oral bioavailability Articles
-
121 - Development of Protease Proprotein Convertase Subtilisin-Like Kexin Type 9 Antagonists
Abstract Protease proprotein convertase subtilisin-like kexin type 9 (PCSK9) is an important target for the treatment of hypercholesterolemia. Several pharmaceutical companies have focused on the development of mAbs. Yet, our approach has focused on developing orally bioavailable small molecule antagonists. PCSK9 is a serine protease that is synthesized as a zymogen that undergoes autocatalytic ...
-
Abstract 15053: New Insights into the Development of the Protease Proprotein Convertase Subtilisin-Like Kexin Type 9 Antagonists
Abstract Protease proprotein convertase subtilisin-like kexin type 9 (PCSK9) is an important target for the treatment of hypercholesterolemia. PCSK9 is synthesized as a zymogen that undergoes autocatalytic processing and secretion. Secreted PCSK9 binds to the LDL-receptor (LDLR) and chaperones it to the degradation pathway. Several pharmaceutical companies have developed injectable mAb PCSK9 ...
-
Abstract 10306: Identification and Characterization of Orally Bioavailable Small Molecule Protease Proprotein Convertase Subtilisin-like Kexin Type 9 Inhibitors (Best of Basic Science Abstract)
Abstract Intervention with drugs to reduce low density lipoprotein-cholesterol (LDL-C) has proven to decrease mortality and morbidity. Here, we report the development of small molecules that lower LDL-C by targeting the LDL-receptor (LDLR) degradation pathway, which is modulated by the protease proprotein convertase subtilisin-like kexin type 9 (PCSK9). PCSK9 is synthesized as a 72-kDa zymogen ...
-
Regulatory Guidelines for API-Excipient Compatibility Studies
Pharmaceutical excipients have important functions such as serving as carriers, improving drug stability, solubilization and slowing down the drug release. They are important ingredients that may affect the quality, safety, and effectiveness of the preparation. Classified by function and purpose, pharmaceutical excipients can be used in different drug forms, including: Injection, where ...
-
Abstract 4842: A comparative preclinical study of PARP inhibitors demonstrates superb properties for IDX-1197
Abstract Background PARP inhibitors have demonstrated clinically meaningful increase in progression-free survival as a single agent in women with recurrent ovarian cancer following a response to platinum-based chemotherapy. We aimed to develop a novel PARP inhibitor that may have potent antitumor efficacy. IDX-1197 is a novel, potent, selective, and orally bioavailable poly (ADP-ribose) ...
-
Protein degradation therapy development: SWOT
The Dana-Farber Cancer Institute utilized SWOT analysis to targeted protein degradation drug development to better evaluate the approach's strengths, weaknesses, opportunities, and threats. SWOT (Strengths-Weaknesses-Opportunities-Threats) analysis is frequently used in business development and strategic planning, but it may also be used to critically analyze quickly evolving fields, as the ...
-
Philly Pharmacologists are Developing a Promising Pain-Relieving CBD Analog Drug
Scientists from Temple’s Lewis Katz School of Medicine and local biopharma company Neuropathix are testing their compound, KLS-13019, which is intended to target chemotherapy-induced pain in cancer patients. Sara Jane Ward, assistant professor of pharmacology at Temple University’s Lewis Katz School of Medicine, and Douglas Brenneman, chief pharmacologist at Neuropathix, discuss ...
-
Applications of Liposomal Drug Delivery System Technology
Liposomes are a novel drug delivery system (DDS). They are bimolecular vesicles that form spontaneously when phospholipids are dispersed in water. Liposomes vary in size, composition and charge and can be used as carriers for a wide range of drug molecules, such as chemotherapeutic agents, antimicrobial and antiviral drugs, antiparasitic drugs, genetic material, vaccines, therapeutic proteins, ...
-
The Spark for Decoding Biology: An Origin Story
Recursion is entering an exciting period in our evolution as a clinical-stage biotechnology company. We recently announced that we’ve enrolled the first patient in the first human efficacy trial in our company’s history — a significant milestone for us, and for the patients we hope to serve. Our Phase 2 trial is investigating the treatment of a disease called cerebral ...
By Recursion
-
Based on Antibody Targeted Protein Degradation
In recent years, PROteolysis TArgeting Chimeras (PROTAC), which utilizes the cell's own degradation mechanisms to eliminate specific disease-related proteins, has emerged as one of the most promising methods. Apart from PROTAC, various targeted protein degradation (TPD) strategies are emerging, involving molecular glue, Autophagy-Targeting Chimera (AUTEC), Autophagosome Tethering Compound ...
By BOC Sciences
-
Rani Therapeutics Debuts on the Nasdaq: What uou should know About the Biopharma
IMPORTANT MESSAGE: Benzinga prides itself as a media platform that is "For the People, By the People." We understand the markets are scary right now. For that reason, we are here to help. For today only get access to our #1 Options Newsletter for only $1. Rani Therapeutics Holdings, Inc. RANI+ Free Alerts, a San Jose, California-based early stage biopharma, debuted Friday on the Nasdaq ...
-
Antibody-Drug Conjugates: New Strategies of ADC Payloads
The concept of ADCs was first proposed by Nobel Prize winner Paul Ehrlich in 1913. But it was not until 1975, when hybridoma technology began to be used to produce monoclonal antibodies, that the era of ADC drug development truly began. Driven by increasingly mature technology, ADC drugs have gone through three iterations (Fig. 1). Although ADCs have gone through three iterations, current ...
By BOC Sciences
-
What are the ADC drugs?
Antibody-drug conjugates (ADCs) continue to rise at home and abroad, but ADCs are not a new thing. Why has ADC been surging for so many years? What kind of magic power it contains, and what makes its growth path so tortuous? Let's take a brief look at the magical "magic bullet"-ADC. ADC (antibody-conjugated drug) is not a new concept. As early as the early 20th century, the Nobel Prize winner ...
By BOC Sciences
-
Anticoagulants and Rat Poison
What do rat poison and anticoagulation medicine have in common? As often happens in scientific discovery, research follows a twisted route to the most effective remedy. ...
-
Comprehensive Insights into Native Porcine Pancreatin: A Versatile Enzyme Preparation
Native Porcine Pancreatin, an enzymatic mixture derived from the porcine pancreas, has emerged as a fundamental component in various industries due to its unique enzymatic composition. Comprising amylase, lipase, and protease enzymes, this preparation is celebrated for its multifaceted applications and plays an indispensable role in the pharmaceutical, food, and biotechnology sectors. In this ...
Need help finding the right suppliers? Try XPRT Sourcing. Let the XPRTs do the work for you