- Toxic effects of arbidol include allergic reactions, gastrointestinal issues, and elevated levels of transaminases


Smith College

Arbidol is an antiviral drug that binds to the antigenic protein hemagglutinin and prevents host cell adhesion and membrane fusion and is used to treat influenza. Lopinavir and ritonavir are HIV protease inhibitors that target 3CL protease. 

- Combined therapy of arbidol and lopinavir/ritonavir, rather than lopinavir/ritonavir only, have shown to improve COVID-19 outcomes significantly.
- Arbidol monotherapy may be superior to lopinavir/ritonavir in treating COVID-19 
- Toxicities of Arbidol 
- Toxicities of Lopinavir/Ritonavir 
- Scaffold morphing of arbidol to create analogues for treatment of COVID-19


Arbidol + lopinavir/ritonavir as treatment for COVID-19

Sanders, J. M., Monogue, M. L., Jodlowski, T. Z., & Cutrell, J. B. (2020). Pharmacologic treatments for coronavirus disease 2019 (COVID-19): a review. Jama, 323(18), 1824-1836.
doi:10.1001/jama.2020.6019
https://jamanetwork.com/journals/jama/fullarticle/2764727/

Pharmacologic Treatments for Coronavirus Disease 2019 (COVID-19)


In a recent study published by the Journal of Infection, investigators evaluated the antiviral effects and safety of administering arbidol and lopinavir/ritonavir to treat patients with COVID-19. Fifty patients that had tested positive for COVID-19 were divided into the following two groups, an arbidol group that had 16 patients and a lopinavir/ritonavir group that had 34 patients. The former group received 0.2 g of arbidol, three times a day for a week, while the latter group was given 400 mg/100 mg of lopinavir/ritonavir, twice a day. The data was retrospectively analyzed. RT-PCR assays were used to monitor cycle threshold values of open reading frame 1ab and nucleocapsid genes during antiviral therapy. On day 14 after the admission of the drugs, viral load was not detected in the arbidol group, but was detected in 44.1% patients treated with lopinavir/ritonavir. These results show that the patients receiving arbidol had a shorter duration of the positive RNA test compared to those in the other group. Additionally, apparent side effects were not observed in both groups. Overall, the data reported in this study suggest that arbidol monotherapy may be superior to lopinavir/ritonavir in treating COVID-19.  

Findings suggesting that arbidol monotherapy may be superior to lopinavir/ritonavir in treating COVID-19

In a retrospective cohort study, 33 patients with confirmed COVID-19 infection between 1/17/2020 and 2/13/2020 were divided into two groups: one group received combination therapy of arbidol and lopinavir/ ritonavir (LPV/r) and the other group received LPV/r only. Oral drug administration lasted for 5-21 days. Drug dosages were as follows: 200 mg of arbidol every 8 hours, 400 mg of lopinavir every 12 hours, and 100 mg of ritonavir every 12 hours. Participants had pneumonia but were not receiving invasive ventilation. Nasopharyngeal and stool specimen tests for COVID-19 and chest CT scans were performed regularly.  The outcomes of the study showed that after 7 days, 75% and 69% of patients in the combination therapy group and 35% and 29% of patients in the monotherapy group had negative nasopharyngeal specimen test results and improving CT scans, respectively. Although there was no significant difference between the positive stool tests for COVID-19 of the two groups, it is suggested that the combination therapy drugs can be excreted in feces at high concentrations, making this combination potentially useful for patients with stool-positive results for the virus. Combination therapy was well tolerated by participants. 

Findings in favor of treating COVID-19 infections with arbidol + lopinavir /ritonavir 

- Common toxicities include gastrointestinal intolerance, nausea, vomiting, and 
diarrhea
- Major toxicities include pancreatitis, hepatotoxicity and cardiac conduction abnormalities 

Toxicities of Lopinavir/Ritonavir

- slight structural modification of arbidol can be used to create various analogues that can hinder interactions between SARS-CoV-2 spike protein, ACE2 and host proteases furin and TMPRSS2
- from 569 analogues, 36 were chosen for study for further potential as therapeutics
- A_BR4, A_BR9, A_BR18, A_BR22, and A_BR28 may limit interactions between spike protein and ACE2 receptor as well as other proteases
- A_BR18 and A_BR28 showed multi-targeting potential
- further studies are needed to determine the inhibitory effects on SARS-CoV-2

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