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Synthetic Approaches to Inhibitors of Isoprenoid Biosynthesis
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Pedro Merino, Loredana Maiuolo, Ignacio Delso, Vincenzo Algieri, Antonio De Nino, Tomas Tejero
Labeled pamidronic acid-13C3,15N, alendronic acid-15N, zoledronic acid-15N2 and risedronic acid-15N were also synthesized by using typical reaction conditions (Mao et al., 2006). Fluorescently labeled conjugates of risedronate (9) were synthesized using an epoxide linker which was bound to the pyridyl nitrogen. The conjugates were used for fluorescence imaging of Bacillus subtilis (Zhou et al., 2013). Pamidronate (5) have been employed as starting material for the synthesis of 211At-labeled amidobisphosphonates (Yang et al., 2010), while Pamidronate (5), Alendronate (6) and Neridronate (7) were used as precursors to construct new bioconjugates incorporated to polysaccharides, nucleosides (Schott et al., 2011) and oligonucleotides (Lecouvey et al., 1999) in order to increase BPs lifetime in bloodstream or their biological activity.
Bone-targeted agent treatment patterns and the impact of bone metastases on patients with advanced breast cancer in the United States
Published in Current Medical Research and Opinion, 2019
David Henry, Roger von Moos, Jean-Jacques Body, Alex Rider, Jonathan De Courcy, Debajyoti Bhowmik, Francesca Gatta, Guy Hechmati, Yi Qian
Some (25/161; 16%) patients discontinued treatment with zoledronic acid. The main reasons for treatment discontinuation were primary tumor progression (6/25; 24%), short life expectancy (5/25; 20%), poor Karnofsky performance status (4/25; 16%) and patient request (3/25; 12%). Ten patients were switched to a different bone-targeted agent (seven patients were given denosumab, and three were given pamidronic acid). The main reason for the change to an alternative bone-targeted agent was primary tumor progression (4/10; 40%). Thirteen out of 161 patients (8%) received a temporary or permanent dose or regimen change of zoledronic acid. Five of these patients were given zoledronic acid every 4 weeks; three patients were given zoledronic acid every 12 weeks, two patients each were given zoledronic acid either every 3 weeks or every 6 weeks, and one patient was given an alternate regimen. For most patients (7/13), the change in frequency of dosing occurred within the first 3 months of treatment. The main reasons for the switch in dosing frequency were synchronization with other therapies, risk of osteonecrosis of the jaw, presence of hypocalcemia and literature findings (each 2/13).