Trial reportClinical drug investigation2017
Pharmacokinetics, Pharmacodynamics, and Safety of Entospletinib, a Novel pSYK Inhibitor, Following Single and Multiple Oral Dosing in Healthy Volunteers.
Trial report in Clinical drug investigation, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
9 citing papers in PubMed, 25 citations in OpenAlex.
- Kinetics of basophil hyporesponsiveness during short-course peanut oral immunotherapy.The Journal of allergy and clinical immunology · 2022Trial
- The spleen tyrosine kinase inhibitor entospletinib resolves inflammation to promote repair following acute kidney injury.JCI insight · 2025Article
- Identification of new drugs to counteract anti-spike IgG-induced hyperinflammation in severe COVID-19.Life science alliance · 2023Article
- Src- and Abl-family kinases activate spleen tyrosine kinase to maximize phagocytosis and Leishmania infection.Journal of cell science · 2023Article
- Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.ACS medicinal chemistry letters · 2020Article
- Evaluating emtricitabine + rilpivirine + tenofovir alafenamide in combination for the treatment of HIV-infection.Expert opinion on pharmacotherapy · 2020Review
- Resistance Mechanisms to SYK Inhibition in Acute Myeloid Leukemia.Cancer discovery · 2020Article
- SYK inhibitor entospletinib prevents ocular and skin GVHD in mice.JCI insight · 2018Article
- Targeting the B cell receptor pathway in non-Hodgkin lymphoma.Expert opinion on investigational drugs · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesEntospletinib is a selective, reversible, adenosine triphosphate-competitive small-molecule spleen tyrosine kinase (SYK) inhibitor that blocks B cell receptor-mediated signaling and proliferation in B lymphocytes. This study evaluated the safety, pharmacokinetics, and pharmacodynamics of entospletinib in a double-blind, single/multiple ascending dose study in healthy volunteers.
methodsIn sequential cohorts, 120 subjects received entospletinib (25-1200 mg; fasted) as single or twice-daily oral doses for 7 days. Along with pharmacokinetics, the study assessed functional inhibition of ex vivo anti-immunoglobulin E-stimulated CD63 expression on basophils and pervanadate-evoked phosphorylated SYK (pSYK) Y525. Safety and tolerability were assessed throughout the study.
resultsEntospletinib was generally well-tolerated over a 48-fold dose range. Adverse events (AEs) were generally mild to moderate, with no AE-driven study drug discontinuations noted. Entospletinib displayed a median plasma half-life of 9-15 h; entospletinib exposures reached a plateau at ≥600 mg twice daily (likely due to solubility-limited absorption) and provided >90% CD63 inhibition at peak concentrations and >60% inhibition at trough concentrations (corresponding pSYK inhibition of >70 and >50%).
conclusionThe overall safety, pharmacokinetics, and pharmacodynamics profiles of entospletinib support further clinical evaluation.
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