{"doi":"10.1101/2020.09.16.299800","title":"Lopinavir-ritonavir is not an effective inhibitor of the main protease activity of SARS-CoV-2\n                  <i>in vitro</i>","abstract":"<jats:title>ABSTRACT</jats:title>\n                <jats:p>COVID-19 has caused over 900,000 deaths worldwide as of September 2020, and effective medicines are urgently needed. Lopinavir was identified as an inhibitor of the HIV protease, and a lopinavir-ritonavir combination therapy was reported to be beneficial for the treatment of SARS and MERS. However, recent clinical tests could not prove that lopinavir-ritonavir therapy was an effective treatment for COVID-19. In this report, we examined the effect of lopinavir and ritonavir to the activity of the purified main protease (Mpro) protein of SARS- CoV-2, the causative virus of COVID-19. Unexpectedly, lopinavir and ritonavir did not inhibit Mpro activity. These results will aid the drug candidate selection for ongoing and future COVID-19 clinical trials.</jats:p>","journal":null,"year":null,"id":633299,"datarank":0.37273599746820013,"base_score":2.4849066497880004,"endowment":2.4849066497880004,"self_citation_contribution":0.37273599746820013,"citation_network_contribution":0.0,"self_endowment_contribution":0.37273599746820013,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":11,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1641871,"name":"Yea-In Park","orcid":null,"position":1,"is_corresponding":false},{"id":1641872,"name":"Rackhyun Park","orcid":null,"position":2,"is_corresponding":false},{"id":1641873,"name":"Yeo-Eun Cha","orcid":null,"position":3,"is_corresponding":false},{"id":273634,"name":"Sim Namkoong","orcid":"0000-0003-1007-0371","position":4,"is_corresponding":false},{"id":1083709,"name":"Jin I. Lee","orcid":"0000-0001-8074-5413","position":5,"is_corresponding":false},{"id":1641874,"name":"Junsoo Park","orcid":"0000-0002-2355-6760","position":6,"is_corresponding":false},{"id":1641870,"name":"Minsu Jang","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Lopinavir-ritonavir is not an effective inhibitor of the main protease activity of SARS-CoV-2\n                  <i>in vitro</i>","abstract":"<jats:title>ABSTRACT</jats:title>\n                <jats:p>COVID-19 has caused over 900,000 deaths worldwide as of September 2020, and effective medicines are urgently needed. Lopinavir was identified as an inhibitor of the HIV protease, and a lopinavir-ritonavir combination therapy was reported to be beneficial for the treatment of SARS and MERS. However, recent clinical tests could not prove that lopinavir-ritonavir therapy was an effective treatment for COVID-19. In this report, we examined the effect of lopinavir and ritonavir to the activity of the purified main protease (Mpro) protein of SARS- CoV-2, the causative virus of COVID-19. Unexpectedly, lopinavir and ritonavir did not inhibit Mpro activity. These results will aid the drug candidate selection for ongoing and future COVID-19 clinical trials.</jats:p>","is_dataset_classified":null,"base_score":2.4849066497880004,"endowment":2.4849066497880004,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"19910364","pmcid":null,"openalex_id":"https://openalex.org/W3084956028","authors":[],"funders":[],"total_grants":0,"fwci":null,"citation_percentile":null,"influential_citations":0,"citation_trend":[{"year":2021,"count":5},{"year":2022,"count":3},{"year":2023,"count":3}],"oa_status":"green","license":"cc-by-nc-nd","oa_locations":[{"url":"https://www.biorxiv.org/content/biorxiv/early/2020/09/16/2020.09.16.299800.full.pdf","host_type":"repository"},{"url":"https://www.biorxiv.org/content/biorxiv/early/2020/09/16/2020.09.16.299800.full.pdf","host_type":"repository"},{"url":"https://syndication.highwire.org/content/doi/10.1101/2020.09.16.299800","host_type":"publisher"},{"url":"https://doi.org/10.1101/2020.09.16.299800","host_type":"repository"},{"url":"https://europepmc.org/article/PPR/PPR215756","host_type":"Europe_PMC"},{"url":"https://europepmc.org/api/fulltextRepo?pprId=PPR215756&type=FILE&fileName=EMS97951-pdf.pdf&mimeType=application/pdf","host_type":"Europe_PMC"}],"fields_of_study":["COVID-19 Clinical Research Studies","SARS-CoV-2 and COVID-19 Research","SARS-CoV-2 detection and testing"],"mesh_terms":[],"keywords":["Lopinavir","Ritonavir","Lopinavir/ritonavir","Protease inhibitor (pharmacology)","Pharmacology","Virology","Medicine","Protease","Coronavirus disease 2019 (COVID-19)","Virus","Viral load","Biology","Internal medicine","Enzyme","Antiretroviral therapy","Biochemistry","Disease"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-06T11:45:50.069105Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}