ArticleJournal of medicinal chemistry2017
Design, Synthesis, and Antimicrobial Evaluation of a Novel Bone-Targeting Bisphosphonate-Ciprofloxacin Conjugate for the Treatment of Osteomyelitis Biofilms.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed.
- Targeting a Myeloid-Regulatory B Cell Network Reverses Immune Paralysis in Periprosthetic Joint Infections.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Effects of hydroxybisphosphonates-conjugated sitafloxacin on fracture healing and skeletal growth in mice.JBMR plus · 2026Article
- Bisphosphonate-Conjugated Sitafloxacin for Treatment ofPharmaceuticals (Basel, Switzerland) · 2025Article
- Fluoroquinolones and Biofilm: A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Article
- Bisphosphonates synergistically enhance the antifungal activity of azoles in dermatophytes and other pathogenic molds.mSphere · 2024Article
- Advances in the targeted theragnostics of osteomyelitis caused by Staphylococcus aureus.Archives of microbiology · 2024Review
- Advances in Bone-Targeting Drug Delivery: Emerging Strategies Using Adeno-Associated Virus.Human gene therapy · 2024Review
- Bisphosphonates for osteoporosis: from bench to clinic.The Journal of clinical investigation · 2024Article
- Article
- Real-Time Impedance-Based Monitoring of the Growth and Inhibition of Osteomyelitis Biofilm PathogenInternational journal of molecular sciences · 2023Article
- The role of myeloid derived suppressor cells in musculoskeletal disorders.Frontiers in immunology · 2023Review
- Article
- Efficacy of Bisphosphonate-Conjugated Sitafloxacin in a Murine Model ofFrontiers in cellular and infection microbiology · 2022Article
- Mini Review Therapeutic Strategies Targeting for Biofilm and Bone Infections.Frontiers in microbiology · 2022Review
- Hydroxy- and Amino-Phosphonates and -Bisphosphonates: Synthetic Methods and Their Biological Applications.Frontiers in chemistry · 2022Review
- Recent Advances in Multifunctional Hydrogels for the Treatment of Osteomyelitis.Frontiers in bioengineering and biotechnology · 2022Review
- Targeting Notch Inhibitors to the Myeloma Bone Marrow Niche Decreases Tumor Growth and Bone Destruction without Gut Toxicity.Cancer research · 2021Article
- Strategies and Approaches for Discovery of Small Molecule Disruptors of Biofilm Physiology.Molecules (Basel, Switzerland) · 2021Review
- Development of Bisphosphonate-Conjugated Antibiotics to Overcome Pharmacodynamic Limitations of Local Therapy: Initial Results with Carbamate Linked Sitafloxacin and Tedizolid.Antibiotics (Basel, Switzerland) · 2021Article
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Authors and funding
16 authors.
Funding
Abstract
Osteomyelitis is a major problem worldwide and is devastating due to the potential for limb-threatening sequelae and mortality. Osteomyelitis pathogens are bone-attached biofilms, making antibiotic delivery challenging. Here we describe a novel osteoadsorptive bisphosphonate-ciprofloxacin conjugate (BV600022), utilizing a "target and release" chemical strategy, which demonstrated a significantly enhanced therapeutic index versus ciprofloxacin for the treatment of osteomyelitis in vivo. In vitro antimicrobial susceptibility testing of the conjugate against common osteomyelitis pathogens revealed an effective bactericidal profile and sustained release of the parent antibiotic over time. Efficacy and safety were demonstrated in an animal model of periprosthetic osteomyelitis, where a single dose of 10 mg/kg (15.6 μmol/kg) conjugate reduced the bacterial load by 99% and demonstrated nearly an order of magnitude greater activity than the parent antibiotic ciprofloxacin (30 mg/kg, 90.6 μmol/kg) given in multiple doses. Conjugates incorporating a bisphosphonate and an antibiotic for bone-targeted delivery to treat osteomyelitis biofilm pathogens constitute a promising approach to providing high bone-antimicrobial potency while minimizing systemic exposure.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.