March, 2023

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Reversible Dual-Covalent Molecular Locking of the 14-3-3/ERR? Protein–Protein Interaction as a Molecular Glue Drug Discovery Approach

Covalent Modifiers

Bente A. Somsen, Rick J.C. Schellekens, Carlo J.A. Verhoef, Michelle R. Arkin, Christian Ottmann, Peter J. Cossar, and Luc Brunsveld Journal of the American Chemical Society 2023 DOI: 10.1021/jacs.2c12781 Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool compounds for biophysics and (structural) biology, and as starting points for molecular glue drug discovery.

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2023 IS the Year for OTC Naloxone!

FDA Law Blog: Biosimilars

By Kalie E. Richardson — Early on March 29, 2023, FDA announced the landmark approval of Narcan (naloxone hydrochloride) Nasal Spray for use as a nonprescription opioid overdose reversal agent. I previously blogged on the February 15, 2023 Joint Meeting of the Nonprescription Drugs Advisory Committee (NDAC) and the Anesthetic and Analgesic Drug Products Advisory Committee (AADPAC) which unanimously agreed that the benefit-risk profile of Narcan Nasal Spray (NNS) is “supportive of its use as a n

Pharmacy 105
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Molecular targets of metformin against ovarian cancer based on network pharmacology

Chemical Biology and Drug Design

In this study, 255 drug targets of metformin were obtained from the BATMAN, Drugbank, PharmMapper, SwissTargetPrediction, and TargetNet databases. Meanwhile, 10,463 differentially expressed genes (DEGs) in OC were screened from GSE29450, GSE10971, GSE18520, GSE14407, and TCGA + GTEx datasets. A total of 95 common targets were obtained by deintersection of drug targets of metformin and DEGs in OC.

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KATP Channel Prodrugs Reduce Inflammatory and Neuropathic Hypersensitivity, Morphine Induced Hypersensitivity, and Precipitated Withdrawal in Mice [Behavioral Pharmacology]

ASPET

Previous studies show ATP-sensitive potassium (K ATP ) channel openers can reduce hypersensitivity associated with chronic pain models in rodents, and reduce morphine tolerance. Many agonists of K ATP channels are not soluble in physiologically relevant vehicles, requiring adaptation for clinical use. This study compared the antinociception activity of novel K ATP channel targeting prodrugs, CKLP1, CKLP2, and CF3-CKLP.

Treatment 100
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Bridging Innovation & Patient Care: The Growing Role of AI

Speaker: Simran Kaur, Co-founder & CEO at Tattva.Health

AI is transforming clinical trials—accelerating drug discovery, optimizing patient recruitment, and improving data analysis. But its impact goes far beyond research. As AI-driven innovation reshapes the clinical trial process, it’s also influencing broader healthcare trends, from personalized medicine to patient outcomes. Join this new webinar featuring Simran Kaur for an insightful discussion on what all of this means for the future of healthcare!

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Webinar recap: Kidney Action Week webinar featuring Antidote’s Rich Towne, PharmD

Antidote

The annual Kidney Action Week is a virtual event put on by the American Kidney Fund designed to bring the entire kidney health community together for a week of amazing and informative content on all things related to kidney health. The event is filled with discussions, Q&As, webinars, and more — and this year, Antidote was thrilled to be involved!

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Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry

Covalent Modifiers

John C. Tran, Thomas Hunsaker, Christina Bell, Taylur P. Ma, Emily Chan, Pablo Saenz-Lopez Larrocha, Kelsey Homyk, Liling Liu, Hank La, Jialin Mao, Cecile C. de la Cruz, Kebing Yu, Maureen Beresini, William F. Forrest, Yang Xiao, Anne Jang, Natalia Samus, Nicholas Dupuis Stesco, Marija Mentinova, Stephane Parent, Gwenael Pottiez, Michael Schirm, Hans E.

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HP&M Attorney Mark Tobolowsky Co-Authors Article in Human Gene Therapy Advocating for the Acceptance of Microdystrophin Expression in DMD Patients as a Surrogate Endpoint for Accelerated Approval

FDA Law Blog: Drug Discovery

Hyman, Phelps & McNamara, P.C.’s Mark Tobolowsky co-authored the peer-reviewed article “ Microdystrophin Expression as a Surrogate Endpoint for Duchenne Muscular Dystrophy Clinical Trials ” in the recently published edition of Human Gene Therapy. The article arose out of work conducted by the Pathway Development Consortium , a partnership between stakeholders in the AAV gene therapy space.

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Therapeutic efficacy of caffeic acid phenethyl ester in cancer therapy: An updated review

Chemical Biology and Drug Design

Caffeic acid phenethyl ester (CAPE) demonstrating its anticancer potential through specifically targets genes involved in cell death, cell cycle regulation, angiogenesis, and metastasis in various types of cancers. Abstract Nowadays, there is a lot of public and scientific interest in using phytochemicals to treat human ailments. Existing cancer medicines still run across obstacles, despite significant advancements in the field.

Therapies 100
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Sickle Cell Disease: The Importance of Amplifying Patient Voices

Advarra

Having a one in four chance of developing sickle cell disease (SCD) is uniquely, and overwhelmingly, familiar to the African American population. Considered a rare disease, research in finding better therapies – and possibly even a cure – for SCD may be competing for funding with conditions impacting broader populations. SCD’s significant impact on African Americans also means it predominantly impacts a minority community historically underserved by clinical research.

Disease 98
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From Diagnosis to Delivery: How AI is Revolutionizing the Patient Experience

Speaker: Simran Kaur, Founder & CEO at Tattva Health Inc.

The healthcare landscape is being revolutionized by AI and cutting-edge digital technologies, reshaping how patients receive care and interact with providers. In this webinar led by Simran Kaur, we will explore how AI-driven solutions are enhancing patient communication, improving care quality, and empowering preventive and predictive medicine. You'll also learn how AI is streamlining healthcare processes, helping providers offer more efficient, personalized care and enabling faster, data-driven

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An overview of key hemophilia facts

Antidote

The rare, inherited blood disorder hemophilia is estimated to impact approximately 20,000 individuals in the United States , and over 400,000 worldwide. Currently, there is no cure for hemophilia — but through ongoing research, medical experts are continually learning more about the disease.

Disease 98
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NOW AVAILABLE: The 2023 Economic Report on U.S. Pharmacies and Pharmacy Benefit Managers

Drug Channels

I am pleased to announce our new 2023 Economic Report on U.S. Pharmacies and Pharmacy Benefit Managers , available for purchase and immediate download. Click here to download a free report overview (including key industry trends, the Table of Contents, and a List of Exhibits) New Drug Channels Institute Study Analyzes Impact of Inflation Reduction Act on U.S.

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Development and applications of chimera platforms for tyrosine phosphorylation

Covalent Modifiers

Rajaiah Pergu, Veronika M. Shoba, Santosh K. Chaudhary, Dhanushka N. P. Munkanatta Godage, Arghya Deb, Santanu Singha, Uttam Dhawa, Viktoriya Anokhina, Sameek Singh, Sachini U. Siriwardena, Amit Choudhary bioRxiv 2023.03.05.531183; doi: [link] Chimeric small molecules that induce post-translational modification (PTM) on a target protein by bringing it in proximity to a PTM-inducing enzyme are furnishing novel modalities to perturb protein function.

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What Do Patients Have to Say about Gene Therapy Trials? An Upcoming FDA Public Meeting to Hear from Patients and Caregivers

FDA Law Blog: Drug Discovery

By Larry J. Bauer, Senior Regulatory Drug Expert & James E. Valentine — Incorporating patient and caregiver experiences into every phase of drug development has become increasingly prioritized during both development and review ( see, e.g. , previous coverage here ). Who better than people living with a condition to inform drug companies, physicians, academics, and the FDA on what it is like to live with their condition, what symptoms most impact their lives, what goes into their decision ab

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How Machine Learning Drives Clinical Trial Efficiency

Clinical trial data management is increasingly challenging as studies grow in complexity. Quickly accessing and analyzing study data is vital for assessing trial progress and patient safety. In this paper, we explore real-time data access and analysis for proactive study management. We investigate using adverse event (AE) data to monitor safety and discuss a clinical analytics platform that supports collaboration and data review workflows.

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Perspectives on cutting?edge nanoparticulate drug delivery technologies based on lipids and their applications

Chemical Biology and Drug Design

Lipidic Nanoparticle drug and technology. Lipidic carriers like Liposomes, Niosomes, Solid-Lipid Nanoparticles, Micelles etc. Abstract Numerous nanotech arenas in therapeutic biology have recently provided a scientific platform to manufacture a considerable swath of unique chemical entities focusing on drugs. Recently, nanoparticulate drug delivery systems have emerged to deliver a specific drug to a specified site.

Drugs 100
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Pharmaceutical companies with the most ‘Pediatric Exclusivity’ drugs

Drug Patent Watch

This chart shows the companies which have received the most pediatric exclusivities in the past five years. Pediatric exclusivity is granted to drug companies for conducting pediatric studies on their… The post Pharmaceutical companies with the most ‘Pediatric Exclusivity’ drugs appeared first on DrugPatentWatch - Make Better Decisions.

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Understanding viral load and hepatitis B infections

Antidote

Hepatitis B , sometimes abbreviated to HBV, is a liver infection that is one of the most serious in the world. If left untreated, hepatitis B can cause fibrosis, cirrhosis, hepatocellular carcinoma, and end-stage liver disease.

Disease 98
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The Top 15 U.S. Pharmacies of 2022: Market Shares and Revenues at the Biggest Companies

Drug Channels

Next week, Drug Channels Institute will release our 2023 Economic Report on U.S. Pharmacies and Pharmacy Benefit Managers. It’s the 14th edition of our popular and comprehensive examination of the entire U.S. drug pricing, reimbursement, and dispensing system. The exhibit below—one of 241 in our new report—provides a first look at the 15 largest organizations, ranked by total U.S. prescription dispensing revenues for calendar year 2022.

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Deliver Fast, Flexible Clinical Trial Insights with Spotfire

Clinical research has entered a new era, one that requires real-time analytics and visualization to allow trial leaders to work collaboratively and to develop, at the click of a mouse, deep insights that enable proactive study management. Learn how Revvity Signals helps drug developers deliver clinical trial data insights in real-time using a fast and flexible data and analytics platform to empower data-driven decision-making.

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A covalent BTK ternary complex compatible with targeted protein degradation

Covalent Modifiers

James Schiemer, Andrew Maxwell, Reto Horst, Shenping Liu, Daniel P. Uccello, Kris Borzilleri, Nisha Rajamohan, Matthew F. Brown & Matthew F. Calabrese Nat Commun 14 , 1189, 2023 [link] Targeted protein degradation using heterobifunctional chimeras holds the potential to expand target space and grow the druggable proteome. Most acutely, this provides an opportunity to target proteins that lack enzymatic activity or have otherwise proven intractable to small molecule inhibition.

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JOIN HP&M FOR A WEBINAR: “The ‘End’ of the COVID-19 Emergency: The Ryan Haight Act, Telemedicine, and Next Steps?” on Thursday, March 23, 2023 at 12 Noon EST

FDA Law Blog: Biosimilars

The COVID-19 pandemic emergency forced federal regulators to take extraordinary measures to ensure that patients were permitted continued access to important medicines. These government measures included granting temporary exemptions from certain FDA and DEA legal requirements. When the public health emergency ends on May 11, 2023 , so do these exemptions.

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Formulation, optimization and characterization of raloxifene hydrochloride loaded PLGA nanoparticles by using Taguchi design for breast cancer application

Chemical Biology and Drug Design

Formulation development, optimization and characterization of poly (lactic-co-glycolic acid) nanoparticles loaded with raloxifene by emulsion solvent diffusion evaporation technique to improve oral bioavailability by using Taguchi design. Abstract Multidrug resistance in breast cancer and the associated side-effects of anticancer therapies are significant hurdles in chemotherapy-based treatment.

Treatment 100
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Which pharmaceutical drugs have the most drug patents in Ukraine?

Drug Patent Watch

This chart shows the drugs with the most patents in Ukraine. Patents must be filed in each country (or, in some cases regional patent office) where patent protection is desired.… The post Which pharmaceutical drugs have the most drug patents in Ukraine? appeared first on DrugPatentWatch - Make Better Decisions.

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Clinical Data Like You´ve Never Seen It Before: Why Spotfire Is the Leading Tool for Clinical Analytics

Clinical development organizations face a wide array of challenges when it comes to data, many of which can impact the operational effectiveness of their clinical trials. In this whitepaper, experts from Revvity Signals explore how solutions like TIBCO® Spotfire® enable better, more streamlined studies. The whitepaper also features a success story from Ambrx, a leading biopharmaceutical company, detailing how it has leveraged Spotfire to tackle data quality and collaboration challenges in clinic

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What are the stages of idiopathic pulmonary fibrosis?

Antidote

Idiopathic pulmonary fibrosis , or IPF, can be a frightening diagnosis. IPF is a rare, progressive lung disease that develops differently for everyone, and managing its development can be difficult. However, some individuals are able to live with the disease and stay active for many years.

Disease 98
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It's Not All Bad News: Data Shows There's a Collaborative Future for 340B

Drug Channels

Today’s guest post comes from Rhiannon Naslund, Chief Marketing Officer at Kalderos. Rhiannon discusses the growing collaboration between manufacturers and covered entities regarding 340B discount claims. She goes on to describe the Kalderos Discount Hub solution that reviews claims that have a high likelihood of being a duplicate discount. To stay up-to-date with the latest drug discount developments, sign up for the Kalderos newsletter.

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Critical Steps Your Workplace Can Take Today to Prevent Suicide

NIOSH Science Blog: Drugs

Employers can play a vital role in suicide prevention. Historically, suicide, mental health, and well-being have been underrepresented in workplace health and safety efforts, but this is changing. In some European countries, there are workplace standards for workplace psychosocial hazards that put workers at risk for suicide. Additionally, in France, employers have been made accountable for toxic workplaces and management practices that contributed to worker suicides.[1] Some of the latest workp

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Big Decisions – Reviewing FDA Advisory Committee Outcomes Since 2020

Eye on FDA

In January we took a look at FDA Advisory Committees (AdComms) – FDA AdComms – When the Going Gets Tough – noting, among other things that there had not only been fewer meetings but also that it appeared that the outcomes were increasingly negative. Just to recap, for the entire year of 2022 there were only 14 meetings held to consider whether new medicines should be recommended for approval, a slight increase over the 10 the year before, but considerably lower fewer than 2018

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Evodiamine inhibits malignant progression of ovarian cancer cells by regulating lncRNA?NEAT1/miR?152?3p/CDK19 axis

Chemical Biology and Drug Design

EVO dose-dependently attenuated cell viability, induced G2/M phase arrest, and apoptosis in ovarian cancer cells. EVO regulates ovarian cancer progression through the NEAT1-miR-152-3p-CDK19 axis, which further advances the possibility of EVO as a therapeutic drug for ovarian cancer. Abstract Evodiamine (EVO) has been demonstrated to promote apoptosis of ovarian cancer cells, and upregulate miR-152-3p level in colorectal cancer.