Preferential Inhibition of JAK1 Relative to JAK3 by Upadacitinib: Exposure‐Response Analyses of Ex Vivo Data From 2 Phase 1 Clinical Trials and Comparison to Tofacitinib - Mohamed, Mohamed‐Eslam F.; Beck, Denise; Camp, Heidi S.; Othman, Ahmed A. (Journal of clinical pharmacology, 2020)
Keywords: Adolescent; Adult; Arthritis, Rheumatoid - drug therapy; Clinical Trials, Phase I as Topic; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Healthy Volunteers; Heterocyclic Compounds, 3-Ring - administration & dosage; Heterocyclic Compounds, 3-Ring - pharmacokinetics; Heterocyclic Compounds, 3-Ring - pharmacology; Heterocyclic Compounds, 3-Ring - therapeutic use; Humans; IL‐6; IL‐7; JAK1; JAK3; Janus kinase; Janus Kinase 1 - antagonists & inhibitors; Janus Kinase 3 - antagonists & inhibitors; Male; Middle Aged; Models, Biological; Phosphorylation - drug effects; Piperidines - administration & dosage; Piperidines - pharmacokinetics; Piperidines - pharmacology; Piperidines - therapeutic use; Protein Kinase Inhibitors - administration & dosage; Protein Kinase Inhibitors - pharmacokinetics; Protein Kinase Inhibitors - pharmacology; Protein Kinase Inhibitors - therapeutic use; Pyrimidines - administration & dosage; Pyrimidines - pharmacokinetics; Pyrimidines - pharmacology; Pyrimidines - therapeutic use; rheumatoid arthritis; STAT3; STAT3 Transcription Factor - drug effects; STAT3 Transcription Factor - metabolism; STAT5; STAT5 Transcription Factor - drug effects; STAT5 Transcription Factor - metabolism; target engagement; tofacitinib; upadacitinib; Young Adult; upadacitinib; STAT3; Janus kinase; STAT5; target engagement; JAK3; rheumatoid arthritis; IL-6; IL-7; JAK1; tofacitinib