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We asked the global drug discovery community to nominate and vote on their favorite molecule from 2022, and the results are in. The 2022 winner, with the most overall votes across the ten finalist molecules , is BMS’ oral, deuterated allosteric TYK2 inhibitor, deucravacitinib, the first new treatment for plaque psoriasis in nearly a decade.
At present, there are few studies on the drug resistance of mIDH1 inhibitors. Currently, the FDA has granted approval for the use of the smallmolecule inhibitor Ivosidenib (AG-120) in the treatment of IDH1-mutated AML and cholangiocarcinoma. Representative mIDH1 inhibitors and their binding modes were also discussed.
sPLA 2 inhibitors have been developed for the treatment of inflammatory and other conditions such as cardiovascular disease, arteriosclerosis and rheumatoid arthritis. The three-dimensional structures presented in this review have been published by various research groups and have been deposited in the Protein Data Bank.
We have integrated structural and quantitative proteomics with biochemical assays to decipher the mode of action of covalent USP30 inhibition by a smallmolecule containing a cyanopyrrolidine reactive group, USP30-I-1.
Dynasore and dyngo-4a, smallmolecules developed to inhibit the GTPase activity of classic dynamins DNM1, DNM2 and DNM3, but not mdivi-1, a specific inhibitor of DNM1L, protect corneal epithelial cells exposed to the oxidant tert-butyl hydroperoxide (tBHP).
In this article, Stephan Schann, Chief Scientific Officer at Domain Therapeutics , explains why this class of drug target is so useful despite the challenges they present. Despite this, the therapeutic potential of targeting most GPCRs remains untapped, as only 10 percent of GPCRs have been drugged.
A New Treatment Option for a Debilitating Joint Tumor TGCT is a rare, debilitating condition that primarily affects young and middle-aged adults, often striking individuals in their prime working years. Pimicotinib: A Promising CSF-1R Inhibitor Pimicotinib is an investigational smallmolecule developed by Abbisko Therapeutics Co.,
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. Oxidation of adagrasib occurs on the methylpyrrolidine group 4.
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]. Enzymes involved include CYP1A2, CYP2C8, CYP3A4, CYP4F2, and aldehyde oxidase (AOX).
Susceptibility or risk biomarkers can detect the likelihood of a patient developing a disease or medical condition, which is crucial for treatments that are most effective before the onset of symptoms. A biomarker is a measurable indicator of a biological process, disease state, or response to a treatment.
Supramolecular nanostructured based delivery systems are emerging as a meaningful approach in treatment of cancer, offering controlled drug release and improved therapeutic efficacy. Different SNs approaches and recent literature reviews on peptide delivery are also presented to the readers.
The data were revealed during an oral presentation (S137) at the 2025 European Hematology Association (EHA) Congress in Vienna, reflecting ongoing progress in developing new treatment options for patients battling this aggressive hematologic malignancy.
Loxo Oncology at Lilly, a research and development group of Eli Lilly and Company (NYSE: LLY), and Kumquat Biosciences today announced an exclusive collaboration focused on the discovery, development and commercialization of potential novel smallmolecules that stimulate tumor-specific immune responses.
These multifunctional smallmolecules are like tiny spies, hijacking the body’s natural protein degradation system to remove unwanted proteins. Similarly, PROTACs can target and degrade overexpressed proteins, offering a way to overcome drug resistance, a common issue in cancer treatment.
In the present study, we got the SIRT7 protein structure from Alpha Fold2 Database and performed structure-based virtual screening to develop specific SIRT7 inhibitors using the SIRT7 inhibitor 97,491 interaction mechanism. In our study, we demonstrated that targeting SIRT7 may offer novel therapeutic options for cancer treatment.
4 Another related and well described non-oncogene resistance mechanism is the histological transformation of EGFR-mutated non-small cell lung cancer (NSCLC) to small-cell lung cancer upon treatment with an EGFR inhibitor. This orally available smallmolecule binds to the bromodomain of CBP/p300 in a highly specific manner.
Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as a promising therapeutic target for the treatment of hyperlipidemia. In discovery of novel smallmolecules that interfere PCSK9/LDLR protein–protein interaction (PPI), structural modification was performed based on our previously derived compounds.
Molecular-level biochemical assays like transcriptomics, genomics and proteomics have emerged as valuable tools for identifying potential targets in cancer treatment through deep cyclic inhibition (DCI). How does the DCI mechanism compare to the design of other drugs for cancer treatment?
Drug development faces significant challenges: long timelines, high costs , complex processes and low probabilities of success (PoS), exacerbated by the shift towards more complex molecules, biologics and cell and gene therapies, hindering patient access to vital treatments.
In the dynamic world of drug discovery, the notion of "undruggable" targets presents both a significant challenge and an intriguing frontier for researchers and pharmaceutical companies. Many cancer treatments target DNA, but often these can cause collateral damage, leading to severe side effects.
What makes RRx-001 a first-in-class hypoxia-activated therapeutic, and how does its dual mechanism of action differ from traditional cancer treatments? Most, if not all, traditional cancer treatments are single minded.
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.
As we delve into the intricate world of biosimilar market dynamics, we’ll explore how these complex molecules are reshaping treatment paradigms across diverse patient populations. Let’s explore how biosimilars are reshaping treatment paradigms across different therapeutic areas. from 2020 to 2025[1]. .”
Presentations to highlight the OBI-833 Phase 1 clinical study results in non-small cell lung cancer (NSCLC) and the dose escalation cohort. These results will be presented by the lead investigators of OBI Pharma’s novel anti-Globo H therapeutic cancer vaccine, OBI-833. ” Presentation number: 397P / Poster: ID 680.
Food and Drug Administration (FDA) clearance of an Investigational New Drug (IND) application for SLV213 for the treatment of COVID-19 and has dosed the first subjects in a Phase 1 clinical study. SLV213 is a novel, orally available, smallmolecule antiviral drug candidate that inhibits human host cell cysteine proteases to block viral entry.
Consequently, a GK activator may provide therapeutic treatment for NIDDM and associated complications, inter alia, hyperglycemia, dyslipidemia, insulin resistance syndrome, hyperinsulinemia, hypertension, and obesity. Frequent use of these drugs may lead to weight gain and may induce edema and anemia. (E) For example, U.S.
(Nasdaq: ARDS), a biopharmaceutical company focused on the discovery and development of novel anti-infective therapies to treat life-threatening infections, today announced the Company will present at the ROTH Capital Partners 2020 MedTech Innovation Forum on Wednesday, October 28, 2020. About Aridis Pharmaceuticals, Inc.
New data further reinforce OCREVUS (ocrelizumab) as a highly effective treatment option offering a favourable and consistent benefit:risk profile, with high treatment persistence and adherence. Initiation of Phase IIIb OCREVUS higher dose clinical trial programme and Phase IV study evaluating OCREVUS in minority populations.
Bayer is progressing novel research around its prostate cancer treatment darolutamide. The presentation highlights the synergistic anti-cancer effects of a PSMA (prostate-specific membrane antigen)-actinium-225 conjugate in combination with darolutamide in preclinical prostate cancer models.
This targeted enhancement not only boosts the body’s natural mechanisms but also holds promise for developing novel treatments in immunology, where modulating immune responses can lead to more effective and durable therapeutic outcomes. Immune-mediated inflammatory disease therapeutics: past, present and future.
SH ) submitted its pivotal phase III clinical trial application (IND) of national class I innovative drug Chiauranib to NMPA, for the treatment of Small Cell Lung Cancer (SCLC) as a single agent for the patients after 2nd-line systemic chemotherapy and recurrence afterwards. (Chipscreen Biosciences, Stock Symbol: 688321.SH
Bayer will present new research across its oncology portfolio at the virtual American Association for Cancer Research (AACR) Annual Meeting 2021 , taking place over two weeks on April 10-15 and May 17-21, 2021. This includes preclinical data on darolutamide analyzing the impact of androgen stimulation and darolutamide treatment.
Five Promising Treatment Areas in Early-Phase Drug Development in 2024 aasimakopoulos Wed, 04/17/2024 - 15:52 Early-phase drug development is an ever-changing landscape, as emerging science leads to new promising areas of research for the treatment of human health issues.
The data is being presented today in oral presentations at the 62nd American Society of Hematology (ASH) Annual Meeting. The new data presented today strengthen our conviction that SY-1425 has the potential to become the foundation of care for all RARA-positive patients,” said David A. Chief Medical Officer of Syros.
These Phase 2 results strongly support the continued development of dexpramipexole as a potential first-in-class oral agent for the treatment of eosinophilic asthma,” said Michael Bozik, M.D., Knopp expects to present results of the trial at a forthcoming medical meeting. Measuring Eosinophils to Make Treatment Decisions in Asthma.
HiFi-NN results compared to SoTA models in Enzyme Functional Annotation on the price-149 enzyme benchmarking dataset Developed in collaboration with advisors Noelia Ferruz and Kevin Yang, HiFi-NN was accepted by NeurIPS, a prestigious AI conference, for presentation at their Machine Learning for Structural Biology workshop in December 2023.
However, natural product drug discovery presents several challenges that have reduced industry interest, including the inability to identify and isolate novel bioactive molecules responsible for a desired effect. Natural products have yielded numerous landmark drugs including aspirin, metformin, morphine and quinine.
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. “We are proud to present data on a range of digestive conditions across our portfolio and pipeline. .
IDE397 program update to be presented at the 39th Annual J.P. IDEAYA Biosciences will present a program update on IDE397 and its broader synthetic lethality pipeline at the 39 th Annual J.P. IDEAYA’s presentation for the 39 th Annual J.P.
SOUTH SAN FRANCISCO, Calif. , Morgan Healthcare Conference.
Formula C 27 H 29 Cl 2 FN 2 OS Crinecerfont , sold under the brand name Crenessity , is a medication used for the treatment of congenital adrenal hyperplasia. [1] Monoisotopic: 482.1594906 Chemical FormulaC 27 H 28 ClFN 2 OS CAS No. 321839-75-2 Molecular Weight 519.50 1] It is taken by mouth. [1] The Thermogravimetric Analysis (TGA) (FIG.
Conjugation of smallmolecule drugs to glucuronic acid is catalysed by several UGTs to frequently form N – and O -glucuronides. As in this example, most N -glucuronides of smallmolecule drugs are innocuous and possess no pharmacological activity.
Lessard created and advanced KIF1A.ORG’s Therapeutic Acceleration Program, facilitating the creation of patient-derived cell lines, mouse models, and drug screening platforms that are the bedrock of our search for treatments. Read more to learn about the factors involved in incentivizing investment in rare disease treatments.
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Convergent is currently conducting advanced human trials relating to prostate cancer treatments involving peptide receptor radionuclide therapy (“PRRT”) that targets the prostate-specific membrane antigen (“PSMA”) present on prostate cancer cells. or its ability to internalize PSMA.
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