[HTML][HTML] Deuterium in drug discovery: progress, opportunities and challenges

RMC Di Martino, BD Maxwell, T Pirali - Nature Reviews Drug Discovery, 2023 - nature.com
Substitution of a hydrogen atom with its heavy isotope deuterium entails the addition of one
neutron to a molecule. Despite being a subtle change, this structural modification, known as …

US FDA approved drugs from 2015–June 2020: a perspective

P Bhutani, G Joshi, N Raja, N Bachhav… - Journal of Medicinal …, 2021 - ACS Publications
In the present work, we report compilation and analysis of 245 drugs, including small and
macromolecules approved by the US FDA from 2015 until June 2020. Nearly 29% of the …

[HTML][HTML] Deucravacitinib versus placebo and apremilast in moderate to severe plaque psoriasis: Efficacy and safety results from the 52-week, randomized, double …

B Strober, D Thaçi, H Sofen, L Kircik, KB Gordon… - Journal of the American …, 2023 - Elsevier
Background Deucravacitinib, an oral, selective, allosteric tyrosine kinase 2 inhibitor, inhibits
cytokine signaling in psoriasis pathogenesis. Objective The objective of this study was to …

Therapeutics targeting the IL-23 and IL-17 pathway in psoriasis

K Ghoreschi, A Balato, C Enerbäck, R Sabat - The Lancet, 2021 - thelancet.com
Psoriasis is a chronic inflammatory disease characterised by sharply demarcated
erythematous and scaly skin lesions accompanied by systemic manifestations. Classified by …

[HTML][HTML] A comprehensive overview of globally approved JAK inhibitors

AM Shawky, FA Almalki, AN Abdalla, AH Abdelazeem… - Pharmaceutics, 2022 - mdpi.com
Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes
four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling …

Selective inhibitors of JAK1 targeting an isoform-restricted allosteric cysteine

ME Kavanagh, BD Horning, R Khattri, N Roy… - Nature chemical …, 2022 - nature.com
The Janus tyrosine kinase (JAK) family of non-receptor tyrosine kinases includes four
isoforms (JAK1, JAK2, JAK3, and TYK2) and is responsible for signal transduction …

[HTML][HTML] Protein kinases: drug targets for immunological disorders

L Castelo-Soccio, H Kim, M Gadina… - Nature Reviews …, 2023 - nature.com
Protein kinases play a major role in cellular activation processes, including signal
transduction by diverse immunoreceptors. Given their roles in cell growth and death and in …

hERG toxicity assessment: Useful guidelines for drug design

A Garrido, A Lepailleur, SM Mignani… - European journal of …, 2020 - Elsevier
All along the drug development process, one of the most frequent adverse side effects,
leading to the failure of drugs, is the cardiac arrhythmias. Such failure is mostly related to the …

[HTML][HTML] Deucravacitinib is an allosteric TYK2 protein kinase inhibitor FDA-approved for the treatment of psoriasis

R Roskoski Jr - Pharmacological research, 2023 - Elsevier
Psoriasis is a heterogeneous, inflammatory, autoimmune skin disease that affects up to 2%
of the world's population. There are many treatment modalities including topical medicines …

[HTML][HTML] Deucravacitinib for the treatment of psoriatic disease

AM Lé, L Puig, T Torres - American Journal of Clinical Dermatology, 2022 - Springer
Psoriasis is an immune-mediated disease, with the interleukin (IL)-23/IL-17 axis currently
considered its main pathogenic pathway. Tyrosine kinase 2 (TYK2) is responsible for …