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a new Italian incubator dedicated to the discovery and development of smallmolecule-based treatments for neurodegenerative diseases, announced today that it has adopted Collaborative Drug Discovery’s CDD Vault as its platform of choice for managing drug discovery data.
Table 1: Smallmolecule drugs approved by the FDA in 2023 with reported involvement of phase II mechanisms In vitro : In vivo differences Incubation of the SGLT2 (sodium-glucose co-transporter-2) inhibitor bexagliflozin in human liver microsomes points to metabolism through both oxidation and glucuronidation to 6 main metabolites.
Metabolism of 2022 FDA approved smallmolecule drugs – Part 1 Does CYP3A4 still rule? By Julia Shanu-Wilson It won’t come as much surprise to learn that of the 17 smallmolecules* approved by the FDA in 2022, CYP3A4 was the major player in drug metabolism. References Iversen et al., Front Pharmacol.,
Metabolism of 2022 FDA approved smallmolecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the smallmolecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Dermavant’s tapinarof is one such friend. 8 This is not the only point of interest.
Metabolism of 2023 FDA Approved SmallMolecules – PART 1 By Julia Shanu-Wilson 2023 was a fruitful year for drug approvals by the FDA, with a crop of 34 smallmolecules out of a total of 55 new drugs [1]. References [1] 2023 Novel SmallMolecule FDA Drug Approvals.
The bulk of my nearly three decades of experience up to that point was with drugging protein targets using a variety of modalities, but principally smallmolecules. The post Reinventing the smallmolecule toolbox: from proteins to RNA appeared first on Arrakis Therapeutics. As ever, we proceed fearlessly forward.
A few years ago, at Arrakis Therapeutics, we set out to conquer a strange new territory, drugging RNA structures with smallmolecules. Dramatic discoveries of smallmolecules targeting SMN2 Prior to those outstanding therapeutic achievements, in 2015, a group from Novartis published an important paper in Nature Chemical Biology.
By training PLACER on structures stored in the Protein Data Bank, the team taught the model to predict atom arrangements that follow the physical and chemical rules governing protein-smallmolecule interactions. He also writes on a blog focused on the intersection of biology and AI at owlposting.com.
originally developed the ELISA assay to measure antibody levels, scientists have since adapted it for a host of different proteins and smallmolecules from a variety of sample types (Engvall 1971). An enzyme-linked immunosorbent assay (ELISA) is a versatile method used to quantify the level of target antigen in a sample.
At the American Chemical Society Spring National Meeting & Expo, Atomwise members were selected to present their research and work. Learn what our Atoms have been working on below and visit Atomwise at ACS Spring 2022 National Meeting for other presentation sessions.
The series, held virtually on Tuesday and Thursday afternoons on ACI’s interactive platform, will provide an in-depth review of Hatch-Waxman and the BPCIA, as well as other intellectual property basics related to smallmolecules and biologics. FDA Law Blog readers receive a 10% discount (use FDA Law Blog promo code: D10-999-FDA25).
In the case of urgent or immediate public interest, process validation may be conducted concurrently with manufacturing the commercial smallmolecule or biologic product to expedite product availability for patients.
Now comes word of another absolutely incredible use of cryo-EM: determining with great ease and exquisite precision the structure of the smaller organic chemical compounds, or “smallmolecules,” that play such key roles in biological exploration and drug development. Also analyzed were eight less-familiar smallmolecules.
We want to mark this progress with some updates and perspectives in the Dark Matter blog. Our terra firma is small-molecule medicines. As we know, smallmolecules have been the mainstay of our pharmacopeia for several centuries and have, almost without exception, targeted proteins.
Last week’s guidance is featured on FDA’s new nitrosamines webpage and recommends that manufacturers implement revisions to control measures by August 1, 2025, noting that manufacturers and sponsors of approved products were expected to complete evaluations for smallmolecule nitrosamines last year.
FDA Law Blog readers receive a 10% discount off the tuition fee (promo code D10-999-FDA25 ). Karst will moderate a panel discussion, titled “Fireside Chat on the Future of the FDA: Regulatory Initiatives, and Agency Developments for Hatch Waxman Practitioners to Watch.” You can register for the conference here.
This series will provide an in-depth review of Hatch-Waxman and the BPCIA along with other IP basics relative to smallmolecules and biologics. Save 10% with the FDA Law Blog promo code: D10-999-FDA24. To learn more visit here , or email at customerservice@americanconference.com.
and whether a molecule’s pharmacology can help to mitigate safety risk. Especially for oligo or smallmolecule discovery and development, it’s important to understand whether there are highly homologous sequences or proteins that may be impacted by a given therapeutic approach. based on “tool” molecule precedent.
Recent efforts have focused on the development of small-molecule inhibitors as an alternative approach to therapeutically target PD-1 or PD-L1. Compared with mAbs, smallmolecules can provide increased oral bioavailability, bio-efficiency, and shorter half-life activity.
My pulse will be quickenin' With each drop of strychnine We feed to a pigeon It just takes a smidgin To poison a pigeon in the park Tom Lehrer, Poisoning Pigeons in the Park | video ** Ill be reviewing the H2024 study (Occurrence of Natural Selection in Successful SmallMolecule Drug Discovery) in this post.
AlphaLISA assay technology can be used in smallmolecule discovery but can also be applied to large molecule discovery, including biologics, vaccines and cell-based therapies. The next focus for the team is to identify similar smallmolecules to the 25 hits they uncovered and then try to improve the potency of each.
The addition of Cisbio’s capabilities to PerkinElmer will enable life science researchers to have access to assay tools that address the broad diversity of target types and biological configurations, for both smallmolecule and biologic drug discovery. Learn more about Cisbio here.
In this blog, we take stock of progress, look at what’s in store for drug development, and give examples of ways microplate readers can help advance research into molecular glues. Conventional drug development has often focused on finding smallmolecules that fit the active site of a protein.
Other researchers are investigating approaches that use AAV-mediated trophic support and antibody-based therapies, such as vaccines and smallmolecule drugs, to modify various protein expressions. For a more in-depth discussion on challenges and solutions to ALS research, read our blog.
Since our company’s founding in 2015, we have taken the long view and been singularly focused on building an extremely flexible and broadly applicable platform that can develop a host of RNA‑targeted smallmolecules (rSMs) to deliver precision medicines for dozens of targets that have been out of reach for conventional approaches.
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.
Here are two predictions for the future: Alpha CETSA ® for target engagement While traditional assay methods detect either the displacement of a radioligand binding to the target by a competitor molecule, or the modulation of some function of the target, a new method is making headway: Cellular Thermo Shift Assay (CETSA) from Pelago Bioscience.
Effectors of signal transmission events Second messengers are smallmolecules or ions that transmit signals received at the cell surface to the inside environment of the cell (Fig.
The majority of smallmolecule drugs induce their therapeutic effects by seeking out and binding to their intended target while avoiding most other molecules in the dense milieu of the cell interior. Our overall mission at Arrakis is to expand the set of “druggable” targets for small-molecule medicines to include RNA.
My last stop at Arrakis Therapeutics is with a company targeting RNA with smallmolecules. I was enticed by Arrakis’ founder Jen Petter to serve in one more operational role, leading the research group at Arrakis as the company launched as one of the first biotechs to target RNA with drug-like smallmolecules.
These methods typically use a physics-based scoring function to generate ranked lists of plausible poses, which are models of physical interactions between smallmolecules and protein targets. They are often effective at suggesting good poses, but the best ones are typically not at the top of the list.
As part of a team, the successful applicant will undertake a variety of interesting projects to deliver purified smallmolecules to collaborators and for our own proprietary projects in the field of biotransformation and natural products drug discovery. The role is predominantly lab-based.
Researchers soon began screening a chemical library and its more than 380,000 traditional drug candidates to find the right small-molecule inhibitor, the preferred compound in drug discovery. Missing was the usual pocket-shaped active site, where a traditional smallmolecule can readily bind and block function.
N -glucuronidation: the human element By Julia Shanu-Wilson In our last blog of the year, we look at why N -glucuronidation of drugs is important in human drug metabolism. Conjugation of smallmolecule drugs to glucuronic acid is catalysed by several UGTs to frequently form N – and O -glucuronides. Derun Li, David L.
This blog will outline three characteristics of a successful nonclinical program to support entry into clinical trials for a cell or gene therapy product. Thus, while the same types of safety endpoints need to be evaluated, the studies done to do so often look different compared to those for a smallmolecule.
Gotta be SAFE: A New Framework for Molecular Design [link] A blog post by Edward Williams from Terray Therapeutics introduced Contrastive Optimization for Accelerated Therapeutic Inference (COATI). This novel embedding considers both the topological and three-dimensional structure of molecules. In this paper, the authors then used 1.1
The EnSight multimode plate reader offers best-in-class luminescence detection technology at high throughput rates (less than 1 min per 96-well plate) and can support biologics, vaccines, and smallmolecule research.
Or should I say back to retirement, as he was comfortably relaxing at home back in 2016 when Jen Petter lured him back into the fray with the siren call of developing a new class of RNA-targeted small-molecule medicines here at Arrakis. I won’t dwell on Jim’s many accomplishments here.
In this blog post, we outline typical elements of an IND-enabling package for a single ascending dose (SAD)/multiple ascending dose (MAD) study of an oral smallmolecule for a non-cancer indication with a maximum of 14 days of dosing.
In this blog, we will address common questions we receive from our clients and aspects to consider when designing those nonclinical studies. If the compound is not active in any species (eg, human-specific gene target), a surrogate molecule could be used. In which species should the toxicity study be conducted?
This blog post will explain how the WoE approach is used in toxicology studies and how the S1B(R1) addendum could affect your nonclinical program. Background The addendum’s development was informed by both prospective and retrospective evaluations of animal carcinogenicity data submitted to the ICH.
Scope Part 1— though the Act’s restrictions are seemingly limited to equipment and services that perform activities in relation to “biological materials”—a term that is not defined in the Act—the restrictions may still impact manufacturers of smallmolecule drugs or API that contract with third-parties using covered products or services as part of, (..)
OVERCOMING BOTTLENECKS IN TRADITIONAL WORKFLOWS Conventional smallmolecule drug discovery workflows take upwards of 6 years to progress from target ID through to IND submission with key medicinal chemistry (MedChem) steps involved in lead generation. Ben Miles, Ph.D.,
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