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clodronate disodium (Abioklad / Mebonat / Ostac)

✓ Approved

Abiogen Pharma S.p.A. · SLC17A9 · 小分子

什么是 clodronate disodium?

clodronate disodium 是一种小分子,由Abiogen Pharma S.p.A.研发。该药已获批,用于治疗相关适应症,给药途径:Injectable (Others)、Intraarterial Injection、Intramuscular (IM) Injection。

药物档案

商品名Abioklad, Mebonat, Ostac
公司Abiogen Pharma S.p.A.
药物类别小分子
分子靶点SLC17A9
给药途径Injectable (Others), Intraarterial Injection, Intramuscular (IM) Injection
状态Approved

作用机制

分子靶点

clodronate disodium 作用于 1 个分子靶点:

SLC17A9solute carrier family 17 member 9 (POROK8, VNUT)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

clodronate disodium 针对 6 个适应症,涉及 3 个治疗领域。

治疗领域疾病/病症分期
Endocrine disordersHypercalcaemia of malignancy✓ Approved
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved
Musculoskeletal and connective tissue disordersOsteoarthritis✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cancer pain✓ Approved
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Breast cancerPhase III

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相关研究文献

PubMedJournal of hazardous materials2026-09-09

HIF-1α-associated macrophage metabolic reprogramming mediates intestinal injury induced by acrylamide and 5-hydroxymethylfurfural co-exposure.

Lu Jiawen J, Shen Yangchun Y, Zhou Xingtao X, Wang Yuting Y et al.

Acrylamide (AA) and 5-hydroxymethylfurfural (HMF) are processing-derived contaminants that frequently co-occur in environmental and dietary exposure, yet the health effects of their co-exposure remain poorly understood. Here, we show that co-exposure to AA and HMF induces duodenal injury in mice, whereas neither toxin alone causes significant damage. Macrophage depletion using clodronate liposomes significantly attenuates this pathology, identifying macrophages as important mediators of the intestinal injury. Co-exposure promotes macrophage polarization toward a pro-inflammatory phenotype. Notably, direct exposure of intestinal epithelial cells to AA and HMF produces limited cytotoxicity. In contrast, conditioned medium from AA+HMF-treated macrophages compromises epithelial viability and barrier integrity in both intestinal epithelial cells and mouse intestinal organoids. These findings indicate that macrophage-mediated inflammatory responses, rather than direct epithelial toxicity, contribute substantially to AA+HMF-induced intestinal injury. Mechanistically, AA and HMF co-exposure triggers mitochondrial dysfunction and elevated mitochondrial reactive oxygen species (mtROS) production in macrophages, accompanied by enhanced glycolysis and hypoxia-inducible factor-1α (HIF-1α) activation. Pharmacological inhibition or genetic silencing of HIF-1α attenuates metabolic and inflammatory responses, while scavenging mtROS or iNOS inhibition reduces macrophage activation. Collectively, these findings reveal an immune-mediated mechanism underlying AA and HMF co-exposure-induced intestinal injury and highlight macrophage responses as a determinant of contaminant mixture toxicity.

PMID 42715669
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PubMedJournal of fish biology2026-09-09

Taste preferences of tiger puffer (Takifugu rubripes) to common amino acids and feed attractants.

Ye Zhengwei Z, Liu Jiahao J, Zhang Yanjiao Y, Li Haoxuan H et al.

The taste preferences of fish which directly influence the feeding action are diversified among species. The present study evaluated the taste preference of tiger puffer (Takifugu rubripes) to a number of compounds including an achiral amino acid (glycine), 16 L-amino acids, 15 D-amino acids and seven commonly used feed attractants. A total of 18 intact and healthy tiger puffers (initial body weight 43.33 ± 3.91 g) were randomly separated in nine 100-L tanks (two fish in each tank as one statistical unit). The test compounds were added in aqueous agar solution to make test pellets. Five parameters indicating the response of fish to pellets, namely, pellet grasp number (GN), ingestion ratio (IR, %), touch span (TS), rejection number (RN) and palatability index (PI), were used for the evaluation of feed palatability, based on which the test compounds were finally identified as attractive, indifferent or repulsive. The Spearman correlation analysis revealed that there was a significant correlation among GN, IR, RN and TS (p < 0.05). The L/D-alanine, L/D-proline, L-serine, L-histidine, glycine and inosine-5'-monophosphate disodium salt octahydrate, whose IR (over 90%) is significantly higher than that of the control, were identified as attractive (p < 0.05). This investigation provided basic information about the taste preferences of tiger puffer to potential feed attractants.

PMID 42712100
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PubMediScience2026-09-06

SEI1 complex silences p53 to drive myeloma progression.

Chen Rui R, Liu Rui R, Fang Zhihong Z, Yang Daoyan D et al.

SEI1 is overexpressed in multiple myeloma and correlates with poor prognosis. In this study, we identify SEI1 as a crucial driver of myeloma pathogenesis through a previously unrecognized mechanism: transcriptional inactivation of the tumor suppressor p53. Mechanistically, SEI1 forms a transcriptional complex with histone deacetylase 1 (HDAC1) and forkhead box C1 (FOXC1), which binds to the p53 promoter, decreases histone H3 lysine 27 acetylation (H3K27ac), and suppresses p53 transcription, thereby promoting myeloma cell proliferation. SEI1 enhances the stability of the HDAC1-FOXC1 interaction, further amplifying p53 repression. High-throughput virtual screening has identified tiludronate disodium as a potent inhibitor of FOXC1. Tiludronate disodium disrupts the HDAC1-FOXC1 interaction, restores H3K27ac enrichment and p53 expression, and suppresses myeloma growth both in vitro and in vivo, including a reduction of osteolytic lesions. These findings elucidate the SEI1/HDAC1/FOXC1/p53 axis as a critical driver of myeloma progression and identify tiludronate disodium as a potential therapeutic agent.

PMID 42698665
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PubMedRegulatory toxicology and pharmacology : RTP2026-09-03

Toxicological evaluation of Disialyllacto-N-neotetraose disodium salt.

Park Eun Jung EJ, Go Hiroe H

Human milk oligosaccharides (HMOs) have gained attention owing to their diverse composition and potential functions, including prebiotic effects, pathogen protection, immune system development, and cognitive development. We produced Disialyllacto-N-neotetraose (DSLNnT) disodium salt, an HMO with beneficial effects such as anti-inflammatory activity, using a unique one-pot enzyme reaction system. However, its safety remains unclear. HMO safety is critical for commercial use in food and pharmaceutical industries. We evaluated the safety of DSLNnT disodium salt using genotoxicity tests (bacterial reverse mutation, in vitro mammalian chromosomal aberration, and in vivo micronucleus tests), a 28-day repeated-dose oral toxicity dose range-finding study in rats, and a 90-day repeated-dose oral toxicity study in rats. DSLNnT disodium salt showed no genotoxic effects in the three genotoxicity tests. In the 90-day repeated-dose oral toxicity study, no DSLNnT disodium salt-related effects were observed in clinical signs, body weight, food intake, water intake, hematology, clinical chemistry, organ weight, necropsy, or histopathological findings at concentrations up to 2000 mg/kg/day. The no-observed-adverse-effect level of DSLNnT disodium salt was 2000 mg/kg/day for males and females. These results provide strong evidence that DSLNnT disodium salt is safe for consumption, supporting its potential commercial application as a functional ingredient in food and pharmaceutical industries.

PMID 42686000
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PubMedInternational journal of women's health2026-09-01

Effect of Disodium Etidronate on Bone Mineral Density in Postmenopausal Women: A Six-Month Prospective Study.

Kong Weihan W, Wang Li L, Xue Huiyu H, Feng Xin X

Postmenopausal osteoporosis, characterized by rapid bone loss, raises fracture risk. Bisphosphonates are standard treatments. This study evaluates the 6-month efficacy of Disodium Etidronate, a first-generation bisphosphonate with a distinct mechanism, on bone mineral density (BMD) at the hip and lumbar spine in postmenopausal women, an area with limited data. This study aimed to assess the effect of a 6-month Disodium Etidronate course on BMD in postmenopausal women. A prospective cohort study enrolled 70 postmenopausal women. Participants received 60 mg of Disodium Etidronate orally once daily for six months. BMD at the femoral neck, trochanter, total hip, and lumbar spine (L1-L4) was measured via dual-energy X-ray absorptiometry (DXA) at baseline and post-treatment. Changes in BMD, site-specific differences, and influencing factors (age, BMI, calcium intake, exercise) were analyzed. After treatment, BMD increased significantly at all sites (all P<0.001): femoral neck (0.70±0.15 to 0.75±0.13 g/cm2), trochanter (0.65±0.10 to 0.70±0.15 g/cm2), total hip (0.72±0.14 to 0.77±0.13 g/cm2), and lumbar spine L1-L4 (0.80±0.13 to 0.86±0.14 g/cm2). The lumbar spine increase exceeded the trochanter's (P=0.023). Age negatively correlated with BMD improvement (β=-0.25, P=0.001), while BMI (β=0.18, P=0.012), calcium intake (β=0.12, P=0.035), and exercise (β=0.15, P=0.021) showed positive correlations. Adverse reactions were mild (10% incidence). A six-month Disodium Etidronate regimen effectively increases BMD in postmenopausal women, with greater efficacy in the lumbar spine. Efficacy is influenced by age, BMI, calcium intake, and exercise. The treatment demonstrates good safety and tolerability.

PMID 42677199
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PubMedBrain, behavior, and immunity2026-08-30

Spatial synaptic pruning mechanism of NAC microglia in differential regulation of PTSD- and depression-like behaviors.

Zhao Mingyue M, Tian Wenyu W, Hu Xinyu X, Dai Jiajie J et al.

Post-traumatic stress disorder (PTSD) comorbid with depression is a prevalent, treatment-refractory clinical syndrome. Emerging evidence indicates shared microglial alterations in PTSD and depression, suggesting it may represent a common pathological substrate. However, the underlying neuroimmune mechanisms remain unclear. PTSD- and depression-like behaviors were induced in rats by using single prolonged stress combined with foot shock (SPS&S). Cellular activity, spatial distribution, and morphology were assessed using qPCR, immunofluorescence, and Golgi-Cox staining. Microglial activity was inhibited using clodronate liposomes (CDSlip) and minocycline. Bulk RNA sequencing was performed to profile neuroimmune-related signaling molecules. Stress induced PTSD- and depression-like behaviors, accompanied by region-specific enhanced microglial activity in the anterior-medial NAC core (amNACc) and lateral NAC shell (LNACsh). Selective depletion of microglia in amNACc and LNACsh via CDSlip specifically alleviated stress induced PTSD- and depression-like behaviors, respectively. Morphological and functional analyses in each region revealed that microglia reshaped the spatial pattern of neuronal structure and function, manifested by enhanced in amNAC and inhibited in LNACsh, via differentially pruning adjacent inhibitory synapses in corresponding region. Further transcriptomic analysis of synaptic pruning relevant signaling pathway showed upregulated expression of "Eat me" signal molecules (particularly Mertk) in the amNAC and downregulated expression of "Find me" signal molecules (particularly Cx3cr1) in the LNACsh, consistent with the observed spatial synaptic pruning profiles. Minocycline administration reversed stress-induced PTSD and depression-like behaviors while normalizing the region-specific alterations in synaptic pruning signaling molecules. Stress may elicit two regionally heterogeneous microglial subpopulations within NAC: phagocytosis-enhanced and recognition-impaired, which remodel the structure and function of local neural networks by differential pruning of inhibitory synapses, thereby driving the manifestation of PTSD- and depression-like behaviors, separately. These findings deepen our understanding of the neuroinflammatory mechanisms underlying trauma-related psychiatric disorders and identify novel targets for immunomodulation-based targets for transdiagnostic interventions .

PMID 42669315
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