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Alisporivir

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Chemical compound Pharmaceutical compound
Alisporivir
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
NIAID ChemDB
ECHA InfoCard100.234.903 Edit this at Wikidata
Chemical and physical data
FormulaC63H113N11O12
Molar mass1216.662 g·mol
3D model (JSmol)
SMILES
  • O=C1N(C(=O)N(C)(C(=O)N(C(=O)N(C(=O)N(C)(C(=O)N(C)(C(=O)N(C)(C(=O)N((C(=O)N(C(=O)N(C)(C(=O)N(CC)1C(C)C)C)CC)(O)(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
  (what is this?)  (verify)

Alisporivir (INN), or Debio 025, DEB025, (or UNIL-025) is a cyclophilin inhibitor. Its structure is reminiscent of, and synthesized from ciclosporin.

It inhibits cyclophilin A. Alisporivir is not immunosuppressive.

It is being researched for potential use in the treatment of hepatitis C. It has also been investigated for Duchenne muscular dystrophy and may have therapeutic potential in Alzheimer's disease.

Alisporivir is under development by Debiopharm for Japan and by Novartis for the rest of the world (licence granted by Debiopharm) since February 2010.

References

  1. ^ Reutenauer J, Dorchies OM, Patthey-Vuadens O, Vuagniaux G, Ruegg UT (October 2008). "Investigation of Debio 025, a cyclophilin inhibitor, in the dystrophic mdx mouse, a model for Duchenne muscular dystrophy". British Journal of Pharmacology. 155 (4): 574–584. doi:10.1038/bjp.2008.285. PMC 2579666. PMID 18641676.
  2. Gallay PA, Lin K (15 February 2013). "Profile of alisporivir and its potential in the treatment of hepatitis C". Drug Design, Development and Therapy. 7: 105–115. doi:10.2147/DDDT.S30946. PMC 3578503. PMID 23440335.
  3. Ptak RG, Gallay PA, Jochmans D, Halestrap AP, Ruegg UT, Pallansch LA, et al. (April 2008). "Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent". Antimicrobial Agents and Chemotherapy. 52 (4): 1302–1317. doi:10.1128/AAC.01324-07. PMC 2292519. PMID 18212100.
  4. Paeshuyse J, Kaul A, De Clercq E, Rosenwirth B, Dumont JM, Scalfaro P, et al. (April 2006). "The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro". Hepatology. 43 (4): 761–770. doi:10.1002/hep.21102. PMID 16557546. S2CID 45825453.
  5. Coelmont L, Kaptein S, Paeshuyse J, Vliegen I, Dumont JM, Vuagniaux G, Neyts J (March 2009). "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. 53 (3): 967–976. doi:10.1128/AAC.00939-08. PMC 2650540. PMID 19104013.
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. "USC study reveals potential new treatment target for Alzheimer's disease | Keck School of Medicine of USC". 14 June 2021. Retrieved 2021-06-16.
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