Alisporivir

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Alisporivir
Alisporivir.svg
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
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ECHA InfoCard 100.234.903 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C63H113N11O12
Molar mass 1216.662 g·mol−1
3D model (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 Yes check.svgY
  • Key:OLROWHGDTNFZBH-XEMWPYQTSA-N Yes check.svgY
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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 ]

Related Research Articles

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<span class="mw-page-title-main">Hepatitis C virus</span> Species of virus

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<span class="mw-page-title-main">CXCL10</span> Mammalian protein found in Homo sapiens

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<span class="mw-page-title-main">Telaprevir</span> Chemical compound

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miR-122

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<span class="mw-page-title-main">Sofosbuvir</span> Chemical compound

Sofosbuvir, sold under the brand name Sovaldi among others, is a medication used to treat hepatitis C. It is taken by mouth.

<span class="mw-page-title-main">Simeprevir</span> Chemical compound

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<span class="mw-page-title-main">Faldaprevir</span> Chemical compound

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<span class="mw-page-title-main">Deleobuvir</span> Chemical compound

Deleobuvir was an experimental drug for the treatment of hepatitis C. It was being developed by Boehringer Ingelheim. It is a non-nucleoside hepatitis C virus NS5B polymerase inhibitor. Deleobuvir was tested in combination regimens with pegylated interferon and ribavirin, and in interferon-free regimens with other direct-acting antiviral agents including faldaprevir.

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Ombitasvir is an antiviral drug for the treatment of hepatitis C virus (HCV) infection by AbbVie. In the United States, it is approved by the Food and Drug Administration for use in combination with paritaprevir, ritonavir and dasabuvir in the product Viekira Pak for the treatment of HCV genotype 1, and with paritaprevir and ritonavir in the product Technivie for the treatment of HCV genotype 4.

<span class="mw-page-title-main">Beclabuvir</span> Chemical compound

Beclabuvir is an antiviral drug for the treatment of hepatitis C virus (HCV) infection that has been studied in clinical trials. In February 2017, Bristol-Myers Squibb began sponsoring a post-marketing trial of beclabuvir, in combination with asunaprevir and daclatasvir, to study the combination's safety profile with regard to liver function. From February 2014 to November 2016, a phase II clinical trial was conducted on the combination of asunaprevir/daclatasvir/beclabuvir on patients infected with both HIV and HCV. Furthermore, a recent meta-analysis of six published six clinical trials showed high response rates in HCV genotype 1-infected patients treated with daclatasvir, asunaprevir, and beclabuvir irrespective of ribavirin use, prior interferon-based therapy, or restriction on noncirrhotic patients, IL28B genotype, or baseline resistance-associated variants

<span class="mw-page-title-main">Elbasvir</span> Chemical compound

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References

  1. 1 2 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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