Author: Laura Riva; Shuofeng Yuan; Xin Yin; Laura Martin-Sancho; Naoko Matsunaga; Sebastian Burgstaller-Muehlbacher; Lars Pache; Paul P. De Jesus; Mitchell V. Hull; Max Chang; Jasper Fuk-Woo Chan; Jianli Cao; Vincent Kwok-Man Poon; Kristina Herbert; Tu-Trinh Nguyen; Yuan Pu; Courtney Nguyen; Andrey Rubanov; Luis Martinez-Sobrido; Wen-Chun Liu; Lisa Miorin; Kris M. White; Jeffrey R. Johnson; Christopher Benner; Ren Sun; Peter G. Schultz; Andrew Su; Adolfo Garcia-Sastre; Arnab K. Chatterjee; Kwok-Yung Yuen; Sumit K. Chanda
Title: A Large-scale Drug Repositioning Survey for SARS-CoV-2 Antivirals Document date: 2020_4_17
ID: 1fgnfh62_68
Snippet: These data indicate that therapeutic dosing of apilimod in patients can achieve concentrations that are likely to promote antiviral activity. Apilimod has been evaluated in phase II clinical trials for the treatment of active Crohn's disease and rheumatoid arthritis (RA) 86 , and in additional phase II trials for the oral treatment of common variable immunodeficiency (CVID), but did not show efficacy for these indications 85, 87 . In 2019, orphan.....
Document: These data indicate that therapeutic dosing of apilimod in patients can achieve concentrations that are likely to promote antiviral activity. Apilimod has been evaluated in phase II clinical trials for the treatment of active Crohn's disease and rheumatoid arthritis (RA) 86 , and in additional phase II trials for the oral treatment of common variable immunodeficiency (CVID), but did not show efficacy for these indications 85, 87 . In 2019, orphan drug designation was granted to apilimod in the U.S. for the treatment of follicular lymphoma 88 , with phase I clinical trials ongoing. Notably, it has been reported that apilimod efficiently inhibits EBOV, Lassa virus (LASV), and Marburg virus (MARV) in human cell lines, underscoring its potential broad-spectrum antiviral activity 44, 89 . The underlying mechanism for the inhibition of SARS-CoV-2 infection by apilimod is currently not known. However, since PIKfyve predominately resides in early endosomes and plays an essential role in maintenance of endomembrane homeostasis, apilimod likely blocks viral low pH-dependent entry through inhibition of the lipid kinase activity of PIKfyve.
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