Recalbon (minodronic acid) / Ono Pharma - LARVOL DELTA

In silico evaluation of bisphosphonates identifies leading candidates for SARS-CoV-2 RdRp inhibition. (PubMed, J Mol Graph Model) - "A growing list of drugs are being suggested by various in silico, in vitro and ex vivo models, however currently only two treatment options are widely used: the RNA-dependent RNA polymerase (RdRp) inhibitor remdesivir, and the main protease inhibitor nirmatrelvir in combination with ritonavir. In this study, we have investigated all bisphosphonates (BPs) on the ChEMBL database which can bind competitively to nidovirus RdRp-associated nucleotidyl (NiRAN) transferase domain, and systematically down selected seven candidates (CHEMBL608526, CHEMBL196676, CHEMBL164344, CHEMBL4291724, CHEMBL4569308, CHEMBL387132, CHEMBL98211), two of which closely resemble the approved drugs minodronate and zoledronate. This work and our recent paper together provide an in silico mechanistic explanation for alendronate and zoledronate users having dramatically reduced odds of SARS-CoV-2 testing, COVID-19 diagnosis, and COVID-19-related hospitalizations, and indicate that similar observational..."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Development of Minodronic Acid-Loaded Dissolving Microneedles for Enhanced Osteoporosis Therapy: Influence of Drug Loading on the Bioavailability of Minodronic Acid. (PubMed, AAPS PharmSciTech) - "Moreover, MA-MNs prolonged the half-life of MA and provided more steady plasma drug concentrations than intravenously injected MA, which helps to reduce dosing frequency and side effects. Therefore, dissolving MNs with optimized drug loading provides a promising alternative for bisphosphonate drug delivery."

Journal • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Minodronate for severe multiple vertebral fractures due to pregnancy- and lactation-associated osteoporosis: a case report and literature review. (PubMed, Ther Adv Musculoskelet Dis) - "Therefore, careful consideration is required for patients planning pregnancy. Despite bisphosphonates' widespread use and cost-effectiveness, selecting PLO medications involves multiple factors, necessitating further research."

Journal • Review • Back Pain • Lumbar Back Pain • Musculoskeletal Diseases • Musculoskeletal Pain • Obstetrics • Orthopedics • Osteoporosis • Pain • Rheumatology

Efficacy and safety of minodronate in the treatment of postmenopausal osteoporosis with low back pain: a single-centre, randomized and open-label controlled trial. (PubMed, Trials) - P4 | "This study will provide objective evidence for the efficiency and safety of minodronate. Furthermore, it will be helpful to evaluate the quantitative relationship between BTMs and BMD in patients with osteoporosis under different ages."

Journal • Back Pain • Gastroenterology • Gastrointestinal Disorder • Lumbar Back Pain • Musculoskeletal Pain • Osteoporosis • Pain • Rheumatology

Bone augmentation with alloplastic graft material in a patient under bisphosphonate therapy: A case report and literature review. (PubMed, J Oral Implantol) - "She had been taking minodronic acid hydrate (50 mg/4 wk) for 18 mo to treat steroid-induced osteoporosis...Although protracted wound healing without any symptoms of infection was observed, the wound healed completely. No clinical symptoms were observed, the color of the mucosa at the site was healthy, and imaging findings at a six month post-operation indicated that osteogenesis had progressed uneventfully."

Journal • Review • Infectious Disease • Osteoporosis • Rheumatology

Atypical Fracture of the Scapular Spine: A Case Report. (PubMed, Cureus) - "Atypical fractures are gaining attention as a severe potential side effect of long-term treatment with bone-modifying agents (e.g., bisphosphonate and denosumab) for osteoporosis. We describe an atypical fracture of the scapular spine in a 92-year-old Japanese woman with osteoporosis who had been treated with minodronate for ~7 years. Although the dislocation of the fracture site remained after conservative treatment, there was no obstacle to her daily life."

Journal • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

A case of successful treatment of medication-related osteonecrosis of the jaw with conservative treatment for pathological mandibular fracture. (PubMed, Int J Surg Case Rep) - "Conservative treatment can be effective for medication-related osteonecrosis of the jaw with severe cases."

Journal • Dermatology • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Increased risk of hypocalcemia with decreased kidney function in patients prescribed bisphosphonates based on real-world data from the MID-NET® in Japan: a new-user cohort study. (PubMed, BMC Nephrol) - "These findings suggest that the risk of hypocalcemia during BP prescription is higher in patients with decreased kidney function, particularly those with severely decreased kidney function. The quantitative real-world evidence on the safety risk of BPs obtained in this study has led to the PI revision describing a relationship between hypocalcemia risk and decreased kidney function as a regulatory action in Japan and will contribute to promoting the proper use of BPs with appropriate risk management in clinical practice."

Journal • Real-world • Real-world evidence • Endocrine Disorders • Osteoporosis • Renal Disease • Rheumatology

Characterisation of lepidopteran geranylgeranyl diphosphate synthase as a putative pesticide target. (PubMed, Insect Mol Biol) - "Next, we developed and optimised an enzyme assay to screen for potential inhibitors, such as the zoledronate and the minodronate, which showed a dose-dependent inhibition. Considering the essentiality of GGPPS and its putative binding residue variability qualifies a GGPPS as a novel pesticide target. The developed assay may contribute to the identification of novel insecticide leads."

Journal

Current Market Potential and Prospects of Copper-based Pyridine Derivatives: A Review. (PubMed, Curr Mol Med) - "Nicotine, minodronic acid, nicotinamide (niacin), zolpidem, zolimidine, and other pyridine-based chemicals play vital roles in medicine and biology...This paper also discusses significant innovations in the multi-component copper-catalyzed synthesis of N-heterocycles (pyridine), with the aim of developing precise, cost-effective, and environmentally friendly oxygenation and oxidation synthetic methods for the future synthesis of additional novel pyridine base analogs. Therefore, the review article will serve as a novel platform for researchers investigating copper-based pyridine compounds."

Journal • Review

A Facile Crystallization Strategy To Turn Calcium Bisphosphonates Into Novel Osteogenesis-Inducing Biomaterials. (PubMed, Adv Healthc Mater) - "These crystals, including calcium alendronate (CaAln), calcium pamidronate (CaPam), calcium incadronate (CaInc), calcium risedronate (CaRis), calcium zoledronate (CaZol), and calcium di-minodronate (Ca(Min)2), presented high purity, regular morphologies and excellent biodegradability. We believe that these desired biological properties arise from the capability of our insoluble CaBPs in releasing BPs in a sustained manner for stimulating osteogenesis. This work provides a significant strategy for turning CaBPs into novel biomaterials for tissue regeneration and demonstrates their great potential in the clinic."

Journal

Examination of Risk Factors and Expression Patterns of Atypical Femoral Fractures Using the Japanese Adverse Drug Event Report Database: A Retrospective Pharmacovigilance Study. (PubMed, Pharmaceuticals (Basel)) - "Drug-related risk factors for AFF included BPs (i.e., alendronic acid, ibandronic acid, etidronic acid, zoledronic acid, minodronic acid, risedronic acid), denosumab, prednisolone, lansoprazole, rabeprazole, exemestane, letrozole, eldecalcitol, and menatetrenone. Analysis using a Weibull distribution showed wear-out failure-type AFF onset for BPs and denosumab, and both osteoporosis and cancer patients with long-term administration of these drugs showed a tendency to have an increased risk of onset. AFF developed earlier in osteoporosis patients with long-term administration of BPs and denosumab than in cancer patients."

Adverse events • Journal • Retrospective data • Immunology • Inflammatory Arthritis • Lupus • Musculoskeletal Diseases • Oncology • Orthopedics • Osteoporosis • Rheumatology • Systemic Lupus Erythematosus

Effect of organic solvents on calcium minodronate crystal morphology in aqueous solution: an experimental and theoretical study. (PubMed, RSC Adv) - "Furthermore, it was found that the (2 0 0)/(1 1 0) side ratio of Ca(Min) crystal had a linear relationship with the volume of organic solvent and had a certain correlation with some solvent properties. It is believed that the research developed in this work could have a promising application in prediction of Ca(Min) crystal morphology and could give guidance in the selection of organic solvents to control the desirable crystal morphology."

Journal

Effect of Bone Resorption Inhibitors on Serum Cholesterol Level and Fracture Risk in Osteoporosis: Randomized Comparative Study Between Minodronic Acid and Raloxifene. (PubMed, Calcif Tissue Int) - "These results indicated that MIN treatment was more effective in reducing fracture risk in patients with higher LDL cholesterol levels, although its cholesterol-lowering ability was lesser than the RLX treatment.Trial registration University Hospital Medical Information Network-Clinical Trials Registry (UMIN-CTR), No. UMIN000005433; date: April 13, 2011."

Journal • Dyslipidemia • Metabolic Disorders • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Efficacy and Safety of Minodronate in Patients With Low Back Pain (clinicaltrials.gov) - P4 | N=72 | Not yet recruiting | Sponsor: Peking University Third Hospital

New P4 trial • Back Pain • Lumbar Back Pain • Musculoskeletal Pain • Osteoporosis • Pain • Rheumatology

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. (PubMed, J Obstet Gynaecol) - "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."

Journal • Breast Cancer • Cardiovascular • Gynecology • Hematological Disorders • Oncology • Osteoporosis • Ovarian Cancer • Rheumatology • Solid Tumor • Thrombosis • TRAP

Efficacy and Safety of Monthly Minodronate Therapy in Postmenopausal Breast Cancer Patients Receiving Aromatase Inhibitors. (PubMed, Anticancer Res) - "The combined administration of minodronate and AIs was safe and effective in preventing bone loss complications in postmenopausal BC patients."

Journal • Breast Cancer • Musculoskeletal Diseases • Oncology • Osteoporosis • Rheumatology • Solid Tumor • TRAP

A randomized double-blinded placebo-controlled clinical trial of minodronate tablet in postmenopausal Chinese women with osteoporosis (PubMed, Zhonghua Fu Chan Ke Za Zhi) - "The incidence of adverse events was 71.5% (93/130) in the minodronate group and 78.0% (103/132) in the placebo group (P>0.05). Minodronate is effective and safe in the treatment of postmenopausal osteoporosis without severe side effects."

Clinical • Journal • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

A Bone Histomorphometric Analysis of Hypophosphatasia-related Osteoporosis after Teriparatide Treatment. (PubMed, Intern Med) - "Alendronate, teriparatide, and minodronate were administered in that order. In cortical bone, tetracycline double-labeling indicates enhanced bone formation. Teriparatide may thus be a viable treatment option even in patients with hypophosphatasia."

Journal • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Evidence for Proper Use of Medicines Using Medical Big Data: Formulary in a Clinical Setting Using Medical Big Data (PubMed, Yakugaku Zasshi) - "First and second team recommendations were alendronic acid and minodronic acid, and alendronic acid and risedronic acid, respectively...The formulary is focused on controlling the economic burden of medical expenses. We believe that the formulary needs to represent authenticity, reproducibility, and clarity in the procedure and conflicts of interest, with unbiased data to preclude context (hospital)-convenient decisions."

Journal

A Phase III Clinical Study of Minodronate Tablets in Postmenopausal Women With Osteoporosis (clinicaltrials.gov) - P3 | N=330 | Not yet recruiting | Sponsor: Shandong New Time Pharmaceutical Co., LTD

New P3 trial • Osteoporosis • Rheumatology

Utility of monthly minodronate for osteoporosis after gastrectomy: Prospective multicenter randomized controlled trials. (PubMed, Ann Gastroenterol Surg) - "Serious AEs were not observed in either group. This study demonstrated the safety and efficacy of monthly minodronate, suggesting that this treatment may be useful for osteoporosis after gastrectomy (UMIN000015517)."

Clinical • Journal • Gastric Cancer • Gastrointestinal Cancer • Metabolic Disorders • Oncology • Osteoporosis • Rheumatology • Solid Tumor

Drug-induced hypersensitivity syndrome caused by minodronic acid hydrate. (PubMed, BMC Pulm Med) - "We described the first case of DIHS caused by minodronic acid hydrate. Lung lesions in DIHS can present with bilateral diffuse ground-glass opacities and ill-defined centrilobular nodules on a CT scan during the recovery phase. Clinicians should be aware of DIHS, even if patients are not involved with typical DIHS/DRESS-causing drugs."

Journal • Dermatitis • Dermatology • Eosinophilia • Epstein-Barr Virus Infections • Immunology • Interstitial Lung Disease • Pulmonary Disease • Respiratory Diseases • CD4 • CD8 • FOXP3

Nephrotic syndrome with acute kidney injury due to focal segmental glomerulosclerosis following long-term treatment with minodronate. (PubMed, CEN Case Rep) - "Treatment was initiated with the discontinuation of minodronate followed by intravenous methylprednisolone pulse and prednisolone at 35 mg/day. This is, to our knowledge, the first published case of FSGS induced by long-term use of minodronate, and also the first case of cellular variant FSGS induced by bisphosphonates although collapsing variant of FSGS is commonly caused by bisphosphonates. Our study indicates that patients on bisphosphonates should be closely monitored for proteinuria and renal impairment, regardless of the type of bisphosphonate."

Journal • Acute Kidney Injury • Focal Segmental Glomerulosclerosis • Glomerulonephritis • Nephrology • Renal Disease

Analysis of medication-related osteonecrosis of the jaw with bone SPECT/CT: relationship between patient characteristics and maximum standardized uptake value. (PubMed, Dentomaxillofac Radiol) - "Furthermore, maximum SUV of MRONJ was a significant difference for medication (denosumab: 13.62 ± 5.70 and minodronate: 22.98 ± 11.73, p = 0.009) and staging of MRONJ (Stage 2: 15.59 ± 8.06 and Stage 3: 21.51 ± 7.15, p = 0.014). Maximum SUV assessed by SPECT/CT was significantly increased in MRONJ patients with osteoporosis and Stage 3. Bone SPECT/CT could be an effective tool for the analysis of MRONJ."

Clinical • Journal • Breast Cancer • Colorectal Cancer • Gastrointestinal Cancer • Lung Cancer • Oncology • Osteoporosis • Rectal Cancer • Rheumatology • Solid Tumor