Bioisosteres of the phenyl ring: recent strategic applications in lead optimization and drug design

MAM Subbaiah, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …

Nanomedicine for increasing the oral bioavailability of cancer treatments

A Parodi, P Buzaeva, D Nigovora, A Baldin… - Journal of …, 2021 - Springer
Oral administration is an appealing route of delivering cancer treatments. However, the
gastrointestinal tract is characterized by specific and efficient physical, chemical, and …

[HTML][HTML] Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five

S Stegemann, C Moreton, S Svanbäck, K Box… - Drug Discovery …, 2023 - Elsevier
Highlights•Orally delivered drug products gradually continue to exceed the Rule-of-five on
Molecular Weight and clogP.•New predictive descriptors and tools, advanced chemistry and …

Drug-drug interactions that alter the exposure of glucuronidated drugs: Scope, UDP-glucuronosyltransferase (UGT) enzyme selectivity, mechanisms (inhibition and …

JO Miners, TM Polasek, JA Hulin, A Rowland… - Pharmacology & …, 2023 - Elsevier
Drug-drug interactions (DDIs) arising from the perturbation of drug metabolising enzyme
activities represent both a clinical problem and a potential economic loss for the …

Supporting gut health with medicinal cannabis in people with advanced cancer: potential benefits and challenges

HR Wardill, LT Wooley, OM Bellas, K Cao… - British Journal of …, 2024 - nature.com
The side effects of cancer therapy continue to cause significant health and cost burden to the
patient, their friends and family, and governments. A major barrier in the way in which these …

Inhibition of human UDP-glucuronosyltransferase enzymes by lapatinib, pazopanib, regorafenib and sorafenib: implications for hyperbilirubinemia

JO Miners, N Chau, A Rowland, K Burns… - Biochemical …, 2017 - Elsevier
Kinase inhibitors (KIs) are a rapidly expanding class of drugs used primarily for the treatment
of cancer. Data relating to the inhibition of UDP-glucuronosyltransferase (UGT) enzymes by …

Electronic medical record‐integrated pharmacogenomics and related clinical decision support concepts

PJ Caraballo, SJ Bielinski, JL St. Sauver… - Clinical …, 2017 - Wiley Online Library
Advances in pharmacogenomics (PGx) have the potential to transform healthcare by
allowing precision medicine to become a reality. However, PGx knowledge is new, complex …

CORAL: Monte Carlo based global QSAR modelling of Bruton tyrosine kinase inhibitors using hybrid descriptors

S Ahmadi, S Lotfi, S Afshari, P Kumar… - SAR and QSAR in …, 2021 - Taylor & Francis
Global QSAR modelling was performed to predict the pIC50 values of 233 diverse
heterocyclic compounds as BTK inhibitors with the Monte Carlo algorithm of CORAL …

Role of extracellular vesicles in the pathophysiology, diagnosis and tracking of non-alcoholic fatty liver disease

LA Newman, MJ Sorich, A Rowland - Journal of Clinical Medicine, 2020 - mdpi.com
Non-alcoholic fatty liver disease (NAFLD) is the most common chronic liver disease,
affecting approximately one-third of the global population. Most affected individuals …

Solid lipid nanoparticles for efficient oral delivery of tyrosine kinase inhibitors: a nano targeted cancer drug delivery

S Satapathy, CS Patro - Advanced pharmaceutical bulletin, 2021 - pmc.ncbi.nlm.nih.gov
Tyrosine kinase inhibitors (TKIs) are used as targeted therapy for cancer by inhibiting the
signaling pathway and tumor growth. Many TKIs got approved by FDA in recent times for the …