阿拉泊韦
化合物
阿拉泊韦（INN：Alisporivir；开发代号：Debio 025、DEB025或UNIL-025）是一种亲环蛋白抑制剂。[1]它是环孢素衍生物。[2]
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| 识别信息 | |
| CAS号 | 254435-95-5  |
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| NIAID ChemDB | |
| ECHA InfoCard | 100.234.903 |
| 化学信息 | |
| 化学式 | C63H113N11O12 |
| 摩尔质量 | 1,216.66 g·mol−1 |
| 3D模型（JSmol） | |
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正在研究它在丙型肝炎治疗中的潜在用途。[5][6][7][8][9][10][11]它还被研究用以治疗杜氏肌营养不良症，[1]并可能具有治疗阿尔茨海默病的潜力。[12]
自2010年2月以来，阿拉泊韦在日本的开发和销售由Debiopharm进行，而诺华则负责世界其他地区开发和销售（由Debiopharm授予许可）。[13]
参考资料
编辑- ^ 1.0 1.1 Reutenauer J, Dorchies OM, Patthey-Vuadens O, Vuagniaux G, Ruegg UT. Investigation of Debio 025, a cyclophilin inhibitor, in the dystrophic mdx mouse, a model for Duchenne muscular dystrophy. British Journal of Pharmacology. October 2008, 155 (4): 574–584. PMC 2579666
. PMID 18641676. doi:10.1038/bjp.2008.285.
- ^ Watashi, Koichi. Alisporivir, a cyclosporin derivative that selectively inhibits cyclophilin, for the treatment of HCV infection. Current Opinion in Investigational Drugs (London, England: 2000). 2010-02, 11 (2) [2024-03-03]. ISSN 2040-3429. PMID 20112171. （原始内容存档于2024-04-13）.
- ^ Gallay PA, Lin K. Profile of alisporivir and its potential in the treatment of hepatitis C. Drug Design, Development and Therapy. 15 February 2013, 7: 105–115. PMC 3578503 . PMID 23440335. doi:10.2147/DDDT.S30946 .
- ^ Ptak RG, Gallay PA, Jochmans D, Halestrap AP, Ruegg UT, Pallansch LA, et al. Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. Antimicrobial Agents and Chemotherapy. April 2008, 52 (4): 1302–1317. PMC 2292519 . PMID 18212100. doi:10.1128/AAC.01324-07.
- ^ Paeshuyse J, Kaul A, De Clercq E, Rosenwirth B, Dumont JM, Scalfaro P, et al. The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro. Hepatology. April 2006, 43 (4): 761–770. PMID 16557546. S2CID 45825453. doi:10.1002/hep.21102 .
- ^ Coelmont L, Kaptein S, Paeshuyse J, Vliegen I, Dumont JM, Vuagniaux G, Neyts J. Debio 025, a cyclophilin binding molecule, is highly efficient in clearing hepatitis C virus (HCV) replicon-containing cells when used alone or in combination with specifically targeted antiviral therapy for HCV (STAT-C) inhibitors. Antimicrobial Agents and Chemotherapy. March 2009, 53 (3): 967–976. PMC 2650540 . PMID 19104013. doi:10.1128/AAC.00939-08.
- ^ Flisiak R, Horban A, Gallay P, et al. The cyclophilin inhibitor Debio-025 shows potent anti-hepatitis C effect in patients coinfected with hepatitis C and human immunodeficiency virus. Hepatology. 2008;47(3):817-826. doi:10.1002/hep.22131
- ^ Flisiak R, Feinman SV, Jablkowski M, et al. The cyclophilin inhibitor Debio 025 combined with PEG IFNalpha2a significantly reduces viral load in treatment-naïve hepatitis C patients. Hepatology. 2009;49(5):1460-1468. doi:10.1002/hep.22835
- ^ Buti M, Flisiak R, Kao JH, et al. Alisporivir with peginterferon/ribavirin in patients with chronic hepatitis C genotype 1 infection who failed to respond to or relapsed after prior interferon-based therapy: FUNDAMENTAL, a Phase II trial. J Viral Hepat. 2015;22(7):596-606. doi:10.1111/jvh.12360
- ^ Pawlotsky JM, Flisiak R, Sarin SK, et al. Alisporivir plus ribavirin, interferon free or in combination with pegylated interferon, for hepatitis C virus genotype 2 or 3 infection. Hepatology. 2015;62(4):1013-1023. doi:10.1002/hep.27960
- ^ Zeuzem S, Flisiak R, Vierling JM, et al. Randomised clinical trial: alisporivir combined with peginterferon and ribavirin in treatment-naïve patients with chronic HCV genotype 1 infection (ESSENTIAL II). Aliment Pharmacol Ther. 2015;42(7):829-844. doi:10.1111/apt.13342
- ^ USC study reveals potential new treatment target for Alzheimer's disease | Keck School of Medicine of USC. 14 June 2021 [2021-06-16]. （原始内容存档于2021-06-14） （美国英语）.
- ^ Novartis wins rights to hepatitis drug. www.manufacturingchemist.com. [2024-03-03]. （原始内容存档于2023-08-29） （英语）.
