1. University of Virginia - https://med.virginia.edu/cell-biology/recent-publication/the-phosphatidylinositol-3-phosphate-5-kinase-inhibitor-apilimod-blocks-filoviral-entry-and-infection/

Reference for Mode of Action

Proven by its success in blocking infections by the Ebola virus, the mode of action for apilimod is an entry inhibitor. Apilimod is a phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) inhibitor and is, thus, able to prevent alternative splicing that would have been triggered by the PIKfyve protein kinase. By doing so, apilimod is able to block entry of foreign or infectious substances into the cytoplasm and, as a result, is considered to be a promising drug in treating filoviral infections.


University of California, Santa Cruz

Apilimod, also known as LAM-002A is an anti-cancer drug that is viewed to have high potential in effectively treating COVID-19.

In fact, Dr. Sumit Chanda, a lead investigator at the Sanford Burnham Prebys Medical Discovery Institute claims that apilimod is one of the top candidates to represent a treatment option for COVID-19. 


Apilimod as a Treatment for COVID-19

Dr. Ricardo Battaglino from the University of Minnesota claims that “that apilimod is five times more effective in treating cell cultures with COVID-19 compared to remdesivir.” Battaglino coordinated with a team in Chicago to develop their own version of apilimod that would be 99% pure and geared toward treating COVID-19. 

Researchers working with cells in culture found that the amount needed of their “apilomod-like” drug to successfully block the virus is one-fifth to one-tenth of what is currently needed when using remdesivir. The results of the study suggests that the drug may help treat patients with severe cases, while also being able to prevent the progression from mild to severe symptoms. Furthermore, with the inevitability of more coronavirus outbreaks in the future, Battaaglino believes that apilimod “is going to be effective against any coronavirus because the way it works is not specific to virus strain.”


Clinical Study: University of Minnesota (July 2020 Completion)

Yale University’s School of Medicine and AI Therapeutics, a biopharmaceutical company, have launched a multi-institutional clinical to test the safety and efficacy of using apilimod to reduce virus levels in infected individuals. While Yale will conduct the study, AI Therapeutics, founded by a Yale alumnus, will own intellectual property rights to the drug.

The study is expected to enroll 142 newly diagnosed patients. Murat Gonel, a Yale professor and an advisor at AI Therapeutics says, “LAM-002A holds promise to be a powerful new therapy for COVID-19 patients to prevent progression of disease, hopefully avoiding the need for hospitalization.” Gunel and others involved in the study are hopeful that apilimod will be able to prevent the development of COVID-19 after exposure, particularly among high-risk populations, such as the elderly community.
	


Clinical Study: Yale University & AI Therapeutics (2021 Completion)

Mode of Action

Apilimod’s properties come from its primary mechanism of action, which is its disruption of lysosomal function.

By inhibiting the lipid kinase PIKfyve, apilimod induces cell apoptosis and is, consequently, able to prevent the autophagy of foreign and infectious substances. In addition, PIKfyve inhibition results in the increase of endolysosomal organelles. Since PIKfyve is also a primary regulator of endosome activity, apilimod’s efficiency is further increased as endosomes are how many viruses actually deliver their genetic material into a host cell and are often the beginning of a viral infection.


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