February’s molecule, the Novartis factor B inhibitor LNP023 , targets the serine protease factor B (FB), a key node in the complement system. The complement part of the innate immune system is a hot area for drug discovery due to its increasingly recognized role in a wide range of chronic human diseases, including age-related macular [...]

February’s molecule, the Novartis factor B inhibitor LNP023 , targets the serine protease factor B (FB), a key node in the complement system. The complement part of the innate immune system is a hot area for drug discovery due to its increasingly recognized role in a wide range of chronic human diseases, including age-related macular [...]

Looking at the pipelines of recent biotech IPOs is a great way to get a snapshot of new technologies and approaches to drug discovery or to see what’s coming in smaller indications. Complementing our recent highlight of large molecule-focused companies, below is a summary of 2020’s class of biotech IPOs focused on small molecule drug [...]

In August's edition of Small Molecules of the Month, we have several fascinating molecules including a tri-complex KRAS-ON inhibitor from Revolution Medicines, a targeted protein stabilizer from a Berkeley/Novartis collaboration, and an RNA-modifying enzyme inhibitor from Storm/Cambridge....

We asked the global drug discovery community to vote on their favorite molecule from 2020, and the results are in. The community’s 2020 choice for Small Molecule of the Year is GS-6207 (lenacapavir), the awe-inspiring HIV capsid inhibitor published by Gilead Sciences in a 2020 issue of Nature.

Browsing through the pipelines of recent biotech IPOs is great way to catch up on emerging targets, novel drug modalities, and science at the edge of development. Unlike conferences and publications which tend to be a lagging indicator of what’s going on in industry (with many publications only being released years after a program has ceased [...]

While biologic drugs currently dominate in immunology by sales , small molecule immunomodulators (SMIMs) are making a comeback fueled by better understanding of intracellular signaling pathways and new hit finding technologies. SMIMs can be grouped into two categories: those that engage large molecule (LM) targets in a new [...]

Afternote: We're pleased to see Dan Erlanson made it as a finalist in the awards and Amgen's sotorasib won " Product of the Year ." Well deserved! Thanks to our readers for voting. Which drug hunters are making the greatest scientific contributions to drug discovery R&D? Our non-profit partner, California Life Sciences , is currently taking [...]

July’s edition of Small Molecules of the Month, features a selective monovalent estrogen receptor degrader in Ph. III, a remarkable 4(!) neurology clinical candidates from Takeda (including 2 recently licensed by Takeda to Neurocrine, TAK-653 and TAK-041), several oncology clinical candidates including two sulfoximines, and a small molecule that degrades its target via its own ubiquitination. Thanks to our featured reviewers for their feedback, with special thanks to neuroscience reviewer Jake Schwarz for feedback and commentary on an unusual 5 neuroscience molecules this month....

On Jun. 23 rd at 11AM PST, Dewakar Sangaraju and Dennis Hu gave a PBSS/CLSA webinar titled “Highlights from 2020’s FDA New Drug Approvals,” organized by Cyrus Khojasteh and Shichang Miao . One interesting fact about each approved small molecule drug was shared, along with statistics and specific case studies from the cohort of interest to the [...]

June’s edition of Small Molecules of the Month features a natural product-derived RNA splicing modulator, a mTORC1-selective “bi-steric” inhibitor, numerous low-dose clinical candidates and several unusual chemical motfs (e.g. pyridine N-oxide, sulfinylamine, boronic acid)....

There was a hilarious set of memes circulating the internet on scientific papers thanks to xkcd.com’s original comic . Here’s our drug discovery scientist’s parody. Since people expressed an interest in being able to find this again, here it is: Explore drughunter.com for more on drug discovery.

In May’s edition of Small Molecules of the Month, we have several fascinating molecules including a mutant PI3Kα degrader in Ph. III (GDC-0077, inavolisib), a wild-type CFTR potentiator for COPD, and a Ph. III chemotherapeutic derived from an aerospace compound....

There were 15 novel large molecule drugs approved in 2020, an increase over the 12 large molecule drugs approved in 2019 . Here’s a visual list of the FDA’s 2020 large molecule drug approvals , with more scientific details and references below. There is no significance to the order in which molecules are presented. This summary is intended [...]

In April’s edition of Small Molecules of the Month, we have several fascinating molecules including a tri-complex KRAS-ON inhibitor from Revolution Medicines, a targeted protein stabilizer from a Berkeley/Novartis collaboration, and an RNA-modifying enzyme inhibitor from Storm/Cambridge....

The March 2021 edition of Drug Hunter‘s Small Molecules of the Month series contains several small molecule clinical candidates as well as pre-clinical small molecules with interesting structures or mechanisms. Among the highlights are LSN3318839, a molecular glue that binds both GLP-1R receptor its endogenous GLP peptide, a P-gp inhibitor intended to induce a drug-drug interaction (DDI), and two non-traditional zinc binders including a hydantoin and a phosphinic acid. There are numerous chemistry rule-breakers here, including an oral brain penetrant compound with 5 rings, a compound with a pr...

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 of drug [...]

February was a packed month for interesting molecules – there were nearly 20 molecules we thought about including in this list but couldn’t fit them all. There are several clinical candidates this month including mobocertinib, an exon 20 mutant inhibitor that was recently given Breakthrough Therapy Designation by the FDA. Also included are several interesting modes of action here including two degraders, multiple protein dimerizers, and a mechanism-based inhibitor that modifies its target’s substrate. Finally, chemists will appreciate some interesting structures on this list as well as the fem...