'Remdesivir 200 Times More Effective' Therapeutic Discovered... Gamechanger Emerges (Comprehensive)

KAIST-Pasteur Institute Develops 'Virtual Drug Screening' Technology for Drug Repurposing

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[Asia Economy Reporter Kim Bong-su] Domestic researchers have devised a new method and, for the first time in the world, identified candidate therapeutic substances effective against the COVID-19 virus from thousands of existing drugs.

These candidates are 200 times more effective than the U.S. drug Remdesivir (Veklury), are already in use as medications making regulatory approval simpler, and are administered orally, making them much more convenient to take. If officially approved after clinical trials, they are expected to become a 'game changer' in COVID-19 treatment.

The Korea Advanced Institute of Science and Technology (KAIST) announced on the 8th that a joint research team led by Distinguished Professor Lee Sang-yeop of the Department of Bio and Chemical Engineering succeeded in developing COVID-19 therapeutics using virtual drug screening technology. The team collected FDA-approved drugs or drugs in clinical trials from databases to build a virtual library of 6,218 drugs and quickly screened only those with potential as antiviral agents. They also developed an algorithm that automatically generates the active form structures of nucleotide analogue-based prodrugs, which are mainly used as antiviral agents.

The research team identified 28 candidate compounds, confirmed antiviral effects in 7 of these drugs, and through additional validation experiments discovered COVID-19 treatment effects in 3 substances: Omipalisib, currently in clinical trials for cancer and idiopathic pulmonary fibrosis; Tipifarnib, in clinical trials for cancer and progeria; and Emodin, a plant extract undergoing clinical trials as an anticancer agent.

Among these, Omipalisib showed antiviral activity approximately 200 times higher than Remdesivir, the current standard COVID-19 treatment. Tipifarnib also demonstrated antiviral activity comparable to Remdesivir. However, animal testing of one of these drugs revealed toxicity, prompting further preclinical trials for all three drugs. The research team plans to find the optimal drug concentration that minimizes toxicity while achieving therapeutic efficacy.

If the substances discovered by the research team receive official approval, they are expected to become 'game changers' in COVID-19 treatment, surpassing Remdesivir, which has limitations. Despite FDA approval, Remdesivir has disappointed by failing to reduce mortality and only shortening recovery time by about five days. Additionally, it is administered intravenously, requiring hospitalization for several days. In contrast, the drugs discovered by the team are already in use and are oral medications, making approval, production, prescription, supply, and administration much simpler.

This research was published online on the 7th in the international academic journal 'Proceedings of the National Academy of Sciences (PNAS)'.

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