This section contains case studies, industry highlights, minireviews, and other articles for drug discovery professionals.
RECENT DRUG HUNTER ORIGINAL ARTICLES
How Does This Thing Get in the Brain??
At AAPS 2022, I hosted a symposium where Ovoca Bio plc’s Head of Research, Mikhail Lomonosov told us about orenetide. Orenetide is an internationally approved peptide drug for hypoactive sexual desire disorder (HSDD) (think Viagra for women). It appears to work within a few weeks in humans with a solid safety profile – Mikhail noted…
2021 First-in-Class Large Molecule Drug Approvals (Pt. III)
This deep dive into 2021’s first-in-class large molecule drug approvals is the third in a series of focus articles on 2021’s novel large molecule drugs. See part one here, and part two here. For each of the 11 first-in-class large molecule drug approvals of 2021 (excluding vaccines), we’ll explore in more detail: how they work…
Production-Scale Synthesis of gem-Dimethylcyclopropylproline
The gem-dimethylcyclopropyl group is a key element in drugs, candidates, and agrochemicals, with a recent example being nirmatrelvir, the active ingredient in the Pfizer COVID-19 drug, Paxlovid. Here, we review synthetic strategies used to produce the key gem-dimethylcyclopropylproline intermediate, which may now be required in hundred-ton quantities to support nirmatrelvir manufacturing. Synthesis Spotlight: The gem-Dimethylcyclopropyl…
FDA Novel Drug Approvals: April 2022
There were two novel small molecules approved in April 2022: mavacamten (Camzyos), an oral cardiac myosin inhibitor oteseconazole (Vivjoy), an oral antifungal (jump to section) This deep dive explores each drug in more detail, including the industry context, the clinical data, the target rationale, mechanisms of action, and drug origins.
Drug Hunter Letters #2: On Carboxylic Acids and Acylglucuronides
Recently, Dr. Alf Claesson (CEO of Awametox AB, inventor of SpotRM, and previously Principal Scientist and Section Head at AstraZeneca/Astra AB, Sweden) reached out about our resource on the bioactivation of structural alerts. Dr. Claesson shared the helpful notes that: carboxylic acids forming thioesters with CoA might be a greater danger than those forming acyl…
Letters from Drug Hunters #1 – Apr. 2022
One of the privileges that have come with building Drug Hunter has been all the insightful thoughts and commentary our readers share. We also appreciate how readers help catch mistakes and offer corrections. This new series of “Drug Hunter Letters” highlights recent insightful communications from drug hunters, which includes this time: Dr. Nick Carruthers on…