Small Molecule of the Year – 2022
We asked the global drug discovery community to nominate and vote on their favorite molecule from 2022, and the results are in. The 2022 winner, with the most overall votes across the ten finalist molecules, is BMS’ oral, deuterated allosteric TYK2 inhibitor, deucravacitinib, the first new treatment for plaque psoriasis in nearly a decade. Here,…
Billion-Dollar Biotransformations: On the Metabolism of Ozanimod
Today, ozanimod is a likely megablockbuster drug approved for ulcerative colitis and multiple sclerosis. But before it became the first S1P modulator approved in ulcerative colitis, it received a scary, headline-making “Refuse to File” letter from the FDA due to insufficient preclinical characterization of an active metabolite RP112273 (CC112273). Addressing the refusal to file letter…
Ten Examples of Best-in-Class Drugs
It’s best to be first, but drugs that are approved later with the same mechanism of action can also create significant value for patients and society by being best-in-class (BIC), or what clinicians refer to as “gold standard.” Recently we highlighted key factors that can make a follow-on drug be considered a best-in-class drug. This…
Small Molecule of the Year – 2021
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 Mpro Inhibitor, PF-07321332 (nirmatrelvir, Paxlovid). Published in a November 2021 Science article, the molecule was praised for its impressive…
A Gram-Daily Aldehyde for Anemia: Voxelotor
On Feb. 16, 12:00PM PST, Dr. Mira Pochon, Staff Scientist and Head of Translational Biology at Global Blood Therapeutics, gave a PBSS/CLSA webinar on one of 2019’s drug approvals, voxelotor (GBT440). Mira has been with GBT since it’s early days in 2011. GBT’s chemistry team was led by their CSO Dr. Brian Metcalf, former head…
A Polarized C-H···O Interaction Against IRAK4
The C-H — O hydrogen bond is so well established in structural biology today, that it’s been overlooked that the C-H — O hydrogen bond was first proposed by a woman, June Sutor, in a 1960’s Nature article.[1] Hydrogen bonds were then assumed to be linear (A-H···A’ between 150-180º), and the C-H — O hydrogen…