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Design, synthesis and biological evaluation of deuterated Vismodegib for improving pharmacokinetic properties.

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机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu 610041, China [2]Hinova Pharmaceuticals Inc., Suite 402, Building B, #5 South KeYuan Road, Chengdu 610041, China [3]Chengdu University, Sichuan Industrial Institute of Antibiotics, Chengdu 610052, China [4]Frontier Institute of Science and Technology, Xi’an Jiaotong University, Xi’an 710054, China

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关键词： Vismodegib Hedgehog signaling pathway Basal cell carcinoma Deuterated drug Deuterium-hydrogen replacement Pharmacokinetic properties

摘要：

Vismodegib is an oral and high selective hedgehog (Hh) inhibitor used for the treatment of basal cell carcinoma (BCC). In this work, analogs of Vismodegib with deuterium-for-hydrogen replacement at certain metabolically active sites were prepared and found to have a better pharmacokinetic properties in mice. In particular, deuterated compound SKLB-C2211 obviously altered the blood circulation behavior compared to its prototype, which was demonstrated by significantly prolonged blood circulation half-life time (t1/2) and increased AUC0→∞. These results suggested SKLB-C2211 had the potential to be a long-acting inhibitor against Hh signaling pathway, and laid the foundation for the further research of its druggability. Copyright © 2018 Elsevier Ltd. All rights reserved.

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出版当年[2018]版：

大类 | 3 区医学

小类 | 3 区药物化学 3 区有机化学

最新[2023]版：

大类 | 4 区医学

小类 | 2 区有机化学 4 区药物化学

第一作者：

第一作者机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu 610041, China

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通讯作者：

通讯机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu 610041, China [2]Hinova Pharmaceuticals Inc., Suite 402, Building B, #5 South KeYuan Road, Chengdu 610041, China [3]Chengdu University, Sichuan Industrial Institute of Antibiotics, Chengdu 610052, China [4]Frontier Institute of Science and Technology, Xi’an Jiaotong University, Xi’an 710054, China [*1]Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu 610041, China

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Design, synthesis and biological evaluation of deuterated Vismodegib for improving pharmacokinetic properties.

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