Researchers find COVID-19 Txs more effective than remdesivir

Korean researchers at KAIST found treatments for COVID-19 that is more effective than remdesivir

Antiviral activity found in 7 out of 38 drugs…omipalisib has higher effect

A Korean research team of the Korea Advanced Institute of Science and Technology (KAIST) discovered new drug candidates for the treatment of COVID-19.

 

Some of the candidates are expected to have a better effect than the currently approved remdesivir (product name: Veklury).

 

On the 8th, the joint research team of Sang-yup Lee, Distinguished Professor of Chemical & Biomolecular Engineering at KAIST, and Dr.

 

Seung-taek Kim, researcher of Institut Pasteur Korea (IPK)’s Zoonotic Virus Laboratory announced that they have discovered potential candidates for treating COVID-19 using their virtual screening technology.

 

The team opted for a drug repurposing strategy using virtual screening.

 

In other words, the team sought to find substances that may help treat COVID-19 among drugs with verified efficacy and safety.

 

The researchers first built a virtual library on 6,218 drugs that are FDA-approved or in clinical trials, and then applied their newly developed virtual screening technology.

 

The accuracy of the system was improved by adding structural similarity and interaction similarity analysis modules to the existing docking simulation-based virtual screening technology.

 

Summary of the COVID-19 treatment development process using virtual drug screening technology (source: KAIST)

Using the platform, the team selected 38 candidate compounds that inhibit the protease and RNA-dependent RNA polymerase needed for the replication and proliferation of the COVID-19 virus.

 

Then, the efficacy of the candidates was verified by the Institut Pasteur Korea.

 

Testing was conducted using a monkey’s kidney cells infected with COVID-19.

 

Of the 38 candidates, 7 compounds showed antiviral activity.

 

The 7 compounds that showed promise were further verified on human lung cells to be narrowed down to three: omipalisib, and tipifarnib, and emodin.

 

Among these, omipalisib was found to have an antiviral activity that is over 200 times higher than that of remdesivir.

 

Antiviral activity of tipifarnib was found to be similar to remdesivir.

 

Omipalisib is currently being studied in a clinical trial as a treatment for cancer and pulmonary fibrosis.

 

Tipifarnib is being studied in a clinical as a treatment for and progeria, and emodin, which is derived from plants, is being studied in a clinical trial as an anticancer drug.

 

The research team is planning a preclinical trial on these 3 candidate substances.

 

In the preclinical trial, the team aims to minimize toxicity and reach the effective concentration for treating COVID-19.

 

Regarding the findings, Professor Sang-yup Lee said, ”With the research, we were able to prepare a base technology to promptly respond to new emerging viruses.

 

We will continue our research to develop technologies applicable to new infectious viruses as well as variants of the coronavirus.”