A fat-tissue-targeting clinical candidate, a first-in-class Ph. III molecule that inhibits its target by covalently modifying the target’s substrate, and a fourth-generation glucokinase activator are some examples in Drug Hunter’s May 2022 edition of Molecules of the Month. In this month’s slide deck, you’ll find a molecule that had mitigated QTc prolongation over a prior molecule while hERG inhibition stayed constant, why reversible MAGL inhibition is being pursued, and much more, including:

• Industry context behind the molecules, target, and clinical applications

• Biological rationale for drugging the targets

• Mechanisms of action for the drugs

• Hit-finding and lead optimization strategies and tactics used

• Highlights from the binding modes and PDB codes where relevant

• Interesting aspects from the preclinical and clinical pharmacology

• Relevant patents and company history

Thanks to reviewers Ron Li, Julien Lefranc, Bryan McKibben, and Romyr Dominique for their nominations and commentary this month.