Metabolite Tales Blog

JANUARY 23, 2024

Metabolism of 2023 FDA Approved Small Molecules – PART 1 By Julia Shanu-Wilson 2023 was a fruitful year for drug approvals by the FDA, with a crop of 34 small molecules out of a total of 55 new drugs [1]. References [1] 2023 Novel Small Molecule FDA Drug Approvals. 2] Iversen et al., 131(5): 311- 324.

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Codon

FEBRUARY 13, 2025

Computational Design To design a new serine hydrolase enzyme, Baker’s team turned to RFDiffusion , a protein design tool developed in their lab in 2022. The enzyme must not only bind substrates correctly but also maintain stability through each transformation while handling intermediate products without inhibition.

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The Strateos Blog: Drug Discovery

MARCH 18, 2022

Strateos had the pleasure of participating at the PharmaIQ Live: Smartlab Digital 2022 conference held between March 8-9th, which focused on the potential of Lab 4.0 strategies to increase the speed, efficiency and reduce the cost of the drug discovery process. John Harman, Sr.

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Atomwise Blog

MARCH 9, 2022

Learn what our Atoms have been working on below and visit Atomwise at ACS Spring 2022 National Meeting for other presentation sessions. At the American Chemical Society Spring National Meeting & Expo, Atomwise members were selected to present their research and work.

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Drug Target Review

OCTOBER 11, 2023

Autophagy boosters, in contrast, are conventional small molecule drugs. Small molecules have been the mainstay of the pharmaceutical industry for nearly a century, they are easy to deliver – they are often given orally – and our health systems have a lot of experience of working with them. cited 2023 Sep 5].

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Drug Target Review

JULY 6, 2023

1 TPD is expected to challenge undruggable proteins, which are highly difficult to target by conventional small molecules. 1 The concept of TPD was first demonstrated with a heterobifunctional small molecule to degrader a protein of interest in the early 2000s. Nature Publishing Group; 2022 [cited 2023Feb23].

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NIH Director's Blog: Drug Development

OCTOBER 11, 2022

Those numbers include the news late last week that the 2022 Nobel Prize in Chemistry was shared by two long-time grantees for their work on a transformative scientific approach known as “click chemistry.” 6] Small molecule inhibitors of mucin-type O-glycosylation from a uridine-based library. Science 2008, 320 (5876), 664–667.

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Drug Target Review

APRIL 7, 2025

Advancements in screening technologies for small-molecule drug discovery including cellular assays, computational screening, and biophysics-based methods enhanced by structural biology breakthroughs have improved screening hit rates and facilitated the identification of drug candidates for previously undruggable targets. 2022.02.002.

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The Strateos Blog: Drug Discovery

DECEMBER 13, 2021

We are excited to share that Strateos’ SVP of Strategy & Operations, Daniel Sipes, will be delivering a presentation entitled Accelerating Medicinal Chemistry Cycle Times Through Cloud-Accessible Smart Automated Labs at the upcoming 2022 Society for Laboratory Automation and Screening Conference & Exhibition between February 5-9th.

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DrugBaron

FEBRUARY 7, 2022

Finding small molecule drugs is much harder than finding a needle in a haystack – discovering the right arrangement of atoms to bind precisely to a protein target to elicit a particular response is a problem of vast dimensionality. Yet the situation with small molecules is even worse.

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KIF1A

JUNE 30, 2023

As families, scientists, doctors and our friends around the world navigated the challenges of 2022, the KIF1A.ORG community worked together to reach new heights. Over 162 new families from around the world joined our community since January 2022. What a year! As this community grows, so does our army of advocates and supporters.

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Drug Target Review

JULY 13, 2023

They found that although the targets themselves may not be easily druggable due to their disordered nature, their ability to condense can be modulated using small molecules. By focusing on molecules that modulate the condensate formation, they identified tractable chemical matter that specifically impacted the target of interest.

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Drug Target Review

OCTOBER 4, 2023

Groundbreaking strategies like proteolysis-targeting chimeric molecules (PROTACs) are also being explored. 6 Combining the effect of payloads with different mechanisms of action – an approach that revolutionised small molecule chemotherapy – also holds the promise of enhanced therapeutic activity for ADCs. 51 , 3886–3897 (2022).

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LifeSciVC

JANUARY 16, 2024

By Aimee Raleigh, Principal at Atlas Venture, as part of the From The Trenches feature of LifeSciVC Just in time for new years’ reflections and resolutions, this year’s JPM felt like a refreshing burst of enthusiasm for a sector that has seen its challenges in 2022 and 2023 but also some green shoots. Small molecule GLP1s?

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Drug Target Review

NOVEMBER 6, 2023

These regimens frequently include one or two small molecule inhibitors and immuno-oncology (IO) therapies, such as monoclonal antibodies and T-cell engagers. Published 2022 Apr 27. Cancer Treatment Reviews , (2022);106:102395. Cancers (Basel). 2022;14(9):2182. doi:10.3390/cancers14092182 Fisher R, et al. Br J Cancer.

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Drug Target Review

SEPTEMBER 25, 2024

Applying our technology has enabled us to develop a new small molecule, TT125-802, and to assign a new role to the epigenetic regulator CBP/p300 as a novel master regulator of non-oncogene resistance. This orally available small molecule binds to the bromodomain of CBP/p300 in a highly specific manner. References 1.Jin

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Drug Target Review

OCTOBER 23, 2024

Technologies for the rapid and efficient testing of small molecules and biologics have greatly accelerated drug discovery. Intermediate-sized molecules such as macrocycles combining the beneficial properties of both small molecules and biologics may enable the targeting of currently undruggable targets.

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Drug Target Review

JUNE 19, 2024

Transplanting cells could prove to be more beneficial than treating a particular condition with a small molecule or an antibody, and that really speaks to the power of cell therapy. Just like small molecules and antibodies, cell therapies are changing how we treat patients. from May 2017 until December 2022.

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Drug Target Review

MARCH 28, 2024

Between 2000 and 2020, approximately 30 percent of the newly introduced small molecule drugs were derived from natural products. 1 Surprisingly, however, less than one percent of the natural world’s chemical composition has been identified or studied by scientists. Journal of Natural Products. 2020;83(3):770–803. 9b01285 Young, R.J.,

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The Pharma Data

FEBRUARY 24, 2022

They then developed a new therapeutic approach with a potent small-molecule inhibitor of this enzyme. “We are amazed by the efficiency of small-molecule PROTAC in simultaneously targeting EZH2 and cMyc in cancer cells.” Nat Cell Biol, 2022. Their findings are published online in Nature Cell Biology.

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New Drug Approvals

SEPTEMBER 29, 2024

link] 01 Aug 2022 Cortexyme is now called Quince Therapeutics You need to be a logged in or subscribed to view this content This small molecule is an orally available protease inhibitor targeting the lysine proteases of the periodontal pathogen Porphyromonas gingivalis. Results were expected in May 2022.

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Conversations in Drug Development Trends

MAY 30, 2024

Initial approval in 2022: FDA, U.S. Other researchers are investigating approaches that use AAV-mediated trophic support and antibody-based therapies, such as vaccines and small molecule drugs, to modify various protein expressions. Dosing & Treatment Regimen: 105mg (5 mL) taken in the morning after overnight fasting.

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The Strateos Blog: Drug Discovery

JULY 26, 2022

On May 24, 2022, 20/15 Visioneers hosted a webinar on the topic of implementing cloud lab automation featuring Strateos’ own John Harman, Senior Director of Product Management, and Nicholas Firth, CEO of Evariste Technologies.

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Practical Cheminformatics

JANUARY 8, 2024

The ML model can predict the remaining molecules' free energies and prioritize the next set of free energy calculations. By repeating this process several times, many of the most promising molecules can be identified by evaluating a small fraction of a larger dataset.

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New Drug Approvals

SEPTEMBER 10, 2024

g/mol 1929519-13-0 NBI-1065846 or TAK-041 Phase 2 (S)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide Zelatriazin ( NBI-1065846 or TAK-041 ) is a small-molecule agonist of GPR139. Tauscher, Johannes (June 2022). Hauber, Wolfgang; von Heimendahl, Moritz (August 2022). 15305. .;

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The Premier Consulting Blog

JANUARY 31, 2023

On November 1, 2022, the U.S. Of note, this guidance is specific to small molecule pharmaceuticals; similar guidance for biologics can be found in the ICH’s S6(R1) Preclinical Safety Evaluation for Biotechnology-Derived Pharmaceuticals. Source: ICH S1B(R1), August 2022. 2022 Jan;35(1):53-73. J Toxicol Pathol.

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New Drug Approvals

JANUARY 3, 2023

Adagrasib Formula C32H35ClFN7O2 cas 2326521-71-3 Mol weight 604.1174 Antineoplastic Disease Non-small cell lung cancer 2022/12/12 FDA APPROVED, KRAZATI (Mirati Therapeutics) MRTX-849 MRTX849 KRAS G12C inhibitor MRTX849 Adagrasib , sold under the brand name Krazati , is an anticancer medication used to treat non-small cell lung cancer. [1]

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New Drug Approvals

JANUARY 31, 2024

amcrasto@amcrasto ////////// /////////// References ^ Pognan, François; Buono, Chiara; Couttet, Philippe; Galarneau, Jean-René; Timsit, Yoav; Wolf, Armin (29 October 2022). “Liver enzyme delayed clearance in rat treated by CSF1 receptor specific antagonist Sotuletinib” Current Research in Toxicology. 3 : 100091.

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The Pharma Data

MARCH 13, 2022

Arena has previously indicated that it expected the results of the Phase 3 ELEVATE-UC trial of etrasimod in ulcerative colitis during the first quarter of 2022. In connection with the acquisition, Arena’s shares of common stock will be delisted from the Nasdaq Global Select Market on or about March 11, 2022.

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Drug Target Review

DECEMBER 7, 2023

Specific RNA structure The scientists and their collaborators from Sean Brady’s Laboratory of Genetically Encoded Small Molecules focused on the CBASS system in Staphylococcus schleiferi , a bacterium often located in the mouth of dogs and cats. 2022 September 17 [2023 November 21]; 15(2022):4155-68. But what, exactly?”

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The Pharma Data

MAY 16, 2022

AbbVie (NYSE: ABBV) today announced that 27 abstracts across its gastroenterology portfolio will be presented at the Digestive Disease Week (DDW) Annual Meeting, May 21-24, 2022, in San Diego and virtually. A database with all AbbVie abstracts accepted for presentation at DDW 2022 can be found here.

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DrugBank

AUGUST 15, 2024

In 2022 alone, global sales of Repatha reached $1.28 This first-in-class reversible small molecule inhibitor targets specific mutations in the EGFR and HER2 genes, which are known to drive tumor growth in several types of cancer. This partnership proved to be a financial benefit for both parties.

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Drug Target Review

DECEMBER 13, 2024

Typically, these combinations include an immune checkpoint inhibitor (CPI; eg, anti-programmed cell death protein 1 [PD-1] / programmed cell death ligand 1 [PD-L1]) combined with other components such as chemotherapy, a targeted small molecule drug, novel CPIs, or ADCs. Non-small cell lung cancer: current treatment and future advances.

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Drug Target Review

MAY 23, 2023

Micro- and macroalgae from both marine and fresh water produce small molecules and secondary metabolites with aggregative, anti-inflammatory, antioxidant, antimicrobial, anti-viral and anti-tumoural bioactivities. Examples include phlorotannins from brown seaweeds and small molecules like terpenoids and peptides, found in microalgae.

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The Pharma Data

MAY 15, 2023

Through the acquisition, Gilead gains rights to a portfolio of small molecule inhibitors targeting PARP1 for oncology and MK2 for inflammatory diseases that could enter clinical trials later this year. Beginning in the first quarter of 2022, consistent with recent industry communications from the U.S. Qing Dong, Ph.D.,

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The Pharma Data

MARCH 18, 2022

cash dividend per Sanofi share, this additional extraordinary dividend, exclusively in kind, is subject to shareholders approval at Sanofi’s May 3, 2022 Ordinary and Extraordinary Shareholders’ Meeting. In addition to the previously proposed €3.33

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The Pharma Data

JUNE 22, 2023

in December 2022 about changes to their initial 2017 partnership whereby Daiichi Sankyo obtained the Marketing Authorization for Yescarta ®. .–(BUSINESS WIRE)– Kite Pharma, Inc., to Gilead Sciences K.K., the Japan subsidiary of Gilead Sciences, Inc. This follows the announcement made by Daiichi Sankyo and Kite Pharma, Inc.

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