維基百科

阿拉泊韋

化合物

阿拉泊韋（INN：Alisporivir；開發代號：Debio 025、DEB025或UNIL-025）是一種親環蛋白抑制劑。[1]它是環孢素衍生物。[2]

阿拉泊韋
臨床資料
ATC碼
  • 未分配
識別資訊
CAS號254435-95-5  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
NIAID ChemDB
ECHA InfoCard100.234.903 編輯維基數據鏈接
化學資訊
化學式C63H113N11O12
摩爾質量1,216.66 g·mol−1
3D模型（JSmol（英語：JSmol））
  • O=C1N[C@H](C(=O)N(C)[C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N(C)[C@H](C(=O)N(C)[C@H](C(=O)N(C)[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N(C)[C@@H](C(=O)N(CC)[C@H]1C(C)C)C)CC)[C@H](O)[C@H](C)C/C=C/C)C)C(C)C)CC(C)C)CC(C)C)C)C)CC(C)C)C(C)C
  • InChI=1S/C63H113N11O12/c1-26-29-30-40(16)52(75)51-56(79)66-44(27-2)59(82)68(20)43(19)58(81)74(28-3)49(38(12)13)55(78)67-48(37(10)11)62(85)69(21)45(31-34(4)5)54(77)64-41(17)53(76)65-42(18)57(80)70(22)46(32-35(6)7)60(83)71(23)47(33-36(8)9)61(84)72(24)50(39(14)15)63(86)73(51)25/h26,29,34-52,75H,27-28,30-33H2,1-25H3,(H,64,77)(H,65,76)(H,66,79)(H,67,78)/b29-26+/t40-,41+,42-,43-,44+,45+,46+,47+,48+,49+,50+,51+,52-/m1/s1 checkY
  • Key:OLROWHGDTNFZBH-XEMWPYQTSA-N checkY

它抑制親環蛋白A。[3]阿拉泊韋不具有免疫抑制作用。[4]

正在研究它在C型肝炎治療中的潛在用途。[5][6][7][8][9][10][11]它還被研究用以治療杜氏肌營養不良症，[1]並可能具有治療阿爾茨海默病的潛力。[12]

自2010年2月以來，阿拉泊韋在日本的開發和銷售由Debiopharm進行，而諾華則負責世界其他地區開發和銷售（由Debiopharm授予許可）。[13]

參考資料

  1. ^ 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. 
  2. ^ 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. （原始內容存檔於2024-04-13）. 
  3. ^ 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  . 
  4. ^ 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. 
  5. ^ 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  . 
  6. ^ 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. 
  7. ^ 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
  8. ^ 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
  9. ^ 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
  10. ^ 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
  11. ^ 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
  12. ^ USC study reveals potential new treatment target for Alzheimer's disease | Keck School of Medicine of USC. 14 June 2021 [2021-06-16]. （原始內容存檔於2021-06-14） （美國英語）. 
  13. ^ Novartis wins rights to hepatitis drug. www.manufacturingchemist.com. [2024-03-03]. （原始內容存檔於2023-08-29） （英語）. 
取自「https://zh.wikipedia.org/w/index.php?title=阿拉泊韦&oldid=84255002」