Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

The role of JAK/STAT signaling pathway and its inhibitors in diseases

P Xin, X Xu, C Deng, S Liu, Y Wang, X Zhou… - International …, 2020 - Elsevier
The JAK/STAT signaling pathway is an universally expressed intracellular signal
transduction pathway and involved in many crucial biological processes, including cell …

Neutrophils as emerging therapeutic targets

T Németh, M Sperandio, A Mócsai - Nature reviews Drug discovery, 2020 - nature.com
Neutrophils are the most abundant circulating leukocytes, being the first line of defence
against bacterial and fungal infections. However, neutrophils also contribute to tissue …

Diagnosis and management of rheumatoid arthritis: a review

D Aletaha, JS Smolen - Jama, 2018 - jamanetwork.com
Importance Rheumatoid arthritis (RA) occurs in about 5 per 1000 people and can lead to
severe joint damage and disability. Significant progress has been made over the past 2 …

Baricitinib restrains the immune dysregulation in patients with severe COVID-19

V Bronte, S Ugel, E Tinazzi, A Vella… - The Journal of …, 2020 - Am Soc Clin Investig
BACKGROUND Patients with coronavirus disease 2019 (COVID-19) develop pneumonia
generally associated with lymphopenia and a severe inflammatory response due to …

[HTML][HTML] Biologics vs. small molecules: Drug costs and patient access

FD Makurvet - Medicine in Drug Discovery, 2021 - Elsevier
Significant advances in drug research and development are herein reviewed first to set the
background for a critical consideration of the economic sustainability of biologics and small …

JAK inhibition reduces SARS-CoV-2 liver infectivity and modulates inflammatory responses to reduce morbidity and mortality

J Stebbing, G Sánchez Nievas, M Falcone… - Science …, 2021 - science.org
Using AI, we identified baricitinib as having antiviral and anticytokine efficacy. We now show
a 71%(95% CI 0.15 to 0.58) mortality benefit in 83 patients with moderate-severe SARS-CoV …

[HTML][HTML] C-reactive protein and implications in rheumatoid arthritis and associated comorbidities

JE Pope, EH Choy - Seminars in arthritis and rheumatism, 2021 - Elsevier
C-reactive protein (CRP) is routinely assessed as a marker of systemic inflammation in
rheumatoid arthritis (RA). However, it is also an immune regulator that plays an important …

JAK inhibition as a therapeutic strategy for immune and inflammatory diseases

DM Schwartz, Y Kanno, A Villarino, M Ward… - Nature reviews Drug …, 2017 - nature.com
The discovery of cytokines as key drivers of immune-mediated diseases has spurred efforts
to target their associated signalling pathways. Janus kinases (JAKs) are essential signalling …

Upadacitinib versus placebo or adalimumab in patients with rheumatoid arthritis and an inadequate response to methotrexate: results of a phase III, double‐blind …

R Fleischmann, AL Pangan, IH Song… - Arthritis & …, 2019 - Wiley Online Library
Objective To evaluate the efficacy, including capacity for inhibition of radiographic
progression, and safety of upadacitinib, a JAK 1‐selective inhibitor, as compared to placebo …