Pharmaceutical composition for preventing or treating coronavirus disease-19
Inventors
Lee, Sang Yup • JANG, Woo Dae • KIM, Seungtaek • JEON, Sangeun
Assignees
Korea Advanced Institute of Science and Technology KAIST • Institut Pasteur Korea
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Publication Number
US-12544360-B2
Publication Date
2026-02-10
Expiration Date
Abstract
The present invention relates to a pharmaceutical composition for preventing or treating coronavirus disease 2019, and more specifically to a pharmaceutical composition for preventing or treating coronavirus disease 2019 found by drug repositioning technology using drug virtual screening technology. The pharmaceutical composition for preventing or treating coronavirus disease 2019 according to the present invention is a composition obtained by finding new uses for drugs, which have already been proven effective, for preventing or treating coronavirus disease 2019 by drug repositioning technology. The pharmaceutical composition is useful because it has significantly lower side effects than new drugs and can be rapidly applied to clinical practice.
Core Innovation
The invention describes repositioning-based identification and use of COVID-19 therapeutic drug candidates by targeting SARS-CoV-2 main protease (Mpro) and RNA-dependent RNA polymerase (RdRP). It includes virtual screening of drug candidates using drug-structure libraries and molecular docking/interaction-similarity screening to identify compounds with binding to Mpro or RdRP.
The invention further centers on therapeutic treatment of coronavirus disease 2019 (COVID-19) in a subject in need thereof by administering tipifarnib together with one or more compounds selected from omipalisib, blonanserin, emodin, and remdesivir. It also reports synergistic two-drug combinations using concentration-response matrices and synergy models including Loewe, Bliss, ZIP (Zero Interaction Potency), and HSA (Highest Single Agent).
The invention additionally summarizes pharmaceutical composition scope for the disclosed treatment context, including pharmaceutically acceptable carriers and dosage forms/routes, and method/use claims centered on Mpro/RdRP binders and selected multi-compound combinations. Dependent claim refinements are described as focusing on dosing/administration by specifying concentration ranges and bounds (in µM) for tipifarnib and the co-administered compounds.
Claims Coverage
Independent claim clm-00001 covers a prevention or treatment method for COVID-19 using a fixed combination framework: tipifarnib administered with one or more compounds selected from omipalisib, blonanserin, emodin, and remdesivir. The coverage includes multiple inventive features centered on the required drug combination set and specified co-administration context, with dependent claims refining the selection to particular co-administered compounds and adding µM concentration bounds/intervals for administration.
Tipifarnib plus selected COVID-19 co-administered compounds
Administering tipifarnib and administering one or more compounds selected from omipalisib, blonanserin, emodin, and remdesivir for preventing or treating coronavirus disease 2019 (COVID-19) in a subject in need thereof.
Tipifarnib combined with specified blonanserin concentration ranges
Administering blonanserin together with tipifarnib at specified concentration ranges (in µM) for the prevention or treatment of COVID-19.
Tipifarnib combined with specified emodin concentration ranges
Administering emodin together with tipifarnib using defined threshold and interval constraints in µM (including more than 0 µM up to 11 µM for one parameter set, and emodin at 1.97 µM to 31.45 µM) for the prevention or treatment of COVID-19.
Tipifarnib combined with specified omipalisib concentration bounds
Administering omipalisib together with tipifarnib using alternative specified concentration bounds in µM (including options using more than 0 µM and not more than stated maximums) for the prevention or treatment of COVID-19.
Tipifarnib with specified remdesivir and tipifarnib concentration bounds
Administering remdesivir at a concentration greater than 0 µM and up to 20.18 µM and administering tipifarnib at a concentration greater than 0 µM and up to 11 µM for preventing or treating COVID-19.
Across the independent claim and its dependent refinements, the claimed coverage is directed to preventing or treating COVID-19 by administering tipifarnib together with one or more selected co-administered compounds from omipalisib, blonanserin, emodin, and remdesivir, with dependent claims further specifying which co-administered compound is used and adding µM concentration range/bound constraints for administration.
Stated Advantages
Lower side effects.
Rapid clinical application.
Documented Applications
Repositioning-based identification and virtual screening of SARS-CoV-2 Mpro or RdRP binders, followed by cellular efficacy testing in Vero and Calu-3 cells, to support preventing or treating COVID-19.
Prevention or treatment of coronavirus disease 2019 (COVID-19) in a subject in need thereof using tipifarnib with one or more compounds selected from omipalisib, blonanserin, emodin, and remdesivir.
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