Sat.May 06, 2023 - Fri.May 12, 2023

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Molecules of the Month – April 2023

Drug Hunter

An oral macrocyclic peptide PCSK9 inhibitor entering Ph. III for hypercholesterolemia later this year, a Ph. I/Ib KRAS G12C (ON) tri-complex inhibitor for the treatment of advanced solid tumors, an oral mutant-selective BRAFC600X degrader in Ph. I for BRAF-driven cancers, and an orally available AR-degrading PROTAC in Ph. II for advanced prostate cancers are just some of the examples for this month’s MOTM.

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Discovery of [5,5??bibenzo[d][1,3]dioxol]?6?substituted amine derivatives as potent proprotein convertase subtilisin/kexin type 9 inhibitors

Chemical Biology and Drug Design

A series of [5,5′-bibenzo[d][1,3]dioxol]-6-amine analogs were designed and synthesized based on our previous work. Compounds D28 and D29 impaired PCSK9/LDLR PPI, restored LDLR expression, and improved extracellular LDL uptake of HepG2 cells in the presence of PCSK9. Abstract Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as a promising therapeutic target for the treatment of hyperlipidemia.

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ANTINOCICEPTIVE EFFECTS OF AN ANTI-CGRP ANTIBODY IN RAT MODELS OF COLON-BLADDER CROSS ORGAN SENSITIZATION [Gastrointestinal, Hepatic, Pulmonary, and Renal]

ASPET

Irritable bowel syndrome (IBS) and bladder pain syndrome/interstitial cystitis (BPS/IC) are comorbid visceral pain disorders seen commonly in women with unknown etiology, limited treatment options and can involve visceral organ cross-sensitization. Calcitonin gene-related peptide (CGRP) is a mediator of nociceptive processing and may serve as a target for therapy.

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Do patients have to pay for clinical trials?

Antidote

One of the questions most frequently asked by patients is, “Do I have to pay to participate in a clinical trial?” While patients typically will not incur expenses for taking part in a research study, in some instances, they may be responsible for copays and payments towards their deductible depending on their insurance plan.

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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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Change is Inevitable – Plan Ahead: An Assessment of FDA’s Draft Guidance on Predetermined Change Control Plans for Artificial Intelligence/Machine Learning-Enabled Device Software Functions

FDA Law Blog: Biosimilars

By Lisa M. Baumhardt, Senior Medical Device Regulation Expert & Philip Won & Gail H. Javitt — FDA recently published a long-awaited draft guidance aimed at reducing the need for prior FDA authorization of modifications to artificial intelligence/machine learning (AI/ML)-enabled device software functions (ML-DSFs). The draft guidance, “Marketing Submission Recommendations for a Predetermined Change Control Plan for Artificial Intelligence/Machine Learning (AI/ML)-Enabled Device Software

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Biological functions and structural biology of Plasmodium falciparum autophagy?related proteins: The under?explored options for novel antimalarial drug design

Chemical Biology and Drug Design

Certain Plasmodium falciparum autophagy-related proteins ( Pf Atg) play autophagic and/or non-autophagic functions. Also, Pf Atg8 was found to have unique hydrophobic pockets, which it uses for interaction with other proteins. Moreover, the most formidable inhibitor of Pf Atg8- Pf Atg3 PPI was discovered to be 2-bromo-N-(4-pyridin-2-yl-1,3-thiazol-2-yl) benzamide.

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More Trending

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Which pharmaceutical companies have the most SPCs in Lithuania?

Drug Patent Watch

This chart shows the pharmaceutical companies with the most supplementary protection certificates (SPCs) in Lithuania. SPCs are used in European Union and select others to encourage pharmaceutical innovation by compensating… The post Which pharmaceutical companies have the most SPCs in Lithuania? appeared first on DrugPatentWatch - Make Better Decisions.

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Skinny Label and Induced Infringement: The Saga Continues

FDA Law Blog: Biosimilars

By Sara W. Koblitz — Well, we’re a little late to blogging about this, but the significance of the ongoing Teva v. GSK litigation to Hatch-Waxman aficionados makes this case still ripe for blogging. Six months after the Supreme Court asked the Solicitor General to submit a brief on behalf of the U.S. government in the now-infamous (at least in FDA circles) Teva v.

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In vitro and in vivo antileishmanial activity of the hanging sedge flavonoids based on bio? guided fractionation assay

Chemical Biology and Drug Design

In-vitro and in-vivo anti-leishmanial activity of the hanging sedge flavonoids; based on bio- guided fractionation assay. Abstract As a major public health issue, cutaneous leishmaniasis (CL) has a number of complications, including drug resistance and poor response to conventional treatments. Over the last decade, research on natural sources for finding new antileishmanial agents has been a critical part of tropical disease research.

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The State of the Specialty Market 2023: Reflections, Trends, and Photos from #Asembia23

Drug Channels

Last week, Paula and I had the pleasure of attending Asembia’s 2023 Specialty Pharmacy Summit at the wonderful Wynn Las Vegas. As I do every year, I will violate Vegas code and tell you what happened there. I offer reflections on my keynote session with Seema Verma, share my experiences during the featured session, and highlight some crucial specialty industry trends.

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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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New patent for Par Sterile drug VASOSTRICT

Drug Patent Watch

Annual Drug Patent Expirations for VASOSTRICT Vasostrict is a drug marketed by Par Sterile Products and is included in one NDA. It is available from six suppliers. There are fourteen… The post New patent for Par Sterile drug VASOSTRICT appeared first on DrugPatentWatch - Make Better Decisions.

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How Soon Until the Kochava Geolocation Case Catches Up to Medical Device Companies?

FDA Law Blog: Biosimilars

By Jeffrey N. Wasserstein — We were listening to a radio interview last week with Lina Khan , the Chair of the Federal Trade Commission (“FTC”). In the interview, Khan spoke about the Commission’s efforts to regulate geolocation data trackers so that they don’t abuse their abilities. The risks she described caught our attention because two of the risk profiles she cited included things that touched on FDA-related entities, such as medical devices that transmit data.

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A single?chain variable fragment?anticancer lytic peptide (scFv?ACLP) fusion protein for targeted cancer treatment

Chemical Biology and Drug Design

We designed an fusion protein by connecting a cetuximab-derived single-chain variable fragment targeting the epidermal growth factor receptor (anti-EGFR scFv) and the anticancer lytic peptide (ACLP) ZXR2. The results suggest that scFv-ACLP fusion proteins may be potential anticancer drug candidates for targeted cancer treatment. Abstract Antibody-directed drugs for targeted cancer treatment have become a hot topic in new anticancer drug development; however, antibody-fused therapeutic peptides w

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Breaking C-F bonds in drugs

Metabolite Tales Blog

Breaking C-F bonds in drugs – metabolism mediated release of fluorine By Samuel Coe and Julia Shanu-Wilson Lenacapavir, recently approved for multi-drug resistant HIV-1 infection, contains 10 fluorine atoms. Fluorine is a highly reactive chemical element that has a unique electron configuration and provides valuable benefits in medicinal chemistry.

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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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Schizophrenia Assessment in Zebrafish

biobide

Schizophrenia is a chronic psychiatric disorder characterized by continuous or relapsing episodes of psychosis that can alter severely normal brain function. This mental health issue makes it arduous to determine what is real or not, producing symptoms such as hallucinations, delusions, and disorganized thinking. Therefore, this illness is a serious mental disorder that affects around 1 to 300 people, meaning 24 million people globally.

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Adapt or Fall Behind: The Need for Agile Copay Programs in Today's Shifting Payer Landscape

Drug Channels

Today’s guest post comes from Nasir Ali, Chief Product Officer at CareMetx Nasir discusses manufacturers’ strategies for mitigating the patient impact of copay accumulators and maximizers. He then outlines two key tactics that manufacturers should include in hub programs. To learn more how digitally-enabled hub programs help patients, download CareMetx’s report: The Evolving Landscape of Digital Healthcare Hubs.

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Design, synthesis, in vitro evaluation, and molecular modeling studies of N?substituted benzomorphans, analogs of LP2, as novel MOR ligands

Chemical Biology and Drug Design

New analogs of dual-target MOR/DOR ligand LP2 were synthesized. In-vitro, their affinity profile versus opioid receptors was performed and molecular modeling studies were conducted to deeply analyze the binding mode and the interactions between the new ligands and all opioid receptors. Abstract 6,7-Benzomorphans have been investigated in medicinal chemistry for developing new drugs.

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Which pharmaceutical companies have the most emulsion dosed drugs?

Drug Patent Watch

This chart shows the pharmaceutical companies with the most emulsion dosed drugs. For a different perspective, see the most popular dosage types. The companies with the most emulsion dosed drugs… The post Which pharmaceutical companies have the most emulsion dosed drugs? 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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Codon News: Cloned Mongolian Horses

Codon

Hey there. Tap tap tap. Today, we’ve got news about AI mind readers, a child who underwent brain surgery while in the womb, and (another) problem with lab-grown meat. Scroll to the end for a beautiful chart about the Anthropocene & some details on insect engineering companies. Fun. Also. news items are now sent on Thursdays. Research roundups are sent on Sundays.

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Regulatory Developments in Ophthalmology: Applying New FDA Guidance, Part Two

The Premier Consulting Blog

In this second of our two-part series, we continue our discussion about significant recent developments regarding the regulation of ophthalmic products and discuss what to expect in the months ahead. Unsurprisingly, the U.S. Food and Drug Administration’s (FDA) released updated guidance following the landmark Genus Medical Technologies LLC v. United States Food and Drug Administration court decision.

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Estrone analogs as potential inhibitors targeting EGFR?MAPK pathway in non?small?cell lung cancer

Chemical Biology and Drug Design

Synthesized analogs MMA307 and MMA320 induce G1 phase cell cycle arrest and inhibit EGFR-MAPK Proteins involved in tumor progression in non-small-cell lung cancer. Molecular dynamic simulations provided additional confirmation of biological activity. Abstract Lung cancer is the deadliest human cancer globally, with non-small-cell lung cancer (NSCLC) being the most frequent type.

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New patent expiration for Sage Prods drug CHLORHEXIDINE GLUCONATE

Drug Patent Watch

Annual Drug Patent Expirations for CHLORHEXIDINE+GLUCONATE Chlorhexidine Gluconate is a drug marketed by Sage Prods, Akorn, Bajaj, Lyne, Pharm Assoc, Wockhardt Bio Ag, Xttrium, Becton Dickinson, and Kendall Il and,… The post New patent expiration for Sage Prods drug CHLORHEXIDINE GLUCONATE appeared first on DrugPatentWatch - Make Better Decisions.

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Meet the Expert: Alexis O'temro

thought leadership

Our "Meet the Expert" series introduces you to our team of experts around the world. This "behind the curtain" view will help you get to know who we are on a professional and personal level, and highlight how our colleagues work together on our higher purpose to improve patient health and safety throughout the complete product lifecycle.

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A proactive diabetes review model: from concept to nurse-led research

On Medicine

There are a few (but growing) centers that will proactively see patients with diabetes in high-risk areas when admitted to the hospital, however, by far the most common practice is for patients to only be seen by a specialist team, including for diabetes, on receipt of a referral. In diabetes, referrals are often triggered by glycemic-related events, such as hypo/hyperglycemia and ketosis or for patient education.

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Design, synthesis, and evaluation of 1H?benzo[d]imidazole?4?carboxamide PARP?1 inhibitors using different saturated nitrogen?contained heterocycle as linker group

Chemical Biology and Drug Design

A series of 1H-benzimidazole-4-carboxamide PARP-1 inhibitors using different saturated nitrogen-containing heterocycles as linker groups was designed synthesized and evaluated its anti-proliferation activities of MDA-MB-436 cell to obtain the preferred structures of linker group and terminal group in the AD site. Abstract Poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors have been successfully applied in the clinical treatment of various cancer.

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Keys to Success in Vaccine Development for Special Populations

PPD

The global COVID-19 pandemic increased awareness of the importance of vaccine development — both for drug developers and the public. The speed at which COVID-19 vaccines were developed was remarkable, but like most newly developed vaccines, there was variation among who could receive the shots and when. To effectively implement vaccine clinical trials for special populations, it is critical for vaccine developers to partner with a contract research organization (CRO) that has demonstrated

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Let’s Get Personal: Four Benefits to Omnichannel Strategies

H1 Blog

Drive Engagement and Segmentation for Physician Marketing With the proliferation of digital media, marketing in the healthcare industry has shifted from traditional tactics to an omnichannel approach. Omnichannel engagement for physician marketing is a powerful tool for biotechnology and pharma companies looking to increase reach and drive engagement among HCPs.

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Codon News: Cloned Mongolian Horses

Codon

Hey there. Tap tap tap. Today, we’ve got news about AI mind readers, a child who underwent brain surgery while in the womb, and (another) problem with lab-grown meat. Scroll to the end for a beautiful chart about the Anthropocene & some details on insect engineering companies. Fun. Also. news items are now sent on Thursdays. Research roundups are sent on Sundays.

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Baicalin mitigated IL?1??Induced osteoarthritis chondrocytes damage through activating mitophagy

Chemical Biology and Drug Design

Baicalin activated mitophagy in IL-1β-induced chondrocytes by inhibiting PI3K/AKT/mTOR pathway and activating PINK1/Parkin and PINK1/Drp-1 pathway, thereby reducing the chondrocyte injury. Abstract Mitophagy is related to chondrocyte homeostasis and plays a key role in the progress of osteoarthritis (OA). Baicalin has a protective effect on OA chondrocytes, the aim of this study was to explore whether the effect of Baicalin on IL-1β-induced chondrocyte injury is related to the regulation of mito

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Antibodies 101: Epitope tags

addgene Blog

The stress of finding a ‘good’ antibody is something we’ve all experienced. Finding an antibody that works for your application, specifically detects your protein, is species compatible, and doesn’t come with a high background can be a huge challenge. Epitope tags eliminate the need for target-specific antibodies and have been widely used across species and applications.

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Thiomethyltetrazines are Reversible Covalent Cysteine Warheads whose Dynamic Behavior can be "Switched off” via Bioorthogonal Chemistry Inside Live Cells

Covalent Modifiers

Amanda Tallon, Yingrong Xu, Graham West, Christopher am Ende, Joseph Fox ChemRXiv , 2023 [link] Electrophilic small molecules that can reversibly modify proteins are of growing interest in drug discovery. However, the ability to study reversible covalent probes in live cells can be limited by their reversible reactivity after cell lysis and in proteomic workflows, leading to scrambling and signal loss.

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ELRIG UK Appoints Nick Clare to Board as Vendor Strategy Work Group Lead

Elrig

ELRIG UK Appoints new Vendor Strategy Work Group Lead ELRIG UK Appoints Nick Clare to Board as Vendor Strategy Work Group Lead Cambridge, UK, 11 May 2023: The European Laboratory Research & Innovation Group (ELRIG) UK today announced the appointment of Nick Clare to the ELRIG board. He will chair and lead the Vendor Strategy Work Group to help ensure the vendors’ perspectives and interests are represented within the ELRIG board.

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Prediction of bioactivities of microsomal prostaglandin E2 synthase?1 inhibitors by machine learning algorithms

Chemical Biology and Drug Design

Workflow of developing a series of machine learning regression models for predicting bioactivities of mPGES-1 inhibitors. Abstract There is a strong interest in the development of microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors of their potential to safely and effectively treat inflammation. Herein, 70 QSAR models were built on the dataset (735 mPGES-1 inhibitors) characterized with RDKit descriptors by multiple linear regression (MLR), support vector machine (SVM), random forest (RF

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