The Pharmacology of Bisphosphonates: New Advances

Dear Colleagues,

Bisphosphonates (BPs) were first discovered in 1894 by the pharmacist Theodor Salzer. At that time, they were mainly used in industrial processes (in the textile, fertilizer, and oil industries) as corrosion inhibitors or as complexing agents. Bisphosphonates (BPs) are a class of compounds which are receiving growing interest in the pharmaceutical industry. Their therapeutic properties in bone-related disorders (e.g., osteoporosis, Paget′s disease, or bone metastases) makes them the focus of several research studies as well as the main component of numerous pharmaceutical formulations. Their antiresorptive action is related to their high affinity for hydroxyapatite, the main inorganic substituent of bone. On the other hand, the phosphonate groups on their backbone make them excellent ligands for metal ions. The combination of these properties finds potential application in the utilization of such systems as controlled drug release systems (CRSs). Thus, bisphosphonates are currently the target of intensive research, from basic pre-formulation studies to more advanced stages of clinical practice. In addition to such important medicinal use, they display a variety of physiologic activities, which also make them promising anti-cancer, antiprotozoal, antibacterial, and antiviral agents.

It is my great pleasure to invite experts in the field of bisphosphonates to submit manuscripts in the form of short communications, full-length papers, and reviews to this Special Issue. Potential topics include, but are not limited to, the following: innovative synthetic approaches for the preparation of bioactive bisphosphonates, the bioactivity screening of bisphosphonic acids, repurposing and newly discovered biological effects of known compounds, as well as molecular modeling and structure–activity relationship studies. All types of research are encouraged, from in silico studies, through all varieties of in vitro and in vivo research to epidemiological, prospective, and retrospective clinical studies.

I look forward to your valuable contributions.

Dr. Ewa Chmielewska
Prof. Dr. Paweł Kafarski
Guest Editors

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• bisphosphonates
• bisphosphonic acids
• pharmacology of bisphosphonates
• pharmacokinetics
• pharmacodynamics
• hypocalcemia
• osteonecrosis
• gastrointestinal disturbances
• delivery systems of bisphosphonates
• bisphosphonate prodrugs
• osteoporosis
• breast cancer
• prostate cancer
• hypercalcemia
• antiresorptive properties
• antibacterial properties
• anti-cancer properties
• antiparasitic activity
• antiprotozoal properties
• antiviral properties
• effects of drugs on the metabolism and biomechanical properties of bone tissue
• properties and effects of bisphosphonates in in vitro and/or in vivo experimental models of bone disorders
• different bisphosphonates in an in vitro experimental model of bone disease