Context. TXA6101 (TAXIS Pharmaceuticals) is a filamentous temperature-sensitive mutant Z (FtsZ) protein inhibitor being developed for targeting gram-negative bacteria. Drug resistance continues to be a paramount challenge in antibiotic therapy and there is an ongoing need to explore and develop novel antibacterial drugs. FtsZ has long been [...]

Context. RLX-33 (Research Triangle Institute) is a nonpeptide relaxin-3/RXFP3 system antagonist . Evidence over the last 2 decades, since the discovery of relaxin‐3 in 2001 , suggests that the protein, through its receptor RXFP3, regulates responses to stress, anxiety-related and motivated behaviors, circadian rhythms, learning and memory [...]

Context. INCB13739 (Incyte) is an oral 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) antagonist . Inhibition of the tissue-specific generation of cortisol using agents that antagonize 11β-HSD1, the key metabolic enzyme involved in the conversion of inactive glucocorticoids to active ones, has been considered a desirable therapeutic strategy [...]

Context. “compound 4e” (Chiesi Farmaceutici) is an inhaled p38α/β mitogen-activated protein kinase (MAPK) inhibitor being developed for lung inflammatory diseases . As a regulator of key proinflammatory mediators, p38 MAPK has been extensively explored as a therapeutic target for inflammatory diseases, including those of the lung. However [...]

Context. MAGLi 432 (Roche) is a novel, reversible monoacylglycerol lipase (MAGL) inhibitor . There has been increasing interest in the role of inflammation and blood-brain barrier dysfunction in neurology. The appeal of MAGL as an anti-neuroinflammatory therapeutic target comes from its hallmark role as the enzyme that links the [...]

Dorzagliatin (Hua Medicine) is an oral dual-acting full glucokinase (GK) activator being developed for type 2 diabetes . More than 50 years since the first report of the role of GK in glucose metabolism, no agents targeting this enzyme have been approved, although not for lack of trying. We recently covered a partial GK activator [...]

Our first South San Francisco Drug Hunter event was so much fun, we've decided to host in-person events all over the world. The next few events will be networking mixers, but stay tuned for scientific symposia and conferences! Sign up here to get invites to future in-person events around the world, including in Boston, Basel, San Diego [...]

Readers have been asking for more molecules, so this month, we’re starting a new feature that will highlight a few of the molecules we liked that didn’t make it into Molecules of the Month. There were six runners-up this month, including an orally bioavailable, brain penetrant inhibitor of PAAN/MIF, and a STING agonist discovered using [...]

Our team conducted a review of all of the biotech mergers and acquisitions of 2021 and distilled it down to the acquisitions of drug discovery-focused biotechs here. There were 10 acquisitions of companies with large molecule drug assets in 2021. Here is a more in-depth look into all of the lead large molecules acquired in 2021, including a [...]

There were 16 acquisitions of companies with small molecule drug assets in 2021 and one merger. Here is a more in-depth look into all of the lead small molecules acquired in 2021, including a review of: The lead molecules in each acquisition and their structural representations where disclosed The mechanism of action, stage, and indication of [...]

There were two novel small molecules approved in May 2022: vonoprazan (Voquezna) : a potassium-competitive acid blocker (PCAB) tapinarof (Vtama) : an aryl hydrocarbon receptor (AhR) agonist And one novel large molecule approval: tirzepatide (Mounjaro) : a glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-like peptide-1 [...]

This article is Part 2 of a review series covering all of the initial public offerings for the biotech and pharmaceutical industries in 2021. Part 1(link to article) provided an overview of 2021 IPOs by therapy area, technology, and therapeutic class. This short article takes a deeper look into the 2021 IPOs by technology and therapeutic [...]

In 2021, the FDA approved two new drugs for endocrinology-related indications, including severe hypoglycemia in diabetes, and chronic kidney disease (CKD) associated with type 2 diabetes. This article and slide deck explores each in more detail, including but not limited to their: target rationale discovery disease context original patents [...]

We did a comprehensive review of all the initial public offerings for the biotech and pharmaceutical industry in 2021. This article is Part 1 in a review series about companies focused on drug discovery that IPO’d during this time. You can find recent years’ IPOs summarized here: 2020 Small Molecule IPOs 2020 Large Molecule IPOs 2019 Small [...]

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 article [...]

In 2021 the FDA approved four new drugs for various immunological diseases, including a molecular glue, the first drug approved for AAV in a decade, and a ROCK kinase inhibitor originally investigated for cancer. This article and slide deck explores each in more detail, including but not limited to their: mechanisms of action target rationale [...]

A SETD2 inhibitor with Fast Track Status for hematological malignancies, a CNS-penetrating, ATP-competitive LRRK2 inhibitor for Parkinson’s disease, and an oral nonsteroidal mineralocorticoid receptor antagonist are some examples of this month's MOTM. In the slide deck, you'll find a small molecule that modulates a protein that has only been targeted with antibodies so far and a drug that takes advantage of the glutamate NMDA receptor hypofunction hypothesis. Check out the ten molecule minireviews in the slide deck, which covers: Where are all of the Molecules of the Month in clinical developm...

Thank you to all of the drug hunters who attended our second drug discovery webinar! You can find the video and slides at the bottom of this page. In part II of this series we covered: Emerging startups, growing drug discovery companies, and IPOs Clinical readouts, positive and negative Big deals and major regulatory actions Check out part [...]