Publications by authors named "Gerard J Bruin"
Article Synopsis
- Antagonism of the calcium-sensing receptor in the parathyroid gland can lead to PTH release, and calcilytics like AXT914 aim to exploit this for potential bone health benefits.
- AXT914 underwent two clinical trials to assess its pharmacokinetics, pharmacodynamics, and tolerability, showing it was well-tolerated and successfully triggered PTH release.
- However, the trials revealed that AXT914 did not produce the expected positive changes in bone biomarkers and led to increased serum calcium levels, leading to the termination of the study.
Article Synopsis
- Parathyroid hormone (PTH) injections are effective for treating osteoporosis, but there’s a new alternative: an oral calcilytic called ATF936 that increases PTH levels similarly.
- Daily oral dosing of ATF936 in rats led to significant improvements in bone density and structure, showing its effectiveness in promoting bone formation.
- In humans, ATF936 also safely raised PTH levels significantly after a single dose, suggesting it could be a promising new osteoporosis treatment route.
Deferasirox (ICL670) is a novel once-daily, orally administered iron chelator to treat chronic iron overload in patients with transfusion-dependent anemias. Absorption, distribution, metabolism, and excretion of [14C]deferasirox at pharmacokinetic steady state was investigated in five adult beta-thalassemic patients. Deferasirox (1000 mg) was given orally once daily for 6 days to achieve steady state.
View Article and Find Full Text PDFDeferasirox (Exjade, ICL670, CGP72670) is an iron-chelating drug for p.o. treatment of transfusional iron overload in patients with beta-thalassemia or sickle cell disease.
View Article and Find Full Text PDFSensitive radioactivity detection following high performance liquid chromatography (HPLC) separation remains a challenge in many drug metabolism studies with radiolabeled compounds. In this work, solid scintillation counting (SSC) after fraction collection into 96-well plates was evaluated as an off-line radioactivity detection method, in comparison with conventional liquid scintillation counting (LSC). The impact of counting time and biological matrix on the quantification of radiolabeled metabolites and parent drug in samples from animal and human absorption, distribution, metabolism and excretion (ADME) studies was investigated.
View Article and Find Full Text PDFHighly efficient capillary electrochromatographic separations of cardiac glycosides and other steroids are presented. Employing butyl-derivatized silica particles as stationary phase resulted in a nearly three times faster electroosmotic flow (EOF) compared to capillary electrochromatography (CEC) with octadecyl silica particles. On-column focusing with a preconcentration factor of 180 was performed and separation efficiencies of up to 240,000 plates per meter were obtained.
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