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alendronate (Binosto / Steovess / EX101)

✓ Approved

Ahn-Gook Pharmaceutical · 小分子 · 小分子

什么是 alendronate？

alendronate 是一种小分子，由Ahn-Gook Pharmaceutical研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Binosto, Steovess, EX101
公司Ahn-Gook Pharmaceutical
药物类别小分子
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Ahn-Gook Pharmaceutical

治疗适应症

alendronate 针对 3 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Musculoskeletal and connective tissue disordersOsteoporosis✓ Approved
Congenital, familial and genetic disordersHypertrophic cardiomyopathyPhase III
Musculoskeletal and connective tissue disordersOsteoarthritisPhase II

相关研究文献

PubMedTalanta2026-10-25

Effervescent-tablet-integrated derivatization and salting-out extraction for LC-FLD determination of neuropathic pain drugs in human plasma.

Gao Yaping Y, Zhang Xiaofei X, Wang Lanjie L, Ma Yixin Y et al.

Reliable measurement of neuropathic pain medications in plasma is required for pharmacokinetic evaluation and therapeutic monitoring; however, their high polarity and weak intrinsic UV/fluorescence signals complicate chromatographic detection. We therefore established a one-pot procedure in which a multifunctional effervescent tablet enables effervescence-assisted derivatization and salting-out liquid-liquid extraction (EAD-SALLE) for pregabalin, gabapentin, and mirogabalin. Each preprepared tablet (8 mm in diameter and 2 mm thick) contained 2.3 mg of 6-aminoquinolyl-N-hydroxysuccinimidyl carbamate (AQC), together with 108.7 mg of Na2CO3 and 47.3 mg of NaH2PO4 (molar ratio, 2.6:1). Introducing the tablet into the aqueous sample-acetonitrile system triggered CO2-mediated mixing, established the required pH, promoted AQC labeling, and induced phase separation; the combined pretreatment was completed in a single tube within approximately 3.5 min. Analyte peak areas obtained using tablets stored dry for 3 months were similar to those obtained using fresh tablets. The assay afforded coefficients of determination above 0.999, limits of detection of 0.011-0.023 μg/mL, relative standard deviations not exceeding 10.71%, and relative recoveries of 96.13-108.42%. Analysis of the tested plasma samples indicated that the platform provides a rapid, practical, and economical route to LC-FLD analysis of these drugs.

PMID 42925680
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PubMedAdvanced materials (Deerfield Beach, Fla.)2026-10-25

A Novel pH-Activatable Nanozyme for Treating Breast Cancer Bone Metastasis by Regulating Cancer Cell Metabolic Reprogramming and the Tumor Microenvironment.

Qiao Qianqian Q, Wang Haosheng H, Chen Ying Y, An Xueying X et al.

Multi-omics analyses implicate enhanced oxidative phosphorylation (OXPHOS) in breast cancer bone metastasis (BCBM). To target this metabolic vulnerability, we develop SPMMPA, a bone-targeted nanozyme comprising a Prussian blue core, a disulfide-bridged mesoporous silica interlayer, and a manganese oxide shell, functionalized with polyethylenimine, alendronate, and the Ser-Asp-Ser-Ser-Asp peptide. Its acid-enhanced catalytic activity promotes reactive oxygen species production and glutathione depletion, accompanied by mitochondrial dysfunction, reduced OXPHOS and adenosine triphosphate production, and downregulation of peroxisome proliferator-activated receptor gamma coactivator 1-alpha. Alendronate and silicon release contribute to reduced osteoclast activity and preservation of bone structure. Near-infrared irradiation further enhances treatment efficacy through photothermal heating below 48°C. In mouse models of BCBM, SPMMPA suppresses tumor growth and alleviates osteolysis, without overt toxicity in the assays performed. These findings support a pH-responsive catalytic strategy that couples disruption of tumor energy metabolism with protection of bone homeostasis.

PMID 42924489
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PubMedAdvanced healthcare materials2026-10-25

Probiotic Extracellular Vesicles Enable Oral Alendronate Therapy for Glucocorticoid-Induced Osteoporosis.

Ruan Jing J, Ma Yilei Y, Zhang Ke K, Wu Baoting B et al.

Glucocorticoid-induced osteoporosis (GIOP) involves impaired bone remodeling, intestinal dysbiosis, and immune imbalance, which together limit the long-term benefit of conventional oral bisphosphonate therapy. Here, we report LpEVs@ALN, a probiotic extracellular vesicle-based oral nanoplatform constructed by loading alendronate (ALN) into Lacticaseibacillus paracasei-derived extracellular vesicles. LpEVs@ALN maintains vesicle integrity and epithelial compatibility, improves ALN retention under acidic exposure, and enables sustained ALN release at intestinal pH conditions. In dexamethasone-suppressed BMSCs, LpEVs@ALN enhances osteogenic differentiation, as evidenced by increased ALP activity and matrix mineralization. In zebrafish GIOP models, LpEVs@ALN improves cranial mineralization, new bone formation, scale regeneration, and locomotor/shoaling performance; accompanied by reduced inflammatory tone, improved ALP/RANKL-associated bone turnover readouts, and rebalanced oxidative-stress indices. Microbiome profiling shows recovery of richness/diversity and reduced Proteobacteria dominance, while scale RNA-seq reveals broad reversal of glucocorticoid-driven dysregulation toward pro-osteogenic and anti-inflammatory programs. Integrated correlation analysis further linked microbial remodeling with systemic and skeletal responses, suggesting involvement of the gut-immune-bone axis. Collectively, LpEVs@ALN alleviates GIOP by combining ALN-mediated bone protection with probiotic extracellular vesicle-associated regulation of intestinal and systemic homeostasis, highlighting its potential as an oral therapeutic strategy for GIOP.

PMID 42926358
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PubMedBone2026-10-25

Cumulative antiresorptive exposure and dentoalveolar procedures increase medication-related osteonecrosis of the jaw risk in U.S. veterans treated for fracture prevention.

Elam Rachel E RE, Schousboe John T JT, Finch Dezon D, Huo Zhiping Z et al.

Medication-related osteonecrosis of the jaw (MRONJ) is a rare but serious complication of bisphosphonate (BP) or denosumab therapy. Prior studies evaluating MRONJ risk factors largely involve cancer populations, small samples, claims-based data, or limited covariate assessment. We sought to determine MRONJ risk factors among patients receiving antiresorptives for osteoporosis. A retrospective cohort study of adults ≥50 years in the U.S. Veterans Health Administration with comprehensive dental benefits prescribed ≥1 oral (alendronate, risedronate, ibandronate) or intravenous (zoledronic acid, ibandronate) BP or denosumab between 10/1/1999-12/31/2022 was performed. Individuals with non-osteoporosis indications or dosing regimens, other BP or anabolic osteoporosis medication use, or missing covariates were excluded. Demographics, clinical characteristics, and medications were determined. Invasive dentoalveolar procedures were ascertained using Current Dental Terminology codes. Natural language processing of electronic medical records identified MRONJ events through 12/31/2023. Cox models estimated hazard ratios (HRs). Baseline characteristics were fixed, while comorbidities, medications (including cumulative antiresorptive exposure), and dental procedures were modeled as time-varying, updated at 90-day intervals. Among 42,378 Veterans contributing 381,437 person-years, 44 developed MRONJ. Cumulative 20-year MRONJ incidence was 0.18% (95% confidence interval (CI): 0.13-0.25%). In multivariable-adjusted analyses, Multiracial versus White race (HR: 5.47; 95% CI: 1.31-22.91), baseline body mass index (HR: 0.89 per 1 kg/m2 increase; 95% CI: 0.84-0.96), cumulative antiresorptive exposure (HR: 1.34 per 1-year increase; 95% CI: 1.15-1.56), and recent invasive dentoalveolar procedure (HR: 4.40; 95% CI: 1.70-11.38) were independently associated with MRONJ. MRONJ incidence was very low among patients receiving antiresorptives for osteoporosis, although associations of cumulative antiresorptive exposure and dentoalveolar procedures with MRONJ risk may inform shared decision-making.

PMID 42926073
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PubMedAdvanced healthcare materials2026-10-23

Alendronate-Conjugated Citrate-Based Composite Microscaffolds Promote Osteoporotic Bone Regeneration via Activating Osteogenesis and Suppressing Osteoclastogenesis.

Ma Shiyuan S, Kang Jingyang J, Jia Lei L, Wang Yue Y et al.

Healing of osteoporotic bone defects is profoundly compromised by the dysregulation of bone remodeling homeostasis, characterized by excessive osteoclastic resorption and diminished osteoblastic activity, thus conventional bioinert bone cements fail to modulate these aberrant conditions or restore physiological remodeling. To address this, alendronate-conjugated citrate-based composite microscaffolds, consisting of an alendronate (ALN) conjugated poly (octamethylene citrate) prepolymer mixed with hydroxyapatite (HA) (APOC-HA), was developed followed by thermal post-polymerization. Benefiting from the novel composite cylinder fabrication process using powder compression method in a custom-designed three-part split mold, and the chelation interaction between ALN and HA, the compression strength of the nonporous composite cylinders exceeded 250 MPa. Upon implantation, ALN conjugated on the polymer chains effectively inhibits osteoclast activity as the material degrades. Simultaneously, the sustained release of citrate, a key metabolic regulator, enhances the energy metabolism of bone marrow mesenchymal stem cells (BMSCs) via participating tricarboxylic acid (TCA) cycle, promoting osteogenic differentiation and mineralization. The crosslinked APOC-HA scaffold provides robust mechanical support and excellent biocompatibility while improving bone homeostasis. Consequently, this dual-functional biomaterial offers favorable conditions for regeneration in osteoporotic defects, representing a promising strategy for future clinical applications.

PMID 42908404
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PubMedChemistry & biodiversity2026-10-23

Synthesis of a Series of Heterocyclic N-Substituted Derivatives of Alendronic Acid and Their Preliminary Biological Evaluation.

Nasulewicz-Goldeman Anna A, Goszczyński Tomasz M TM, Wietrzyk Joanna J, Goldeman Waldemar W

The aim of this work was to examine the influence of introduction of heteroaromatic motifs like pyridyl and imidazole rings into alendronic acid molecule on its biological properties. For this purpose, a series of heterocyclic N-substituted alendronate derivatives were synthesized via a two-step, one-pot procedure. This procedure involves the condensation of alendronate and heteroaromatic aldehydes in the presence of triethylamine, which leads to the formation of appropriate Schiff bases, followed by the in situ reduction of the resulting imines with sodium borohydride. The study investigated the ability of the obtained bisphosphonates to bind to hydroxyapatite (HAP), as well as their antiproliferative effect against RAW 264.7 mouse macrophages, MCF-7 human breast cancer and MCF-10A normal breast epithelial cells. Among the tested derivatives, the 2-imidazole derivative (4f) and its N-methylated analog (4g) showed the best activity against both RAW 264.7 macrophages and MCF-7 cells, with an IC50 value of 19.4 and 76.1 µM and of 26.4 and 107.9 µM, respectively. Furthermore, all synthesized derivatives were non-cytotoxic toward MCF-10A normal cells under the tested experimental conditions. The 4(5)-imidazole (4e) derivative showed the highest affinity to HAP.

PMID 42908356
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