-month period. Of the total interventions documented, 1321 (26.97%) were related to pharmacist medication charting. Of all the interventions related to PMC, 53.29% involved pharmacists charting medications for the continuation or initiation of over-the-counter medications, 13.32% involved pharmacist partnered charting of Prescription Only Medications and Controlled Medications with medical staff, and 33.3% were referred to a credentialled pharmacist for PMC service. With regards to action taken following interventions involving PMC, 1065 (80.62%) were resolved following PMC. Common medications charted by the pharmacists include: macrogol and docusate laxatives (288), pregnancy multivitamin containing iron, iodine and folate (169), colecalciferol (133), iron (127), asthma inhaler (99), paracetamol and ibuprofen (88), nicotine (38), calcium (29), folic acid (26), and pantoprazole (15). Conclusion: Our study demonstrated that hospital pharmacists contribute to the reduction of MRPs, and PMC enables pharmacist to address prescribing omission and conditions untreated in the hospital. This study also reflects skills enhancement in practice for clinical pharmacists and resulted in successful implementation of PMC.

1

项与阿仑膦酸钠/胆骨化醇相关的新闻（医药）

2024-08-15

·PMLiVE

NICE recommends Theramex’s Eladynos to treat bone disease after menopause

The National Institute for Health Care and Research has recommended Theramex’s Eladynos (abaloparatide) as an option for treating bone disease after menopause. Available on the NHS in England in three months, the drug is set to benefit more than 14,000 people in the UK who are seeking treatment for osteoporosis after menopause, if there is a very high risk of fracture. Osteoporosis, a bone disease that affects 3.8 million people in the UK, develops when bone mineral density and bone mass decrease, or when the quality or structure of bone changes, leading to a decrease in bone strength that can increase the risk of broken bones or fractures. The disease particularly affects older women after menopause, as oestrogen, the hormone important for maintaining bone density and strength, decreases and bone density reduces, making broken bones more common. Other treatments for the disease include bisphosphonates such as alendronic acid and ibandronic acid, Eli Lilly’s selective oestrogen receptor modulator, Evista (raloxifene), parathyroid hormone treatments including teriparatide, and biological medicines including Amgen’s Prolia (denosumab) and Amgen/UCB’s Evenity (romosozumab). NICE’s decision was based on patients descriptions of how debilitating osteoporosis can be and how it all impacts day-to-day life, impairing mental and physical health. Theramex’s Eladynos is designed to increase bone density by stimulating the cells that produce new bone while also reducing the risk of fracture, providing an alternative for patients who have not responded to or cannot tolerate usual treatment options. Proven to be more clinically and cost-effective, the alternative treatment option comes as a pre-filled pen that is injected into the muscle through the skin. Prior to this, in March, Bayer shared positive long-term results from the late-stage OASIS 3 study, which supported the use of its investigational non-hormonal menopause drug, elinzanetant, to treat moderate-to-severe vasomotor symptoms (VMS), such as hot flashes, which are reported by up to 80% of women during the menopausal transition. In April, a Canadian study published in Neurology revealed that early menopause and a higher risk of cardiovascular disease could be linked to cognitive decline later in life.

临床结果临床3期上市批准

100 项与阿仑膦酸钠/胆骨化醇相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	M05BB03	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
骨质疏松症	美国	Organon & Co.	2005-04-07
绝经期后骨质疏松	美国	Organon & Co.	2005-04-07

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适应症	最高研发状态	国家/地区	公司	日期
绝经期后骨质疏松	临床前	-	Organon & Co.	2004-05-01
骨质疏松症	临床前	-	Merck Sharp & Dohme Corp.	2004-01-01
维生素D缺乏症	临床前	-	Merck Sharp & Dohme Corp.	2004-01-01

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02132026 (SALTIRE2, Pubmed \| J Am Heart Assoc)	临床3期	血管钙化 18F‐sodium fluoride	-	Denosumab	鑰鹽蓋範廠膚範遞鹽壓(衊鑰淵衊壓鬱餘夢鑰蓋) = 憲繭鏇鹹糧壓製醖積繭襯憲選壓艱廠鏇繭蓋餘 (鹽鏇醖觸齋壓窪構蓋觸, 0 ~ 212) 更多	不佳	2024-09-09
				Alendronic acid	鑰鹽蓋範廠膚範遞鹽壓(衊鑰淵衊壓鬱餘夢鑰蓋) = 獵餘餘獵遞鹽繭淵製鹹襯憲選壓艱廠鏇繭蓋餘 (鹽鏇醖觸齋壓窪構蓋觸, -62 ~ 134) 更多
ASN2021	N/A	小管间质性肾炎和葡萄膜炎	-	Alendronic Acid	鹹夢憲憲夢鑰壓鑰鹽製(範遞壓糧鏇鹹選夢淵齋) = recurrence of her ocular involvement and was diagnosed with anterior uveitis by ophthalmology 餘餘襯網廠願選鑰構顧 (鬱壓鑰積範膚齋窪遞廠 ) 更多	积极	2021-10-27
				Prednisone
WCO_IOF_ESCEO2018	N/A	-	1	Teriparatide	(齋獵選獵憲憲醖糧繭餘) = 夢膚窪夢夢觸夢製餘夢鏇衊獵構廠廠糧憲廠顧 (廠積壓鑰蓋憲製膚膚淵 ) 更多	积极	2018-07-27
				Alendronic acid	願遞廠蓋範鏇製淵廠醖(簾獵顧構襯鑰夢壓蓋鑰) = 簾窪觸範膚繭齋廠範壓鏇餘糧築構鹹鬱蓋艱壓 (願鏇艱觸繭廠獵糧鹽鑰 )
PP.24.09 (ESH2015)	N/A	-	15	Alendronic acid	願衊齋願膚鏇膚憲觸繭(鹹繭範範構範廠簾製齋) = 選壓繭鏇蓋顧蓋襯膚觸築積獵糧遞鑰壓夢積衊 (艱鑰夢構鹹醖遞鹽餘壓 ) 更多	积极	2015-06-01
				Calcium and vitamin D	願衊齋願膚鏇膚憲觸繭(鹹繭範範構範廠簾製齋) = 遞廠衊鹽廠鬱獵夢顧鹹築積獵糧遞鑰壓夢積衊 (艱鑰夢構鹹醖遞鹽餘壓 )