Name | Voclosporin Discontinued |
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Synonyms | voclosporin |
Description | Voclosporin is a calcineurin (CN) inhibitor. |
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Related Catalog | |
Target |
Calcineurin[1] |
In Vitro | This novel semi-synthetic calcineurin (CN) inhibitor is designated Voclosporin (ISATX247). The efficacy of Voclosporin as an immunosuppressive agent is examined using an in vitro calcineurin assay[1]. Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro[2]. |
In Vivo | All animals tolerate Voclosporin (ISATX247) and Cyclosporine A (CsA) very well. There are no severe adverse effects associated with either drug. In the Voclosporin group, all animals except 1 have diarrhea of different durations during the study (mean 2.3 days, range 2 to 7 days). This differs from the CsA and the control groups, where no animals have diarrhea. Mean weight loss at the end of the study is slightly higher in the Voclosporin group than in the CsA and control groups (3.4% vs 2.0% and 1.0%, respectively)[2]. |
Animal Admin | Monkey[2] Wild-caught, male cynomolgus monkeys, weighing between 5 and 8 kg, are used. Four groups of animals are treated twice daily at 8:00 AM and 6:00 PM for 7 days with the following doses: Group I (n=6), Voclosporin 25 mg/kg; Group II (n=6), Voclosporin 50 mg/kg; Group III (n=5), CsA 25 mg/kg; and Group IV (n=4), vehicle (no drug) 1 mL/kg. Levels of Cyclosporine and Voclosporin in whole blood are measured by liquid chromatography/mass spectrometry[2]. |
References |
Molecular Formula | C63H111N11O12 |
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Molecular Weight | 1214.62000 |
Exact Mass | 1213.84000 |
PSA | 278.80000 |
LogP | 4.31560 |
Storage condition | 2-8℃ |