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All Studies   Meta Analysis    Recent:   

Montelukast and Telmisartan as Inhibitors of SARS-CoV-2 Omicron Variant

Mulgaonkar et al., Pharmaceutics, doi:10.3390/pharmaceutics15071891
Jul 2023  
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28th treatment shown to reduce risk in November 2021
 
*, now with p = 0.0045 from 8 studies.
Lower risk for mortality, hospitalization, and cases.
No treatment is 100% effective. Protocols combine treatments. * >10% efficacy, ≥3 studies.
4,300+ studies for 77 treatments. c19early.org
In Silico and In Vitro study showing that montelukast and telmisartan inhibit SARS-CoV-2 wild-type and the omicron variant. In Silico analysis found montelukast and telmisartan bind to the SARS-CoV-2 spike protein receptor binding domain (RBD) at the ACE2 binding interface. In Vitro, both drugs inhibited wild-type SARS-CoV-2 plaque formation in Vero cells at 50μM. For the omicron variant, montelukast showed inhibition at 1-50μM while telmisartan was only effective at 50μM.
3 preclinical studies support the efficacy of montelukast for COVID-19:
Mulgaonkar et al., 5 Jul 2023, USA, peer-reviewed, 9 authors. Contact: sfernando@tamu.edu (corresponding author).
In Vitro studies are an important part of preclinical research, however results may be very different in vivo.
This PaperMontelukastAll
Montelukast and Telmisartan as Inhibitors of SARS-CoV-2 Omicron Variant
Nirmitee Mulgaonkar, Haoqi Wang, Junrui Zhang, Christopher M Roundy, Wendy Tang, Sankar Prasad Chaki, Alex Pauvolid-Corrêa, Gabriel L Hamer, Sandun Fernando
Pharmaceutics, doi:10.3390/pharmaceutics15071891
Earlier studies with montelukast (M) and telmisartan (T) have revealed their potential antiviral properties against SARS-CoV-2 wild-type (WT) but have not assessed their efficacy against emerging Variants of Concern (VOCs) such as Omicron. Our research fills this gap by investigating these drugs' impact on VOCs, a topic that current scientific literature has largely overlooked. We employed computational methodologies, including molecular mechanics and machine learning tools, to identify drugs that could potentially disrupt the SARS-CoV-2 spike RBD-ACE2 protein interaction. This led to the identification of two FDA-approved small molecule drugs, M and T, conventionally used for treating asthma and hypertension, respectively. Our study presents an additional potential use for these drugs as antivirals. Our results show that both M and T can inhibit not only the WT SARS-CoV-2 but also, in the case of M, the Omicron variant, without reaching cytotoxic concentrations. This novel finding fills an existing gap in the literature and introduces the possibility of repurposing these drugs for SARS-CoV-2 VOCs, an essential step in responding to the evolving global pandemic.
Supplementary Materials: The following supporting information can be downloaded at: https: //www.mdpi.com/article/10.3390/pharmaceutics15071891/s1, Figure S1 : Protein information of SARS-CoV-2 RBD-ACE2 complex (PDB: 6VW1) with secondary structure assessment; Table S1 : RMSD and RMSF evaluation for the last 25 ns and entire MD simulation trajectory, respectively; Table S2 : Prime/MM-GBSA binding free energy calculations for MD of screened compounds with SARS-CoV-2 RBD-ACE2 complex from wild type (WT), and omicron variant; Figure S2: (A Conflicts of Interest: The authors declare no conflict of interest.
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Please send us corrections, updates, or comments. c19early involves the extraction of 100,000+ datapoints from thousands of papers. Community updates help ensure high accuracy. Treatments and other interventions are complementary. All practical, effective, and safe means should be used based on risk/benefit analysis. No treatment or intervention is 100% available and effective for all current and future variants. We do not provide medical advice. Before taking any medication, consult a qualified physician who can provide personalized advice and details of risks and benefits based on your medical history and situation. FLCCC and WCH provide treatment protocols.
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