Design, development, and technical considerations for dry powder inhaler devices
Drug Discov Today. 2024 Mar 24:103954. doi: 10.1016/j.drudis.2024.103954. Online ahead of print.ABSTRACTThe dry powder inhaler (DPI) stands out as a highly patient-friendly and effective pulmonary formulation, surpassing traditional and other pulmonary dosage forms in certain disease conditions. The development of DPI products, however, presents more complexities than that of other dosage forms, particularly in device design and the integration of the drug formulation. This review focuses on the capabilities of DPI devices in pulmonary drug delivery, with a special emphasis on device design and formulation development. It ...
Source: Drug Discovery Today - March 26, 2024 Category: Drugs & Pharmacology Authors: Sagar Dhoble Archana Kapse Vaibhav Ghegade Manasi Chogale Vinod Ghodake Vandana Patravale Lalitkumar Vora Source Type: research

Peptide-derived ligands for the discovery of safer opioid analgesics
Drug Discov Today. 2024 Mar 19:103950. doi: 10.1016/j.drudis.2024.103950. Online ahead of print.ABSTRACTDrugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the treatment of pain, but activation of MOR with current opioid analgesics also produces harmful side effects, notably physical dependence, addiction, and respiratory depression. Opioid peptides have been accepted as promising candidates for the development of safer and more efficacious analgesics. To develop peptide-based opioid analgesics, strategies such as modification of endogenous opioid peptides, development of multifunctional...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Abbe Eliasof Lee-Yuan Liu-Chen Yangmei Li Source Type: research

Small molecules targeting canonical transient receptor potential channels: an update
Drug Discov Today. 2024 Mar 20:103951. doi: 10.1016/j.drudis.2024.103951. Online ahead of print.ABSTRACTTransient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different ...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Hua Liu Min Fu Yifan Zhang Qidong You Lei Wang Source Type: research

Peptide-derived ligands for the discovery of safer opioid analgesics
Drug Discov Today. 2024 Mar 19:103950. doi: 10.1016/j.drudis.2024.103950. Online ahead of print.ABSTRACTDrugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the treatment of pain, but activation of MOR with current opioid analgesics also produces harmful side effects, notably physical dependence, addiction, and respiratory depression. Opioid peptides have been accepted as promising candidates for the development of safer and more efficacious analgesics. To develop peptide-based opioid analgesics, strategies such as modification of endogenous opioid peptides, development of multifunctional...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Abbe Eliasof Lee-Yuan Liu-Chen Yangmei Li Source Type: research

Small molecules targeting canonical transient receptor potential channels: an update
Drug Discov Today. 2024 Mar 20:103951. doi: 10.1016/j.drudis.2024.103951. Online ahead of print.ABSTRACTTransient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different ...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Hua Liu Min Fu Yifan Zhang Qidong You Lei Wang Source Type: research

Peptide-derived ligands for the discovery of safer opioid analgesics
Drug Discov Today. 2024 Mar 19:103950. doi: 10.1016/j.drudis.2024.103950. Online ahead of print.ABSTRACTDrugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the treatment of pain, but activation of MOR with current opioid analgesics also produces harmful side effects, notably physical dependence, addiction, and respiratory depression. Opioid peptides have been accepted as promising candidates for the development of safer and more efficacious analgesics. To develop peptide-based opioid analgesics, strategies such as modification of endogenous opioid peptides, development of multifunctional...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Abbe Eliasof Lee-Yuan Liu-Chen Yangmei Li Source Type: research

Small molecules targeting canonical transient receptor potential channels: an update
Drug Discov Today. 2024 Mar 19:103951. doi: 10.1016/j.drudis.2024.103951. Online ahead of print.ABSTRACTTransient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different ...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Hua Liu Min Fu Yifan Zhang Qidong You Lei Wang Source Type: research

Peptide-derived ligands for the discovery of safer opioid analgesics
Drug Discov Today. 2024 Mar 19:103950. doi: 10.1016/j.drudis.2024.103950. Online ahead of print.ABSTRACTDrugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the treatment of pain, but activation of MOR with current opioid analgesics also produces harmful side effects, notably physical dependence, addiction, and respiratory depression. Opioid peptides have been accepted as promising candidates for the development of safer and more efficacious analgesics. To develop peptide-based opioid analgesics, strategies such as modification of endogenous opioid peptides, development of multifunctional...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Abbe Eliasof Lee-Yuan Liu-Chen Yangmei Li Source Type: research

Small molecules targeting canonical transient receptor potential channels: an update
Drug Discov Today. 2024 Mar 19:103951. doi: 10.1016/j.drudis.2024.103951. Online ahead of print.ABSTRACTTransient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different ...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Hua Liu Min Fu Yifan Zhang Qidong You Lei Wang Source Type: research

Peptide-derived ligands for the discovery of safer opioid analgesics
Drug Discov Today. 2024 Mar 19:103950. doi: 10.1016/j.drudis.2024.103950. Online ahead of print.ABSTRACTDrugs targeting the μ-opioid receptor (MOR) remain the most efficacious analgesics for the treatment of pain, but activation of MOR with current opioid analgesics also produces harmful side effects, notably physical dependence, addiction, and respiratory depression. Opioid peptides have been accepted as promising candidates for the development of safer and more efficacious analgesics. To develop peptide-based opioid analgesics, strategies such as modification of endogenous opioid peptides, development of multifunctional...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Abbe Eliasof Lee-Yuan Liu-Chen Yangmei Li Source Type: research

Small molecules targeting canonical transient receptor potential channels: an update
Drug Discov Today. 2024 Mar 19:103951. doi: 10.1016/j.drudis.2024.103951. Online ahead of print.ABSTRACTTransient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different ...
Source: Drug Discovery Today - March 21, 2024 Category: Drugs & Pharmacology Authors: Hua Liu Min Fu Yifan Zhang Qidong You Lei Wang Source Type: research

Accelerating drug development at Bristol Myers Squibb through innovation
Drug Discov Today. 2024 Mar 18:103952. doi: 10.1016/j.drudis.2024.103952. Online ahead of print.ABSTRACTThis paper focuses on the use of novel technologies and innovative trial designs to accelerate evidence generation and increase pharmaceutical Research and Development (R&D) productivity, at Bristol Myers Squibb. We summarize learnings with case examples, on how we prepared and continuously evolved to address the increasing cost, complexities, and external pressures in drug development, to bring innovative medicines to patients much faster. These learnings were based on review of internal efforts toward accelerating ...
Source: Drug Discovery Today - March 20, 2024 Category: Drugs & Pharmacology Authors: Kalyanee Viraswami-Appanna Joan Buenconsejo Charlotte Baidoo Ivan Chan Daniel Li Mariann Micsinai-Balan Ram Tiwari Ling Yang Venkat Sethuraman Source Type: research

Best practices for managing and disseminating resources and outreach and evaluating the impact of the IDG Consortium
Drug Discov Today. 2024 Mar 18:103953. doi: 10.1016/j.drudis.2024.103953. Online ahead of print.ABSTRACTThe Illuminating the Druggable Genome (IDG) consortium generated reagents, biological model systems, data, informatic databases, and computational tools. The Resource Dissemination and Outreach Center (RDOC) played a central administrative role, organized internal meetings, fostered collaboration, and coordinated consortium-wide efforts. The RDOC developed and deployed a Resource Management System (RMS) to enable efficient workflows for collecting, accessing, validating, registering, and publishing resource metadata. IDG...
Source: Drug Discovery Today - March 20, 2024 Category: Drugs & Pharmacology Authors: Du šica Vidović Anna Waller Jayme Holmes Larry A Sklar Stephan C Sch ürer Source Type: research

Rare diseases and pyruvate kinase M2: a promising therapeutic connection
Drug Discov Today. 2024 Mar 14:103949. doi: 10.1016/j.drudis.2024.103949. Online ahead of print.ABSTRACTPyruvate kinase M2 (PKM2) is a key glycolytic enzyme that regulates proliferating cell metabolism. The role of PKM2 in common diseases has been well established, but its role in rare diseases (RDs) is less well understood. Over the past few years, PKM2 has emerged as a crucial player in RDs, including, neoplastic, respiratory, metabolic, and neurological disorders. Herein, we summarize recent findings and developments highlighting PKM2 as an emerging key player in RDs. We also discuss the current status of PKM2 modulatio...
Source: Drug Discovery Today - March 16, 2024 Category: Drugs & Pharmacology Authors: Saumya Kapoor Vaishnavi Kalmegh Hemant Kumar Amit Mandoli Amit Shard Source Type: research

Rare diseases and pyruvate kinase M2: a promising therapeutic connection
Drug Discov Today. 2024 Mar 14:103949. doi: 10.1016/j.drudis.2024.103949. Online ahead of print.ABSTRACTPyruvate kinase M2 (PKM2) is a key glycolytic enzyme that regulates proliferating cell metabolism. The role of PKM2 in common diseases has been well established, but its role in rare diseases (RDs) is less well understood. Over the past few years, PKM2 has emerged as a crucial player in RDs, including, neoplastic, respiratory, metabolic, and neurological disorders. Herein, we summarize recent findings and developments highlighting PKM2 as an emerging key player in RDs. We also discuss the current status of PKM2 modulatio...
Source: Drug Discovery Today - March 16, 2024 Category: Drugs & Pharmacology Authors: Saumya Kapoor Vaishnavi Kalmegh Hemant Kumar Amit Mandoli Amit Shard Source Type: research