阿拉泊韦

阿拉泊韦
臨床資料
ATC碼	未分配;
识别信息
CAS号	254435-95-5
PubChem CID	11513676;
ChemSpider	9688467 ;
UNII	VBP9099AA6;
KEGG	D10087 ;
ChEMBL	ChEMBL1651956 ;
NIAID ChemDB	268533;
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（英语：JSmol））	交互式图像;
	SMILES 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 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 ; Key:OLROWHGDTNFZBH-XEMWPYQTSA-N ;

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]

它抑制亲环蛋白A。^[3]阿拉泊韦不具有免疫抑制作用。^[4]

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

^ ^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）.

[pmid18641676-1] 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. （原始内容存档于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 .

[pmid18212100-4] 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.

[pmid16557546-5] 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 .

[pmid19104013-6] 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]. （原始内容存档于2021-06-14）（美国英语）.

[13] Novartis wins rights to hepatitis drug. www.manufacturingchemist.com. [2024-03-03]. （原始内容存档于2023-08-29）（英语）.

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