In June, we saw several FDA approvals for treatments targeting primary biliary cholangitis and COPD. The industry witnessed multibillion- and multimillion-dollar deals across various therapeutic areas. Advances were made in obesity therapeutics, with novel targets and clinical readouts for GLP-1 agonists and NLRP3 inhibitors. Alkermes and Takeda reported results for OX2R agonists in narcolepsy, while an antimalarial drug showed promise in PCOS. Despite these advancements, there were clinical trial failures for key molecules. Here's a recap of the most notable news highlights from June 2024!

To help you quickly scan the patent literature, we’ve distilled down thousands of new documents into a searchable table of over 200 selected patents focused on key areas in drug discovery, all published in May 2024. This resource is enriched with detailed highlights on selected molecules targeting high-interest areas such as STING antagonists, WIZ degraders, RNA degraders, and macrocyclic amine-based OX2R modulators.

To select May’s Molecules of the Month, our team evaluated hundreds of molecules from thousands of papers, press releases, conference presentations, and other materials. Check out our curated roundup of more than 60 additional molecules below that caught our interest from May, including highlights of some of our favorites, and perspectives on why these are molecules to watch.

In May 2024, several significant transactions worth millions and billions of dollars took place to advance next-generation neuroplastogens, KRAS G12C inhibitors, Pompe disease treatments, and molecular glues. We also highlight positive clinical readouts for hot targets such as tetrameric transthyretin (TTR) stabilizers, Hedgehog pathway inhibitors, plasma kallikrein inhibitors, dipeptidyl peptidase 1 (DPP-1) inhibitors, and PCSK9 inhibitors. Here's a recap of the most notable news highlights from May 2024!

To select April’s Molecules of the Month, our team evaluated hundreds of molecules from thousands of papers, press releases, conference presentations, and other materials. Here we’ve curated a roundup of more than 60 additional molecules that caught our interest from April, along with highlights we found most notable.

In April 2024, patent disclosures continued to highlight the swift progress in targeting key therapeutic areas. The Drug Hunter team has carefully compiled a searchable database containing over 200 patents relevant to drug discovery. This resource is enhanced with detailed annotations and highlights some of the most promising molecules and targets, such as GPR84 antagonists, brain-penetrant TYK2 inhibitors, and tricyclic urea JAK2 V617F inhibitors, among others. This compilation serves as a valuable tool for drug hunters to stay abreast of the latest trends in drug discovery.

In April 2024, there were promising examples of drug repurposing, significant clinical and regulatory milestones for therapies aimed at rare and pediatric diseases, the initiation of a rolling NDA submission for suzetrigine, substantial billion-dollar acquisitions, and positive trial results were reported for both a D1/D5 receptor agonist and a PARP1 inhibitor. However, the industry also had setbacks as demonstrated by the failed clinical trials for an MNK inhibitor and an NMDA receptor modulator. In case you missed anything, here’s a recap of the most notable news highlights from April 2024!

Throughout each month, the Drug Hunter team evaluates hundreds of molecules found in thousands of papers, press releases, conference presentations, and other materials to pick contenders for Molecules of the Month. Here, we curated a roundup of nearly 70 additional molecules that caught our interest from March 2024, including highlights from some of our favorites.

In March 2024, the landscape of patent disclosures continued to reflect the rapid pace of advances against key therapeutic targets. The Drug Hunter team has curated a searchable database encompassing over 200 patents pertinent to the field of drug discovery. This resource is further enriched with insightful spotlight on some of the most promising molecules and targets, including OX2R agonists, TEAD covalent inhibitors, NaV1.8 inhibitors, and selective PI3Kγ inhibitors, among others. This round-up provides a valuable tool for drug hunters to navigate the most recent trends in drug discovery.

Companies inked notable high-profile transactions in March 2024, including AbbVie's purchase of Landos Biopharma for $137.5M, AstraZeneca's $2.4B acquisition of Fusion Pharmaceuticals, and its subsequent deal to buy Amolyt for up to $1.05B. The FDA approved the first treatment for MASH. In parallel, expectations are high for the approval of Xcovery's ALK inhibitor, ensartinib. Praxis made headlines with PRAX-628, a next-generation oral NaV modulator, which showed anti-seizure efficacy in a Ph. IIa trial. Read below for more details on these and other drug discovery news stories from March 2024

February 2024 saw numerous notable patent disclosures aimed at a variety of therapeutic targets across different disease areas. The Drug Hunter team has compiled a searchable table that includes more than 200 patents of relevance to the drug discovery industry. Accompanying the table are detailed notes, as well as standout features from some of our top picks, including MTA-cooperative PRMT5 inhibitors, heterobifunctional TYK2 degraders, strategies for engaging and reactivating mutant p53, and more.

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >60 additional molecules that were of interest in February 2024 along with some highlights from some of our favorites below.

February 2024 was filled with notable scientific achievements and partnerships. Gilead and Novartis inked billion-dollar acquisitions, and Novo Nordisk and NeoMorph agreed to a $1.46B deal to discover molecular glue degraders. Additionally, Vertex introduced a promising new treatment for cystic fibrosis that is potentially superior to Trikafta. Takeda also made strides by advancing their OX2R agonist TAK-861, for treating narcolepsy type 1, into Ph. III clinical trials. Read this news roundup for more details on these and other drug discovery news stories that you may have missed from Feb 2024

From WRN helicase to KRAS G12V, there were numerous hot targets of interest with patent applications published in January 2024. Here, we curated a searchable table comprising key information for more than 200 patents from January 2024 of potential interest to drug hunters, along with highlights from some of our favorites, including several degraders and molecules targeting Nrf2, KRAS G12V, MAGL, WRN, among others.

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >70 additional molecules that were of interest in January 2024 along with highlights from some of our favorites, including molecules targeting SOS1, NLRP3, SMARCA2, and more.

Among the small molecule highlights in January’s news were a $100M+ Series A for a PARP1 + PI3Kα-focused company, clinical data with an SLC inhibitor for PKU, a 5-HT2C superagonist for seizures, and a NK1,3 dual antagonist for women’s health. A novel anti-obesity agent from phenotypic screening also made headlines, and the close of a major acquisition may bring relief to the industry. You can read about these notable scientific highlights and more below.

The Drug Hunter team is piloting a new series highlighting notable disclosures in the patent literature to provide our readers a timely and scientifically flavorful synopsis of therapeutic targets being actively pursued, emerging industry breakthroughs, and fascinating chemical matter. Here we highlight 12 patents published in December 2023 that piqued our interest, and compiled a searchable table comprising key information from more than 180 additional patents of potential interest to drug hunters. If you have any suggestions on how to make this more useful, please let us know!

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >60 additional molecules that were of interest in December 2023 along with highlights from some of the team’s favorites in the article.

There were several key clinical readouts in Dec. 2023 for small molecules in areas ranging from non-opioid pain management to sickle cell disease. While most results were positive, one pivotal trial led to a program discontinuation. This roundup highlights key data recently reported for selected molecules targeting NaV1.8, BTK, and more.

2023 was an incredible year in drug discovery. Drug Hunter featured many remarkable case studies last year including campaigns on challenging targets like KRAS, programs employing emerging modalities like degraders or oral macrocyclic peptides, and compounds with fascinating properties like allostery and mutant-selectivity. In case you missed these stories, here are the top 12 most popular Drug Hunter case studies published in 2023.

Drug Hunter regularly reviews trends and topics of industry interest, from hot new molecules from conferences to recently notable targets and technologies. Here are ten of the most popular reviews accessed on Drug Hunter in 2023.

An aldosterone synthase inhibitor, a pFOX inhibitor, a brain-penetrant MEK1/2 inhibitor, and several other modulators had major trial results disclosed recently. In case you missed them, this article rounds up key results of general industry interest, with representative patent structures for undisclosed molecules. Read this review to get a sneak peek at potential future approvals, as well as some informative disappointments.

Last November saw several notable updates for molecules we previously covered on Drug Hunter. These updates ranged from positive Ph. III results and NDA submission to failed clinical trials and discontinuation, for TTR, FXIa, GLP-1R modulators, and more. In case you missed it, this article is a round-up of these clinical updates from Nov. ’23.

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >70 additional molecules that were of interest in November 2023 along with some highlights from some of our favorites below.

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Here we have compiled a table of >70 additional molecules that were of interest in October 2023 but we did not have space for in MOTM. A few highlights are also discussed, including Novartis’s Werner helicase (WRN) inhibitor, APJ agonist AMG985 molecular glue degrader golcadomide, and more in the full article.

The team reviews hundreds of compounds from thousands of papers, press releases, and other sources each month to select candidates for Molecules of the Month. Based on requests from readers to see more molecules, this article contains a table of >40 additional molecules that were of interest last month but not included in MOTM, with a few highlights including off-target toxicity seen in a KRAS(G12D) program and hits on challenging target classes.

To help drug discovery professionals get the most out of your trip to ACS San Francisco 2023, we compiled a table of sessions that are likely to be of high interest to industry scientists here.

This article compiles recent high-profile clinical readouts and related news with small molecules of general interest and structures where they are available. Targets and indications discussed in this article include BTK for MS, Axl, TYRO3, and Mer for oncology, HIF prolyl-hydroxylase in anemia, ET/AT in nephrology, a JAK2 inhibitor for myelofibrosis, and THR-beta in NASH. [...]

Test This article compiles 20+ recent small molecules of general interest in the news in April 2023, with structures where they are available. Capacity Bio’s MAS Receptor Agonists with $35M Raised for FIH Clinical Trials MAS modulator from WO2022165189 example 107 New start-up Capacity Bio backed by RA Capital, Insight Partners, and Remiges [...]

We couldn’t include everything in Molecules of the Month, but here’s a round-up of up of 16 additional molecules of potential interest that we didn’t have space for in April, including a highly selective caspase inhibitor from a non-catalytic cysteine, a GPR40 AgoPAM from BMS with activity on GLP-1, a few examples of both on- and off-target [...]

There were plenty of scientific highlights from the literature that we didn’t have space for in Molecules of the Month - here’s a reader’s digest rounding up ~20 molecules of potential interest that we didn’t have space to highlight, including Pfizer’s covalent heterobifunctional BTK degrader, BMS' brain-penetrant GSK-3β inhibitor, the [...]

Keep up with the latest updates on past Molecules of the Month! From a Ph. III oral HIF-PH inhibitor receiving a favorable response from the EMA to an oral mutant IDH1/2 inhibitor with FIC potential having favorable Ph. III results for hard-to-treat brain tumors, read more about the recent updates in the full article! Want updates like this [...]

This article highlights some recent million-dollar molecules, including: Gilead's exclusively licensed preclinical, oral IRAK4 degrader from Nurix Biohaven's exclusively licensed oral, brain-penetrant, dual TYK2/JAK1 inhibitor from Highlightll Pharmaceutical Eli Lilly's acquisition of a Ph. I oral AT 2 R inhibitor from Confo Therapeutics Read [...]

This article discusses scientifically interesting molecules that have unfortunately had negative recent readouts. Aptinyx’s therapeutic approach of targeting positive allosteric modulators (PAMs) of NMDA receptors has hit another setback in Ph. II for NYX-458. The oral, twice-daily MK2 inhibitor from Aclaris Therapeutics has results from its [...]

The AACR 2023 first disclosures presented in the Chemistry in Cancer Research’s “New Drugs on the Horizon” sessions are always fascinating. This article contains the structures of all of the novel small molecule first disclosures presented at AACR in the session, along with notes on their significance, and another molecule disclosed in the [...]

Merck’s oral PCSK9 inhibitor is a surprisingly bioavailable and orally effective macrocyclic peptide with picomolar activity. It recently demonstrated significant LDL cholesterol reduction in Ph. IIb, paving the way for it to enter Ph. III later this year. Roche’s oral, SMN2-directed RNA splicing modifier and first molecule of its kind to be [...]

The First Disclosures section of the 2023 ACS Spring Meeting in Indianapolis, organized by GSK’s Nikki Goodwin , covers three novel small molecules and an ADC this year. The molecules include: MK-0616, Merck’s macrocyclic oral PCSK9 inhibitor (presented by Abbas Walji ) NX-2127, Nurix’s oral BTK degrader (presented by Jeff Wu ) BI 1015550 [...]

While the Molecules of the Month are being selected and our deep dive reviews are being prepared, you can find early highlights from our team’s journal club from February 2023. Check out AstraZeneca’s preclinical SERD, Merck’s Ph. I c-KIT inhibitor, University of Michigan’s STAT5 PROTAC degrader, and more snippets to jumpstart your reading [...]

Here’s a preview of two molecules acquired in January 2023 among 14 mentioned in this article: deuruxolitinib (CTP-543) This molecule, a deuterated version of JAK1/2 inhibitor ruxolitinib (Opzelura, Incyte), has received Breakthrough Therapy designation from the FDA and is being acquired by Sun Pharma via Concert in a $0.576B transaction [...]

Two past Molecules of the Month inductees had significant updates recently, showing they’re still moving forward: upacicalcet This September ‘22 Molecule of the Month is an IV calcium-sensing receptor (CaSR) agonist first identified in flavor studies of peptides. It is already approved in Japan for secondary hyperparathyroidism (SHPT), and [...]

Our latest roundup of small molecules in the news includes three molecules moving into development for the first time: MRTX1133 Mirati’s reversible, long-acting KRASG12D inhibitor, and December ‘21 Molecule of the Month, is going into the clinic as an oral compound. While initial disclosures referred to its potential as an IV agent, Mirati [...]

In this update of small molecules in the news we will cover recent: (B/M)illion-Dollar Molecules: recent M&A’s, IPOs, and other fundraising Molecules in Motion: clinical trial updates and FDA filings Where Are They Now? updates on past Drug Hunter Molecules of the Month Potential Upcoming Approvals : recent NDA filings and upcoming PDUFA [...]

You’ve read about the top 10 molecules with publications from July, but what about the ones we found interesting that didn’t make it into Molecules of the Month? There were six runners-up this month, including a selective covalent K-Ras(G12S) inhibitor with a butyrolactone warhead, a κ opioid receptor agonist, and a dinucleotide STING agonist [...]

This year’s EFMC-ISMC conference in Nice, France, had a fantastic collection of talks. Among the highlights were the two First Disclosure sections, where companies shared the structures of their latest clinical candidates for the first time. Many thanks to Dr. Julien Lefranc , one of our featured reviewers , for sharing his notes on these [...]

We're here at ACS Chicago 2022, covering sections of particular interest to drug discovery scientists. Among the highlights are the First Disclosures sections, where companies are sharing structures of clinical candidates for the first time. We'll go more in-depth into the science from the conference soon - for now, here's a high-level [...]

Readers have been asking for more molecules, so we started a new feature that highlights 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 available ALK2 inhibitor and a direct AMPK activator for X-linked adrenoleukodystrophy. You can read more about all [...]

There’s so many interesting new publications that don’t necessarily feature key molecules, but are helpful for drug hunters to know about. Here are some other interesting reviews, technology, and targets to watch from April and May: April 2022 Best Practices : Understanding PK-PD for Protein Degraders: A Review . Derek Bartlett and Adam [...]

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 [...]

One of the privileges that have come with building Drug Hunter has been all the insightful thoughts and commentary our readers share. We also appreciate how readers help catch mistakes and offer corrections. This new series of “ Drug Hunter Letters” highlights recent insightful communications from drug hunters, which includes this time: Dr [...]

There were six small molecule candidates disclosed on Apr. 10th at AACR New Orleans 2022 at the New Drugs on the Horizon session, with another four on Apr. 11th. The New Drugs on the Horizon session is organized by the Chemistry in Cancer Research (CICR) Working Group , this year chaired by Joachim Rudolph . Thanks to reviewer Julien Lefranc [...]

The FDA approved five novel small molecule drugs in neurology in 2021. Addressing a range of conditions from ADHD to relapsing MS, the 2021 neurology drug approvals are: atogepant (Qulipta): calcitonin gene-related peptide (CGRP) receptor antagonist ponsimod (Ponvory): selective sphingosine-1-phosphate (S1P) receptor 1 (S1PR1) modulator [...]

Dear Drug Hunter, It's gotten harder and harder to keep up with everything that's going on in the industry. From new company launches to drug approvals, endless publications to regulatory updates, the volume of information drug discovery leaders need to make good decisions seems endless. Our mission is to save you time by curating industry [...]

The first disclosures of new drug candidates are always the highlight of medicinal chemistry conferences. Six novel drug candidates were recently disclosed by European companies at the European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry (EFMC-ISMC) Conference in [...]

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 [...]

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 bonds proposed by Sutor are [...]

Scientists from GlaxoSmithKline’s Stevenage site have an excellent article in J. Med. Chem. showing that cyclopropyl pyran (CPP) groups can serve as viable isosteres to N-pyrimidyl morpholines thanks in part to favorable cyclopropane σ -> aryl π interactions. N -aryl morpholines are privileged motifs in drug discovery, and suitable [...]