A lot of very interesting drug discovery campaigns have already been published online this year. A summary of some of the resulting small molecules that I found most interesting appears below, including several clinical candidates and many fit-for-purpose biological tool compounds to assess efficacy and toxicity. Grab a coffee and use this post as a …
This post briefly introduces chimeric molecules and companies working on them, contains a list of 10 recent “hot” papers in this field, and some predictions for where chimeras might head. It’s Chinese New Year time, which means a significant part of the global biopharma supply chain has ground to a halt, due to our colleagues …
2019 was another big year for novel drug approvals (48 in total) though it wasn’t the record year of 2018 (with 59). The overall explosion in biologic drugs / non-small molecule modalities continued with year with 14 novel biologic drugs, including 3 monoclonal antibodies, a recombinant fusion protein (Reblozyl), 3 ADCs, an siRNA drug (Givlaari), …
2019 was another big year for drug discovery, with 29 FDA novel drug approvals for small molecules[note]Including istradefylline which was first approved in Japan, but not including brilliant blue G, fluorodopa F18, Ga-68-DOTATOC, bremelanotide, afamelanotide, and ferric maltol, which could all be considered small molecules by some definitions: https://www.fda.gov/drugs/new-drugs-fda-cders-new-molecular-entities-and-new-therapeutic-biological-products/novel-drug-approvals-2019[/note] and 3 for antibody-drug-conjugates so far.[note]The …
We all knew process scientists were good, but the Merck and Codexis teams just took it to another level! Unnatural nucleosides like Merck’s reverse transcriptase inhibitor islatravir (1, Figure 1) are well-known to be challenging to synthesize by traditional methods, as evidenced by several published chemical syntheses of this molecule requiring a dozen steps or …
Merck/Codexis Magic: Biocatalytic Synthesis of Islatravir Read More »
You’ve probably lived this story before: you’re working on your favorite kinase, YFK1, and are looking for selective inhibitors over YFK2. The problem is, they’re virtually identical near the active site, save for a single residue sitting in the back pocket that your amazing structural biologist has identified. The team thinks you have a better …
Kinase Inhibitor Types Predicted with Machine-Learning Read More »