Chloroquine and hydroxychloroquine for COVID-19 treatment

https://doi.org/10.19106/JMedSciSI005203202002

Dwi Aris Agung Nugrahaningsih(1*), Eko Purnomo(2)

(1) Department of Pharmacology and Therapy, Faculty of Medicine, Public Health, and Nursing Universitas Gadjah Mada
(2) Division of Pediatric Surgery, Department of Pediatric Surgery, Faculty of Medicine, Public Health and Nursing/ Academic Hospital, Universitas Gadjah Mada, Indonesia
(*) Corresponding Author

Abstract


Coronavirus disease 2019 (COVID-19) is an emerging disease caused bysevere acute respiratory syndrome coronavirus-2 (SARS-CoV-2) that has been causing many people around the world affected. There is no approved treatment for COVID-19. Meanwhile, vaccine development still needs a long time before it becomes available to protect people from contracting COVID-19. Repurposing the available drugs is one of the fastest ways to get COVID-19 treatment. Studies have been conducted to discover for COVID-19 treatment that results in the finding of potential medication for COVID-19. Chloroquine and hydroxychloroquine are some of the available medication that shows potential for COVID-19 treatment. Preclinical study showed that the both drugs are active against SARS-CoV-2 in vitro. A pilot clinical study also showed their efficacy in COVID-19 treatment. Many clinical trials are now being conducted to prove their safety and efficacy for the prevention and treatment of COVID-19. However, until now there are not enough data to support the use of these drugs in COVID-19 management. Under the pressure to treat COVID-19 patients with chloroquine or hydroxychloroquine, clinicians shouldnot use these drugs for COVID-19 without considering the available information regarding theiruse for COVID-19. This review summarized the evidence regarding the potential of chloroquine and hydroxychloroquine in COVID-19 management.

Keywords


chloroquine; hydroxychloroquine; COVID-19

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References

  1. Permin H, Norn S, Kruse E, Kruse PR. On the history of Cinchona bark in the treatment of Malaria. Dan Medicinhist Arbog 2016; 44:9-30.
  2. Schrezenmeier E, Dorner T. Mechanism of action ofhydroxychloroquine and chloroquine: implications for rheumatology. Nat Rev Rheumatol 2020; 16(3):155-66. https://doi.org/10.1038/s41584-020-0372-x
  3. Al-Bari MA. Chloroquine analogues in drug discovery: New directions of uses, mechanisms of actions and toxic manifestations from malaria to multifarious diseases. J Antimicrob Chemother 2015; 70:1608–21. https://doi.org/10.1093/jac/dkv018
  4. Rainsfors KD, Parke AL, Clifford-Rashotte M, Kean WF. Therapy and pharmacological properties of hydroxychloroquine and chloroquine in treatment of systemic lupus erythematosus, rheumatoid arthritis and related diseases. Inflammopharmacology 2015; 23(5):231-69. https://doi.org/10.1007/s10787-015-0239-y
  5. Liu J, Cao R, Xu M, Wang X, Zhang H, Hu H, et al. Hydroxychloroquine, a less toxic derivate of chloroquine, is as effective in inhibiting SARS-CoV-2 infection in vitro. Cell Discov 2020; 6:16. https://doi.org/10.1038/s41421-020-0156-0
  6. Ridley RG. Malaria: dissecting chloroquine resistance. Curr Biol 1998; 8(10):R346-9. https://doi.org/10.1016/s0960-9822(98)70218-0
  7. Homewood CA, Warhurst DC, Peters W, Baggaley VC. Lysosomes, pH and the anti-malarial action of chloroquine. Nature 1972; 235(5332):50-2. https://doi.org/10.1038/235050a0
  8. Yayon A, Cabantchik ZI, Ginsburg H. Identification of the acidic compartment of Plasmodium falciparum-infected human erythrocytes as the target of the antimalarial drug chloroquine. EMBO J 1984; 3(11):2695-700.
  9. Sullivan DJ Jr, Matile H, Ridley RG, Goldberg DE. A common mechanism for blockade of heme polymerization by antimalarial quinolines. J Biol Chem 1998; 273(47):31103–7. https://doi.org/0.1074/jbc.273.47.31103
  10. Circu M, Cardelli J, Barr MP, O’Byrne K, Mills G, El-Osta H. Modulating lysosomal function through lysosome membrane permeabilization or autophagy suppression restores sensitivity to cisplatin in refractory non-small-cell lung cancer cells. PLoS One 2017; 12(9):e0184922. https://doi.org/10.1371/journal.pone.0184922
  11. Ballabio A, Bonifacino JS. Lysosomes as dynamic regulators of cell and organismal homeostasis. Nat Rev Mol Cell Biol 2019; 21(2):101-18. https://doi.org/10.1038/s41580-019-0185-4
  12. Ghislat G, Lawrence T. Autophagy in dendritic cells. Cell Mol. Immunol 2018; 15:944-52. https://doi.org/10.1038/cmi.2018.2
  13. Rebecca VW, Nicastri MC, Fennelly C, Chude CI, Barber-Rotenberg JS, Ronghe A, et al. PPT1 promotes tumor growth and is the molecular target of chloroquine derivatives in cancer. Cancer Discov 2019; 9(2):220-9. https://doi.org/10.1158/2159-8290.CD-18-0706
  14. Ewald SE, Lee BL, Lau L, Wickliffe KE, Shi GP, Chapman HA, et al. The ectodomain of Toll-like receptor 9 is cleaved to generate a functional receptor. Nature 2008; 456(7222):658-62. https://doi.org/10.1038/nature07405
  15. van den Borne BE, Dijkmans BA, de Rooij HH, le Cessie S, Verweij CL. Chloroquine and hydroxychloroquine equally affect tumor necrosis factor-alpha, interleukin 6, and interferon-gamma production by peripheral blood mononuclear cells. J Rheumatol 1997; 24(1):55-60.
  16. D’Alessandro S, Scaccabarozzi D, Signorini L, Perego F, Ilboudo DP, Ferrante P, et al. Theuse of antimalarial drugs against viralinfection. Microorganism 2020; 8(1):E85. https://doi.org/10.3390/microorganisms8010085
  17. Khan M, Santhosh SR, Tiwari M, Lakshmana Rao PV, Parida M. Assessment of in vitro prophylactic and therapeutic efficacy of chloroquine against Chikungunya virus in Vero cells. J Med Virol 2010; 82(5):817-24. https://doi.org/10.1002/jmv.21663
  18. De Lamballerie X, Boisson V, Reynier JC, Enault S, Charrel RN, Flahault A, et al. On chikungunya acute infection and chloroquine treatment. Vector Borne Zoonotic Dis 2008; 8(6):837-9. https://doi.org/10.1089/vbz.2008.0049
  19. Dowall SD, Bosworth A, Watson R, Bewley K, Taylor I, Rayner E, et al. Chloroquine inhibited Ebola virus replication in vitro but failed to protect against infection and disease in the in vivo guinea pig model. J Gen Virol 2015; 96:3484-92. https://doi.org/10.1089/vbz.2008.0049
  20. Ooi EE, Chew JS, Loh JP, Chua RC. In vitro inhibition of human influenza A virus replication by chloroquine. Virol J 2006; 3:39. https://doi.org/10.1186/1743-422X-3-39
  21. Paton NI, Lee L, Xu Y, Ooi EE, Cheung YB, Archuleta S, et al. Chloroquine for influenza prevention: A randomised, double-blind, placebocontrolled trial. Lancet Infect Dis 2011; 11:677-83. https://doi.org/10.1016/s1473-3099(11)70065-2
  22. Jacobson JM, Bosinger SE, Kang M, Belaunzaran-Zamudio P, Matining RM, Wilson CC, et al. The effect of chloroquine on immune activation and interferon signatures associated with HIV-1. AIDS Res Hum Retrovir 2016; 32(7):636-47. https://doi.org/10.1089/AID.2015.0336
  23. Blanchard E, Belouzard S, Goueslain L, Wakita T, Dubuisson J, Wychowski C, et al. Hepatitis C virus entry depends on clathrin-mediated endocytosis. J Virol 2006; 80:6964-72. https://doi.org/10.1128/JVI.00024-06
  24. Borges MC, Castro LA, Fonseca BA. Chloroquine use improves dengue-related symptoms. Mem Inst Oswaldo Cruz 2013; 108(5):596-9. https://doi.org/10.1590/s0074-02762013000500010
  25. Keyaerts E, Vijgen L, Maes P, Neyts J, Van Ranst M. In vitro inhibition of severe acute respiratory syndrome coronavirus by chloroquine. Biochem Biophys Res Commun 2004; 323(1):264-8. https://doi.org/10.1016/j.bbrc.2004.08.085
  26. Dyall J, Coleman CM, Hart BJ, Venkataraman T, Holbrook MR, Kindrachuk J, et al. Repurposing of clinically developed drugs for treatment of Middle East respiratory syndrome coronavirus infection. Antimicrob Agents Chemother 2014; 58(8):4885-93. https://doi.org/10.1128/AAC.03036-14
  27. Cassell S, Edwards J, Brown DT. Effects of lysosomotropic weak bases on infection of BHK-21 cells by Sindbis virus. J Virol 1984; 52(3):857-64.
  28. Savarino A, Gennero L, Sperber K, Boelaert JR. The anti-HIV-1 activity of chloroquine. J Clin Virol 2001; 20(3):131-5. https://doi.org/10.1016/s1386-6532(00)00139-6
  29. Vincent MJ, Bergeron E, Benjannet S, Erickson BR, Rollin PE, Ksiazek TG. Chloroquine is a potent inhibitor of SARS coronavirus infection and spread. Virol J 2005; 2:69. https://doi.org/ 10.1186/1743-422X-2-69
  30. Wang M, Cao R, Zhang L, Yang X, Liu J, Xu M, et al. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro. Cell Res 2020; 30(3):269-71. https://doi.org/10.1038/s41422-020-0282-0
  31. Liu J, Cao R, Xu M, Wang X, Zhang H, Hu H, et al. Hydroxychloroquine, a less toxic derivate of chloroquine, is as effective in inhibiting SARS-CoV-2 infection in vitro. Cell Discov 2020; 6:16. https://doi.org/10.1038/s41421-020-0156-0
  32. Gao J, Tian Z, Yang X. Breakthrough: chloroquine phosphate has shown apparent efficacy in treatment of COVID-19 associated pneumonia in clinical studies. Biosci Trends 2020; 14(1):72-3. https://doi.org/10.5582/bst.2020.01047
  33. Borba MGS, Val FFA, Sampaio VS, Alexandre MAA, Melo GC, Brito M, et al. Effect of high vs low doses of chloroquine diphosphate as adjunctive therapy for patients hospitalized with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection: arandomized clinical trial. JAMA Netw Open 2020; 3(4):e208857.
  34. China National Health Comission. Chinese clinical guidance for COVID-19 pneumonia diagnosis and treatment, 7th ed. March 4th, 2020. Available from:http://kjfy.meetingchina.org/msite/news/show/cn/3337.html
  35. Korea Biomedical Review. Physicians work out treatment guidelines for coronavirus. Available from: https://www.koreabiomed.com/news/articleView.html?idxno=7428.
  36. Interim clinical guideline for adult with suspected or conformed COVID-19 in Belgium. Available from: https://epidemio.wiv-isp.be/ID/Documents/Covid19/COVID19_InterimGuidelines_Treatment_ENG.
  37. Italian Society of Infectious and Tropical Diseases. Handbook for the care of people with disease-COVI 19. 2.0 ed., 2020.
  38. Clinical trial. gov. Available from: https://clinicaltrials.gov/ct2/results?cond=COVID19&term=chloroquine&cntry=&state=&city=&dist.Accessed on April 30th, 2020.
  39. Gautret P, Lagier JC, Parola P, Hoang VT, Meddeb L, Mailhe M, et al.Hydroxychloroquine and azithromycin as a treatment of COVID-19: results of an open-label non-randomized clinical trial. Int J Antimicrob Agents 2020; 105949. https://doi.org/10.1016/j.ijantimicag.2020.105949
  40. Srinivasa A, Tosounidou S, Gordon C. Increased incidence of gastrointestinal side effects in patients taking hydroxychloroquine: a brand-related issue? J Rheumatol 2017; 44(3):398. https://doi.org/10.3899/jrheum.161063
  41. Chatre C, Roubille F, Vernhet H, Jorgensen C, Pers YM. Cardiac complications attributed to chloroquine and hydroxychloroquine: a systematic reviewof the literature. Drug Saf 2018; 41(10):919-31. https://doi.org/10.1007/s40264-018-0689-4
  42. Jorge A, Ung C, Young LH, Melles RB, Choi HK. Hydroxychloroquine retinopathy implications of research advances for rheumatology care. Nat Rev Rheumatol 2018; 14(12):693-703. https://doi.org/10.1038/s41584-018-0111-8
  43. Rx List. Aralendrug description. Available from: https://www.rxlist.com/aralen-drug.htm. Accessed on April 30th, 2020.
  44. Rx List. Plaquenil drug description. Available from: https://www.rxlist.com/ plaquenil-drug.htm. Accessed on April 30th, 2020.
  45. Mehra MR, Desai SS, Ruschitzka F, Patel AN. Hydroxychloroquine or chloroquine with or without a macrolide for treatment of COVID-19: a multinational registry analysis. Lancet 2020; S0140-6736(20):31180-6. https://doi.org/10.1016/S0140-6736(20)31180-6



DOI: https://doi.org/10.19106/JMedSciSI005203202002

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