Lessons learnt from the preclinical discovery and development of ensitrelvir as a COVID-19 therapeutic option

Tixagevimab + cilgavimab against SARS-CoV-2: the preclinical and clinical development and real-world evidence

(2023) Irma Convertino et al.   Expert Opinion on Drug Discovery

Development of Highly Potent Noncovalent Inhibitors of SARS-CoV-2 3CLpro

(2023) Ningke Hou et al.   ACS Central Science

Novel Investigational Anti-SARS-CoV-2 Agent Ensitrelvir “S-217622”: A Very Promising Potential Universal Broad-Spectrum Antiviral at the Therapeutic Frontline of Coronavirus Species

(2023) Wafa A. Eltayb et al.   ACS Omega

Evaluation of Drug‐Drug Interactions of Ensitrelvir, a SARS‐CoV‐2 3CL Protease Inhibitor, With Transporter Substrates Based on In Vitro and Clinical Studies

(2023) Ryosuke Shimizu et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Transmissible SARS-CoV-2 variants with resistance to clinical protease inhibitors

(2023) Seyed Arad Moghadasi et al.   Science Advances

Global prevalence of SARS-CoV-2 3CL protease mutations associated with nirmatrelvir or ensitrelvir resistance

(2023) Jonathan Daniel Ip et al.   EBioMedicine

Naturally Occurring Mutations of SARS-CoV-2 Main Protease Confer Drug Resistance to Nirmatrelvir

(2023) Yanmei Hu et al.   ACS Central Science

Nirmatrelvir Plus Ritonavir: First Approval

(2022) Yvette N. Lamb   DRUGS

Preclinical discovery and development of the casirivimab + imdevimab cocktail for the treatment of novel coronavirus infection: the rise and fall

(2022) Marco Tuccori et al.   Expert Opinion on Drug Discovery

Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19

(2022) Yuto Unoh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of ensitrelvir against SARS-CoV-2 in a delayed-treatment mouse model

(2022) Haruaki Nobori et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Monoclonal antibody therapies against SARS-CoV-2

(2022) Daniele Focosi et al.   LANCET INFECTIOUS DISEASES

A Randomized Phase 2/3 Study of Ensitrelvir, a Novel Oral SARS-CoV-2 3C-Like Protease Inhibitor, in Japanese Patients with Mild-to-Moderate COVID-19 or Asymptomatic SARS-CoV-2 Infection: Results of the Phase 2a Part

(2022) Hiroshi Mukae et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Safety, Tolerability, and Pharmacokinetics of the Novel Antiviral Agent Ensitrelvir Fumaric Acid, a SARS-CoV-2 3CL Protease Inhibitor, in Healthy Adults

(2022) Ryosuke Shimizu et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

S-217622, a SARS-CoV-2 main protease inhibitor, decreases viral load and ameliorates COVID-19 severity in hamsters

(2022) Michihito Sasaki et al.   Science Translational Medicine

Efficacy and Safety of Ensitrelvir in Patients With Mild-to-Moderate Coronavirus Disease 2019 (COVID-19): The Phase 2b Part of a Randomized, Placebo-Controlled, Phase 2/3 Study

(2022) Hiroshi Mukae et al.   CLINICAL INFECTIOUS DISEASES

Ensitrelvir as a potential treatment for COVID-19

(2022) Matthew W. McCarthy   EXPERT OPINION ON PHARMACOTHERAPY

Multiple pathways for SARS-CoV-2 resistance to nirmatrelvir

(2022) Sho Iketani et al.   NATURE

Potency, Safety, and Pharmacokinetic Profiles of Potential Inhibitors Targeting SARS-CoV-2 Main Protease

(2021) Hylemariam Mihiretie Mengist et al.   Frontiers in Pharmacology

Potent Noncovalent Inhibitors of the Main Protease of SARS-CoV-2 from Molecular Sculpting of the Drug Perampanel Guided by Free Energy Perturbation Calculations

(2021) Chun-Hui Zhang et al.   ACS Central Science

Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors

(2021) Naoya Kitamura et al.   JOURNAL OF MEDICINAL CHEMISTRY

An overview of the preclinical discovery and development of bamlanivimab for the treatment of novel coronavirus infection (COVID-19): reasons for limited clinical use and lessons for the future

(2021) Marco Tuccori et al.   Expert Opinion on Drug Discovery

The SARS-CoV-2 main protease as drug target

(2020) Sven Ullrich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Crystallographic structure of wild-type SARS-CoV-2 main protease acyl-enzyme intermediate with physiological C-terminal autoprocessing site

(2020) Jaeyong Lee et al.   Nature Communications

Proteases and protease inhibitors in infectious diseases

(2017) Ayodeji A. Agbowuro et al.   MEDICINAL RESEARCH REVIEWS

Darunavir/cobicistat for the treatment of HIV-1: a new era for compact drugs with high genetic barrier to resistance

(2015) Amedeo Capetti et al.   EXPERT OPINION ON PHARMACOTHERAPY