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Topic Review
Delivery Systems for Nucleic Acids/Proteins
Gene therapy has been used as a potential approach to address the diagnosis and treatment of genetic diseases and inherited disorders. In this line, non-viral systems have been exploited as promising alternatives for delivering therapeutic transgenes and proteins. In this entry, we explored how biological barriers are effectively overcome by non-viral systems, usually nanoparticles, to reach an efficient delivery of cargoes.
  • 730
  • 31 Mar 2021
Topic Review
Delpazolid for Tuberculosis Treatment
A novel oxazolidinone with cyclic amidrazone, delpazolid (LCB01-0371), was synthesized by LegoChem BioSciences, Inc. (Daejeon, Korea). Delpazolid can improve the minimum bactericidal concentration of Mycobacterium tuberculosis H37Rv and significantly reduce resistance rates,especially of multi-drug-resistant tuberculosis (MDR-TB) isolates, compared with linezolid. Therefore, delpazolid can be used to treat MDR-TB. The safety, tolerability, and pharmacokinetics of delpazolid have been evaluated in a phase 1 clinical trial, which revealed that it does not cause adverse events such as myelosuppression even after three weeks of repeated dosing. 
  • 932
  • 29 Oct 2020
Topic Review
Development and Regulatory Approval of Biosimilars
Biological therapies have transformed high-burden treatments. As the patent and exclusivity period for biological medicines draws to a close, there is a possibility for the development and authorization of biosimilars. These products boast comparable levels of safety, quality, and effectiveness to their precursor reference products. Biosimilars, although similar to reference products, are not identical copies and should not be considered generic substitutes for the original. Their development and evaluation involve a rigorous step-by-step process that includes analytical, functional, and nonclinical evaluations and clinical trials. Clinical studies conducted for biosimilars aim to establish similar efficacy, safety, and immunogenicity, rather than demonstrating a clinical benefit, as with the reference product. 
  • 119
  • 29 Feb 2024
Topic Review
Development of Agents with Biological Activities by Umbelliferone
Umbelliferone (UMB), known as 7-hydroxycoumarin, hydrangine, or skimmetine, is a naturally occurring coumarin in the plant kingdom, mainly from the Umbelliferae family that possesses a wide variety of pharmacological properties. In addition, the use of nanoparticles containing umbelliferone may improve anti-inflammatory or anticancer therapy. Also, its derivatives are endowed with great potential for therapeutic applications due to their broad spectrum of biological activities such as anti-inflammatory, antioxidant, neuroprotective, antipsychotic, antiepileptic, antidiabetic, antimicrobial, antiviral, and antiproliferative effects.
  • 302
  • 22 Dec 2023
Topic Review
Development of Nitroheterocyclic Drugs against Trypanosomes
Human African Trypanosomiasis (HAT), commonly called sleeping sickness, is a zoonotic disease caused by different subspecies of the bloodstream parasite T. brucei and transmitted by the Glossina tsetse fly. Nitroaromatic rings are privileged pharmacophores of many antimicrobials in clinical use, including antifungal and antiparasitic drugs.
  • 289
  • 10 Apr 2023
Topic Review
Development of Peptide Biopharmaceuticals
Peptides are low-molecular-weight substances that participate in numerous important physiological functions, such as human growth and development, stress, regulation of the emotional state, sexual behavior, and immune responses. Their mechanisms of action are based on receptor–ligand interactions, which result in highly selective effects. These properties and low toxicity enable them to be considered potent drugs. Peptide preparations became possible at the beginning of the 20th century after a method was developed for selectively synthesizing peptides; however, after synthesis of the first peptide drugs, several issues related to increasing the stability, bioavailability, half-life, and ability to move across cell membranes remain unresolved. 
  • 463
  • 07 Apr 2022
Topic Review
Development of Trichosanthin
Tian Hua Fen, a herbal powder extract that contains trichosanthin (TCS), was used as an abortifacient in traditional Chinese medicine. In 1972, TCS was purified to alleviate the side effects. Because of its clinical applications, TCS became one of the most active research areas in the 1960s to the 1980s in China. These include obtaining the sequence information in the 1980s and the crystal structure in 1995. The replication block of TCS on human immunodeficiency virus in lymphocytes and macrophages was found in 1989 and started a new chapter of its development.
  • 618
  • 21 Mar 2022
Topic Review
Developments on 14-Oxygenated-N-methylmorphinan-6-ones
Adequate pain management, particularly chronic pain, remains a major challenge associated with modern-day medicine. Current pharmacotherapy offers unsatisfactory long-term solutions due to serious side effects related to the chronic administration of analgesic drugs. Morphine and structurally related derivatives (e.g., oxycodone, oxymorphone, buprenorphine) are highly effective opioid analgesics, mediating their effects via the activation of opioid receptors, with the mu-opioid receptor subtype as the primary molecular target. However, they also cause addiction and overdose deaths, which has led to a global opioid crisis in the last decades. Therefore, research efforts are needed to overcome the limitations of present pain therapies with the aim to improve treatment efficacy and to reduce complications.
  • 379
  • 30 Sep 2021
Topic Review
Dexibuprofen
S-(+) enantiomer of ibuprofen (IBU) dexibuprofen (DXI) is known to be more potent than its R-(−) form and exhibits many advantages over the racemic mixture of IBU such as lower toxicity, greater clinical efficacy, and lesser variability in therapeutic effects. Moreover, DXI potential has been recently advocated to reduce cancer development and prevent the development of neurodegenerative diseases in addition to its anti-inflammatory properties. 
  • 1.8K
  • 23 Jun 2021
Topic Review
Diabetic Micro-Complication Management—Diabetic Neuropathy
The progression of diabetes leads to macro and microvascular complications, including diabetic neuropathy, which is the most prevalent microvascular complication with diabetes. Clinical manifestations of diabetic neuropathy begin with the loss of distal sensory function, pain, and substantial morbidity.
  • 550
  • 11 Nov 2021
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