Antiviral Drugs - SARS-CoV-2
From the work of Dr John Campbell - UK
- Pfizer develops new antiviral, PF-07321332, C₂₃H₃₂F₃N₅O₄ PF-07321332 designed to block the activity of the SARS-CoV-2-3CL protease,
(PFIZER’S NOVEL COVID-19 ORAL ANTIVIRAL TREATMENT CANDIDATE REDUCED RISK OF HOSPITALIZATION OR DEATH BY 89% IN INTERIM ANALYSIS OF PHASE 2/3 EPIC-HR STUDY)
"Pfizer is committed to working toward equitable access to PAXLOVID™ for all people, aiming to deliver safe and effective antiviral therapeutics as soon as possible and at an affordable price. If our candidate is successful, during the pandemic, Pfizer will offer our investigational oral antiviral therapy through a tiered pricing approach based on the income level of each country to promote equity of access across the globe. High and upper-middle income countries will pay more than lower income countries. The company has entered into advance purchase agreements with multiple countries and is in negotiations with several others. Pfizer has also begun and will continue to invest up to approximately $1 billion to support the manufacturing and distribution of this investigational treatment, including exploring potential contract manufacturing options to help ensure access across low- and middle-income countries, pending regulatory authorization."
"The company is working to ensure access for its novel antiviral candidate for those most in need around the world, pending successful trial results and regulatory approval."
- Chymotrypsin-like protease (3CL main protease, or 3CL Mpro) explained:
Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-Throughput Screening
"The outbreak of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has emphasized the urgency to develop effective therapeutics. Drug repurposing screening is regarded as one of the most practical and rapid approaches for the discovery of such therapeutics. The 3C-like protease (3CLpro), or main protease (Mpro) of SARS-CoV-2 is a valid drug target as it is a specific viral enzyme and plays an essential role in viral replication. We performed a quantitative high-throughput screening (qHTS) of 10 755 compounds consisting of approved and investigational drugs, and bioactive compounds using a SARS-CoV-2 3CLpro assay. Twenty-three small molecule inhibitors of SARS-CoV-2 3CLpro have been identified with IC50s ranging from 0.26 to 28.85 μM. Walrycin B (IC50 = 0.26 μM), hydroxocobalamin (IC50 = 3.29 μM), suramin sodium (IC50 = 6.5 μM), Z-DEVD-FMK (IC50 = 6.81 μM), LLL-12 (IC50 = 9.84 μM), and Z-FA-FMK (IC50 = 11.39 μM) are the most potent 3CLpro inhibitors. The activity of the anti-SARS-CoV-2 viral infection was confirmed in 7 of 23 compounds using a SARS-CoV-2 cytopathic effect assay. The results demonstrated a set of SARS-CoV-2 3CLpro inhibitors that may have potential for further clinical evaluation as part of drug combination therapies to treating COVID-19 patients and as starting points for chemistry optimization for new drug development."
- Identification of potential candidates for 3CLPro inhibition
Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents
"We have identified that boceprevir, micafungin, ombitasvir, paritaprevir, and tipranavir exhibited partial inhibitory effect, whereas ivermectin was able to completely inhibit the SARS-COV-2 3CLpro enzymatic activity in vitro at the tested doses."
Here is the original video - 'fact-checked' by the government and big pharma - therefore hidden somewhere in this post in order to escape the FB censorship.