PF-07817883 (Ibuzatrelvir): A Second-Generation SARS-CoV-2 Main Protease Inhibitor with Improved Metabolic Stability
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The 2021 New Drug Approvals for Infectious Diseases: Deep Dive
The FDA in 2021 approved four novel small molecule drugs for various infectious diseases, including human immunodeficiency virus type-1 (HIV-1), post-transplant cytomegalovirus (CMV), vulvovaginal candidiasis, and human African trypanosomiasis (HAT; sleeping sickness). This article and slide deck explores each in more detail, including but [...]
The Covalent Drug Comeback
Whereas covalent drugs were once considered risky for indications other than cancer due to the potential for idiosyncratic drug-induced liver injury and other toxicities, concerns appear to have softened as an increasing number of non-oncology covalent inhibitor programs have achieved successful outcomes. Here we highlight several recent anecdotes in covalent inhibitor drug discovery that seem to reflect these changing attitudes, including billion-dollar acquisitions and approvals outside oncology, and a few modern examples that showcase the increasingly rich science in this area.
Vonoprazan, Tapinarof, and Tirzepatide: FDA Novel Drug Approvals in May 2022
There were two novel small molecules approved in May 2022: vonoprazan (Voquezna) : a potassium-competitive acid blocker (PCAB) tapinarof (Vtama) : an aryl hydrocarbon receptor (AhR) agonist And one novel large molecule approval: tirzepatide (Mounjaro) : a glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 [...]
Nirmatrelvir: 2021 Small Molecule of the Year
We asked the global drug discovery community to nominate and vote on their favorite molecule from 2021, and the results are in. The 2021 choice for Drug Hunter’s Small Molecule of the Year is Pfizer’s CoV-2 M pro Inhibitor, PF-07321332 (nirmatrelvir, Paxlovid) . Published in a November 2021 Science article , the molecule was praised for its [...]
Recent Highlights in Covalent Drug Discovery
In Wednesday’s Flash Talk webinar, we covered recent highlights in covalent drug discovery, with lots of great questions from the audience. The webinar and recording are available below to everyone thanks to our sponsor, Revvity Signals, and the slides are available for download to Premium members at the bottom.