Search Results - "DOWTY, Martin"
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The pharmacokinetics, metabolism, and clearance mechanisms of tofacitinib, a janus kinase inhibitor, in humans
Published in Drug metabolism and disposition (01-04-2014)“…Tofacitinib is a novel, oral Janus kinase inhibitor. The objectives of this study were to summarize the pharmacokinetics and metabolism of tofacitinib in…”
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Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis
Published in Journal of inflammation (London, England) (11-08-2010)“…The Janus kinase (JAK) family of tyrosine kinases includes JAK1, JAK2, JAK3 and TYK2, and is required for signaling through Type I and Type II cytokine…”
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The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis
Published in Clinical and experimental rheumatology (01-03-2016)“…Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease characterised by infiltration of immune cells into the affected synovium, release of…”
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Effects of Hepatic Impairment on the Pharmacokinetics of Abrocitinib and Its Metabolites
Published in Journal of clinical pharmacology (01-10-2021)“…Abrocitinib, an oral once‐daily Janus kinase 1 selective inhibitor, is under development for treatment of atopic dermatitis. This phase 1, nonrandomized,…”
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Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure and Support Dosing Recommendations for Potential Drug‐Drug Interactions or in Special Populations: An Example Using Tofacitinib
Published in Journal of clinical pharmacology (01-12-2020)“…Tofacitinib is an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. It is eliminated via…”
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Virtual Bioequivalence Assessment of Ritlecitinib Capsules with Incorporation of Observed Clinical Variability Using a Physiologically Based Pharmacokinetic Model
Published in The AAPS journal (24-01-2024)“…Ritlecitinib, an orally available Janus kinase 3 and tyrosine kinase inhibitor being developed for the treatment of alopecia areata (AA), is highly soluble…”
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Ritlecitinib and brepocitinib demonstrate significant improvement in scalp alopecia areata biomarkers
Published in Journal of allergy and clinical immunology (01-04-2022)“…Janus kinase (JAK) inhibitors have shown encouraging results in the treatment of alopecia areata (AA), an autoimmune form of hair loss, in small, uncontrolled…”
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Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1‑((2S,5R)‑5-((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Published in Journal of medicinal chemistry (09-03-2017)“…Significant work has been dedicated to the discovery of JAK kinase inhibitors resulting in several compounds entering clinical development and two FDA approved…”
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Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550)
Published in The Journal of immunology (1950) (01-04-2011)“…Inhibitors of the JAK family of nonreceptor tyrosine kinases have demonstrated clinical efficacy in rheumatoid arthritis and other inflammatory disorders;…”
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The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF‐06700841) in Healthy Subjects and Patients With Plaque Psoriasis
Published in Journal of clinical pharmacology (01-04-2018)“…The safety, tolerability, pharmacokinetics, and pharmacodynamics of PF‐06700841 were assessed in a randomized, double‐blind, placebo‐controlled, single‐ and…”
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Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis
Published in The Journal of pharmacology and experimental therapeutics (01-01-2014)“…A critical piece in the translation of preclinical studies to clinical trials is the determination of dosing regimens that allow maximum therapeutic benefit…”
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A phase 1 study to investigate the absorption, distribution, metabolism and excretion of brepocitinib in healthy males using a 14 C-microdose approach
Published in British journal of clinical pharmacology (01-10-2023)“…Brepocitinib is a tyrosine kinase 2/Janus kinase 1 inhibitor being investigated for the treatment of several autoimmune diseases. This study assessed the…”
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Integrating Clinical Variability into PBPK Models for Virtual Bioequivalence of Single and Multiple Doses of Tofacitinib Modified‐Release Dosage Form
Published in Clinical pharmacology and therapeutics (01-10-2024)“…Tofacitinib is a potent, selective inhibitor of the Janus kinase (JAK) family of kinases with a high degree of selectivity within the human genome's set of…”
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
Published in Journal of medicinal chemistry (08-02-2018)“…Janus kinases (JAKs) are intracellular tyrosine kinases that mediate the signaling of numerous cytokines and growth factors involved in the regulation of…”
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The Metabolism and Disposition of Brepocitinib in Humans and Characterization of the Formation Mechanism of an Aminopyridine Metabolite
Published in Drug metabolism and disposition (17-06-2024)“…Brepocitinib is an oral once-daily Janus kinase 1 and Tyrosine kinase 2 selective inhibitor currently in development for the treatment of several autoimmune…”
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Effects of Renal Impairment on the Pharmacokinetics of Abrocitinib and Its Metabolites
Published in Journal of clinical pharmacology (01-04-2022)“…Abrocitinib, an oral once‐daily Janus kinase 1 selective inhibitor, is under development for the treatment of atopic dermatitis. This phase 1, nonrandomized,…”
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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases
Published in Journal of medicinal chemistry (25-11-2020)“…Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type…”
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Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition
Published in ACS chemical biology (16-12-2016)“…PF-06651600, a newly discovered potent JAK3-selective inhibitor, is highly efficacious at inhibiting γc cytokine signaling, which is dependent on both JAK1 and…”
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The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Abrocitinib, a Selective Janus Kinase Inhibitor, in Humans
Published in Drug metabolism and disposition (01-08-2022)“…Abrocitinib is an oral once-daily Janus kinase 1 selective inhibitor being developed for the treatment of moderate-to-severe atopic dermatitis. This study…”
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