The aim of this study is to assess the efficacy of a biphosphonate (tiludronic acid, Skelid®, Sanofi-Aventis) in the treatment of inner ear involvement in advanced otosclerosis

开始日期2012-05-01

申办/合作机构

Assistance Publique des Hôpitaux de Paris SA

100 项与替鲁膦酸二钠相关的临床结果

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100 项与替鲁膦酸二钠相关的转化医学

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100 项与替鲁膦酸二钠相关的专利（医药）

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163

项与替鲁膦酸二钠相关的文献（医药）

2024-10-01·Pharmacological Reports

Determination of bisphosphonate properties in terms of bioavailability, bone affinity, and cytotoxicity

Article

作者: Chmielewska, Ewa ; Voelkel, Adam ; Kaczorek, Ewa ; Burlaga, Natalia ; Pacholak, Amanda ; Zielińska, Monika

AbstractBackgroundThe study aimed to evaluate the therapeutic potential of fourteen newly synthesized bisphosphonates by assessing their bioavailability, bone affinity, and cytotoxicity. These bisphosphonates included a series of aminomethylenebisphosphonates and standard compounds such as risedronate and tiludronate.MethodsDrug permeability was determined using Parallel Artificial Membrane Permeability Assays (PAMPA), while bone affinity was assessed by sorption on hydroxyapatite. Bacterial cell response to the bisphosphonates was also examined using Lactobacillus paracasei cells as a model.ResultsSeveral tested compounds, including BP3 to BP8 and BP11, which feature substituents in the pyridine ring such as methyl groups, iodine, bromine, chlorine, or hydroxyl groups, demonstrated potentially more beneficial therapeutic properties than commercially used bisphosphonates. These compounds showed stronger bone affinity and higher gastrointestinal absorption with comparable or lower cytotoxic effects. Specifically, BP11 exhibited the highest bone affinity, while BP8 and BP11 showed the greatest permeability.ConclusionsThe findings suggest that BP3 BP8, and BP11 are promising candidates for further research. These results highlight the importance of comprehensively evaluating bisphosphonates' therapeutic properties to identify effective treatments for osteoporosis and other bone diseases.Graphical abstract

2024-05-01·Journal of Veterinary Pharmacology and Therapeutics

Effect of clodronate on gene expression in the peripheral blood of horses

Article

作者: Arthur, Rick M ; Rodriguez, Veronika ; Finno, Carrie J ; Knych, Heather K ; Katzman, Scott A ; Wilcox, Callie V

AbstractThere are two FDA‐approved bisphosphonate products, clodronate (Osphos®) and tiludronate (Tildren®), for use in horses. It is hypothesized that bisphosphonates can produce analgesic effects and prevent proper healing of microcracks in bone. Therefore, bisphosphonate use is banned in racehorses. However, bisphosphonates have a short detection window in the blood before sequestration in the skeleton, making the reliability of current drug tests questionable. Seven exercising Thoroughbred horses were administered clodronate (1.8 mg/kg i.m.), and four were administered saline. RNA was isolated from peripheral blood mononuclear cells (PBMCs) collected immediately before a single dose of clodronate or saline and then on Days 1, 6, 28, 56 and 182 post‐dose. mRNA was sequenced and analysed for differentially expressed transcripts. While no single transcripts were differentially expressed, pathway analysis revealed that p38 MAPK (p = .04) and Ras (p = .04) pathways were upregulated, and cadherin signalling (p = .02) was downregulated on Day 1. Previously investigated biomarkers, cathepsin K (CTSK) and type 5 acid phosphatase (ACP5), were analysed with RT‐qPCR in a targeted gene approach, with no significant difference observed. A significant effect of time on gene expression for ACP5 (p = .03) and CTSK (p < .0001) was observed. Thus, these genes warrant further investigation for detecting clodronate use over time.

2023-11-01·Journal of Veterinary Emergency and Critical Care

Retrospective evaluation of acute kidney injury in horses treated with nonnitrogenous bisphosphonates (2013–2020): 8 cases

Article

作者: Magdesian, K Gary ; Edwards, Lisa

AbstractObjectiveTo describe a population of horses with acute kidney injury (AKI) following administration of bisphosphonates including clinical signs, clinicopathologic data, treatment, and outcome.DesignRetrospective study from August 2013 to July 2020.SettingVeterinary university teaching hospital.AnimalsEight adult horses with AKI following administration of nonnitrogenous bisphosphonates.InterventionsNone.Measurements and Main ResultsFive horses received intramuscular clodronate (5/8; 62.5%) and 3 horses received intravenous tiludronate (3/8; 37.5%). Six horses (6/8; 75%) received concurrent nonsteroidal anti‐inflammatory drugs. The most common initial presenting complaint was poor appetite (6/8; 75%), followed by abnormal urination (2/8; 25%). At the time of initial evaluation, the mean serum or plasma creatinine was 451.72 ± 190.06 μmol/L (5.11 ± 2.15 mg/dL) and BUN was 18.84 ± 8.85 mmol/L (52.75 ± 24.77 mg/dL). Five horses (5/6; 83.3%) had either an increased number of red blood cells (n = 4) or hemoprotein (n = 1) in the urine. All horses were treated with IV isotonic, balanced crystalloids either as a bolus, continuous rate infusion, or a combination of the 2. Seven horses (7/8; 87.5%) survived the initial episode of AKI and 1 horse (1/8; 12.5%) was euthanized. Of the 7 surviving horses, 2 horses (2/7; 28.5%) went on to develop chronic renal dysfunction. Warmblood breeds were overrepresented in the AKI group (P = 0.008; odds ratio: 11.5, 95% confidence interval: 1.8–72.1), when compared to horses that received bisphosphonates during the study period and did not develop AKI.ConclusionsBisphosphonate administration, with or without concurrent nonsteroidal anti‐inflammatory drugs, can be associated with AKI in horses. Serum creatinine should be monitored prior to and following bisphosphonate treatment to minimize this risk. Further evaluation of renal function is warranted in horses that develop clinical signs of poor appetite, lethargy, or altered urination in the days following bisphosphonate treatment.

100 项与替鲁膦酸二钠相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02285	替鲁膦酸二钠	M05BA05	DB01133

研发状态

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适应症	国家/地区	公司	日期
畸形性骨炎	法国	Sanofi	1995-01-01

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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2期	欧盟	-	-
绝经期后骨质疏松	临床2期	澳大利亚	-	-
绝经期后骨质疏松	药物发现	加拿大	-	-
绝经期后骨质疏松	药物发现	美国	Sanofi Winthrop LP	-