Chemistry:Alisporivir

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Alisporivir (INN), or Debio 025, DEB025, (or UNIL-025) is a cyclophilin inhibitor.[1] Its structure is reminiscent of, and synthesized from ciclosporin.[citation needed]

It inhibits cyclophilin A.[2] Alisporivir is not immunosuppressive.[3]

It is being researched for potential use in the treatment of hepatitis C.[4][5][6][7][8][9][10] It has also been investigated for Duchenne muscular dystrophy[1] and may have therapeutic potential in Alzheimer's disease.[11]

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

References

  1. ↑ 1.0 1.1 "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. October 2008. doi:10.1038/bjp.2008.285. PMID 18641676. 
  2. ↑ "Profile of alisporivir and its potential in the treatment of hepatitis C". Drug Design, Development and Therapy 7: 105–115. 15 February 2013. doi:10.2147/DDDT.S30946. PMID 23440335. 
  3. ↑ "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. April 2008. doi:10.1128/AAC.01324-07. PMID 18212100. 
  4. ↑ "The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro". Hepatology 43 (4): 761–770. April 2006. doi:10.1002/hep.21102. PMID 16557546. 
  5. ↑ "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. March 2009. doi:10.1128/AAC.00939-08. 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" (in en-US). 14 June 2021. https://keck.usc.edu/usc-study-reveals-potential-new-treatment-target-for-alzheimers-disease/. 



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