[HTML][HTML] Why 90% of clinical drug development fails and how to improve it?

D Sun, W Gao, H Hu, S Zhou - Acta Pharmaceutica Sinica B, 2022 - Elsevier
Ninety percent of clinical drug development fails despite implementation of many successful
strategies, which raised the question whether certain aspects in target validation and drug …

[HTML][HTML] Blood-brain barrier permeability following conventional photon radiotherapy–A systematic review and meta-analysis of clinical and preclinical studies

Z Odé, MPP Derieppe, L Groenink… - Clinical and …, 2022 - Elsevier
Radiotherapy (RT) is a cornerstone treatment strategy for brain tumours. Besides
cytotoxicity, RT can cause disruption of the blood–brain barrier (BBB), resulting in an …

Study of Carbamoyl Fluoride: Synthesis, Properties and Applications

C Bonnefoy, E Chefdeville, C Tourvieille… - … A European Journal, 2022 - Wiley Online Library
Carbamoyl fluoride is a fluorinated group that, to this date, remains underexplored, probably
due to the lack of data concerning its properties. In this paper, a study of carbamoyl fluoride …

The Future of (Radio)‐Labeled Compounds in Research and Development within the Life Science Industry

V Derdau, CS Elmore, T Hartung… - Angewandte Chemie …, 2023 - Wiley Online Library
In this review the applications of isotopically labeled compounds are discussed and put into
the context of their future impact in the life sciences. Especially discussing their use in the …

New Long-Acting [89Zr]Zr-DFO GLP-1 PET Tracers with Increased Molar Activity and Reduced Kidney Accumulation

J Wilbs, R Raavé, M Boswinkel, T Glendorf… - Journal of Medicinal …, 2023 - ACS Publications
Positron emission tomography (PET) imaging is used in drug development to noninvasively
measure biodistribution and receptor occupancy. Ideally, PET tracers retain target binding …

Strategies for designing novel positron emission tomography (PET) radiotracers to cross the blood–brain barrier

A Lindberg, M Chassé, C Varlow… - Journal of Labelled …, 2023 - Wiley Online Library
Positron emission tomography (PET) is a powerful tool for imaging biological processes in
the central nervous system (CNS). Designing PET radiotracers capable of crossing the …

Broad‐scope Syntheses of [11C/18F]Trifluoromethylarenes from Aryl(mesityl)iodonium Salts

S Telu, S Jana, MB Haskali… - … A European Journal, 2023 - Wiley Online Library
Efficient methods for labeling aryl trifluoromethyl groups to provide novel radiotracers for use
in biomedical research with positron emission tomography (PET) are keenly sought. We …

EFMC: Trends in Medicinal Chemistry and Chemical Biology

YP Auberson, PB Arimondo, M Duca, S Essig… - …, 2023 - Wiley Online Library
Ground‐breaking research in disease biology and continuous efforts in method
development have uncovered a range of potential new drug targets. Increasingly, the drug …

[HTML][HTML] Structure‒tissue exposure/selectivity relationship (STR) correlates with clinical efficacy/safety

W Gao, H Hu, L Dai, M He, H Yuan, H Zhang… - … Pharmaceutica Sinica B, 2022 - Elsevier
Drug optimization, which improves drug potency/specificity by structure‒activity relationship
(SAR) and drug-like properties, is rigorously performed to select drug candidates for clinical …

Synthesis and Preclinical Positron Emission Tomography Imaging of the p38 MAPK Inhibitor [11C]Talmapimod: Effects of Drug Efflux and Sex Differences

M Chassé, N Vasdev - ACS Chemical Neuroscience, 2023 - ACS Publications
Stress-activated kinases are targets of interest in neurodegenerative disease due to their
involvement in inflammatory signaling and synaptic dysfunction. The p38α kinase has …