University of Minnesota Investigators: Apilimod 5X More Potent Against COVID-19 than Remdesivir in Cell Culture

Aug 15, 2020 | Apilimod, Coronavirus, COVID-19, News, Popular Posts, Preclinical Research

University of Minnesota Investigators: Apilimod 5X More Potent Against COVID-19 than Remdesivir in Cell Culture

Researchers led by Ricardo Battaglino, PhD, with the University of Minnesota Medical School, see significant promise for the anti-cancer drug apilimod. The university recently reported that early results show that apilimod is five times more effective in treating cell cultures with COVID-19 as compared to remdesivir. Will this benefit translate to clinical trials? In the power of science, Sanford Burnham Prebys Medical Discovery Institute identified apilimod as one of 21 drugs that could strongly act against SARS-CoV-2, the virus behind COVID-19.

The professor and vice-chair of research in the Department of Rehabilitation Medicine recently articulated the powerful findings, “That means that this drug is more specific.” Dr. Battaglino continued, “This comparison is something that we need to do because remdesivir is the current standard of care, and this drug needs to perform better than that or the same, in order to be considered a good therapeutic candidate.”

Background

The University of Minnesota team including Battaglino, Leslie Morse, DO, professor and head of the Department of Rehabilitation Medicine, and Vadim Gurvich, PhD, MBA, an associate professor in the College of Pharmacy commenced the apilimod research on COVID-19 back in March. They found that the drug had shown potential in treating viral infections, such as the Ebola virus. So the group applied for and received a CO:VID (Collaborative Outcomes: Visionary Innovation & Discovery) grant to kick-start their research, ultimately designing a 99% variety of apilimod.

Preclinical Study

The team, based on Vadim Gurvich’s network, found a team in Chicago where there is the ability to test various investigational therapies in animals. The Minnesota team moved quickly to capitalize on the facility. While collaborating on preclinical cell culture study, they found that the amount necessary of their “apilimod-like” therapy to block SARS-CoV-2 is one-fifth to one-tenth of what is needed when using remdesivir. 

After analyzing their findings, Dr. Battaglino suggests this therapy approach may be superior to that of remdesivir to treat patients with severe cases of COVID-19 and possibly prevent progression from mild to severe symptoms.

‘Cells in a Dish’ to Live Subjects

The team now needs to identify if this drug can make the transition from “cells in a dish” into live subjects that have COVID-19. They are applying for grants with the National Institutes of Health and the U.S. Department of Defense while also keeping close to the U.S. Food and Drug Administration. They are now on a mission to provide the safety and efficacy of their apilimod-like drug.

The Drug

Apilimod (STA-5326) is a drug that was finally identified as an inhibitor of the production of the interleukins IL-12 and IL-23 and developed for the oral treatment of autoimmune conditions such as Crohn’s disease and rheumatoid arthritis through clinical trial results disappointing, and development of these applications were halted.

Later on, however, scientists found that apilimod has an additional mode of action as an inhibitor of the lipid kinase enzyme PIKfyve. PIKfyve makes two lipids, PtdIns5P and PtdIns (3,5)P2, whose Administration of apilimod (100 nM; 60 min) in human embryonic kidney cells powerfully reduces levels of both PtdIns5P and PtdIns (3,5)P2.

More recently, apilimod was repurposed as a potential antiviral and anti-cancer drug, with possible applications in the treatment of non-Hodgkin lymphoma and viral diseases such as Ebola, Lassa fever, and COVID-19.

TrialSite recently reported that apilimod was identified as one of 21 drugs that identified as a potential weapon against COVID-19 based on the research of a group out of Sanford Burnham Prebys Medical Discovery Institute led by Sumit Chandra.

Lead Research/Investigator

Ricardo Battaglino, PhD, with the University of Minnesota Medical School

Leslie Morse, DO, professor and head of the Department of Rehabilitation Medicine

Vadim Gurvich, PhD, MBA, an associate professor in the College of Pharmacy

Call to Action: The team hopes to have clinical trials going by the Fall of 2020. Sign up for the TrialSite daily newsletter for updates.

3 Comments

  1. Paul Elkins

    Sounds very promising. However, Vero cells are not good models to SARS-COV-2 antiviral activity. They are derived from kidneys and lack TMPRSS2. A much better model is Calu3 cells which are derived from human epithelial cells. Calu3 cells express TMPRSS2 which is key to for SARS-COV-2 cell entry. Here us a good paper on the topic:

    https://www.nature.com/articles/s41586-020-2575-3

    Hopefully, apilimod will preserve its antiviral activity when tested in vitro against Calu3 (or lung organoids) and ultimately in vivo.

    • TrialSite

      Paul this is interesting points you raise. We will review this carefully.
      Thanks!
      Publisher

    • TrialSite

      Thank You Sir. It means a lot. We are planning on doing other investigational documentaries in other countries. Working on those now!
      Thanks for the visit–we appreciate your contribution to TrialSite Dr.Keizer.
      Regards, Publisher

Pin It on Pinterest