The two studies were conducted in collaboration with the Italian National Institute for the Infectious Diseases "Lazzaro Spallanzani" in Rome and other important clinical and preclinical research groups highly committed to COVID-19 research.
"The clinical results on raloxifene published on Lancet's eClinical Medicine show a significant virological impact in term of negative nasopharyngeal swab at day 7 in COVID-19 patients treated at home with raloxifene compared to standard of care.
This randomized clinical trial confirm the in vitro data published in Nature's Cell Death and Disease, on the efficacy of Raloxifene on cellular lines experimentally infected by SARS-CoV-2" said Emanuele Nicastri, author of both studies and Director of the Infectious and Tropical Diseases Unit of the Spallanzani Institute in Rome, where Italy's very first Covid-19 patients were hospitalized.
A virtual working environment: Exscalate platform is capable of evaluating more than three million molecules per second drawing on a “chemical library†of trillion molecules.
Raloxifene was identified by the Exscalate4CoV (E4C) project, a group composed of 30 public and private institutions from seven countries and funded by EU Commission's in the frame of its Horizon 2020 Framework Programme, aimed at fighting Coronavirus with the latest European supercomputing resources and experimental facilities.
Due to its processing capacity of more than 3 million molecules per second, Exscalate is currently the most powerful intelligent supercomputing drug design platform. This processing power allowed the E4C researchers to rapidly select and repurpose a generic molecule with known efficacy and tolerability to make it available to the global community.
As raloxifene is a generic molecule already tested and approved for the treatment of osteoporosis, this was a not for profit effort aimed at providing a globally available low cost treatment.
The first study on raloxifene, published in The Lancet's eClinical Medicine, demonstrated that after seven days of treatment, patients taking raloxifene showed an improvement in symptoms compared to patients receiving placebo.
The second study, published in Cell Death and Disease), indicates raloxifene as a potential agent to treat mild-to-moderate COVID-19 caused by the most common SARS-CoV-2 variants. Mechanistic studies confirmed the significant affinity of raloxifene for the Spike protein, as predicted by in silico studies.
Researchers concluded that raloxifene is efficacious against the main SARS-CoV-2 variants and could represent a useful addition to the therapeutic arm for the management of Covid-19. ■