Bennett Ma
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View article: P10.05.B RECAPITULATING PATIENT BIOLOGY IN EX VIVO MODELS: A SCRNASEQ ANALYSIS OF THE BLOOD-BRAIN-TUMOR BARRIER IN PEDIATRIC DIFFUSE MIDLINE GLIOMA
P10.05.B RECAPITULATING PATIENT BIOLOGY IN EX VIVO MODELS: A SCRNASEQ ANALYSIS OF THE BLOOD-BRAIN-TUMOR BARRIER IN PEDIATRIC DIFFUSE MIDLINE GLIOMA Open
BACKGROUND Diffuse midline glioma (DMG) is a highly lethal brain tumor in children with limited treatment options. The blood-brain-barrier (BBB) remains a key challenge for therapeutics, preventing most drugs from entering brain tissue. Ch…
View article: Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia Open
PDE10A is an important regulator of striatal signaling that, when inhibited, can normalize dysfunctional activity. Given the involvement of dysfunctional striatal activity with schizophrenia, PDE10A inhibition represents a potentially nove…
View article: Characterization of the absorption, metabolism, excretion, and mass balance of gefapixant in humans
Characterization of the absorption, metabolism, excretion, and mass balance of gefapixant in humans Open
Gefapixant (MK‐7264) is a first‐in‐class, selective antagonist of the P2X3 purinergic receptor currently being investigated as a therapeutic agent for the treatment of refractory or unexplained chronic cough. In non‐clinical studies, gefap…
View article: Assessment of Pharmacokinetic Interaction Between Gefapixant (MK‐7264), a P2X3 Receptor Antagonist, and the OATP1B1 Drug Transporter Substrate Pitavastatin
Assessment of Pharmacokinetic Interaction Between Gefapixant (MK‐7264), a P2X3 Receptor Antagonist, and the OATP1B1 Drug Transporter Substrate Pitavastatin Open
Gefapixant (MK‐7264, AF‐219), a first‐in‐class P2X3 antagonist, is being developed as oral treatment for refractory or unexplained chronic cough. Based on in vitro data, gefapixant exerts inhibitory activity on the organic anion transporte…
View article: Suppression of cathepsin K biomarker in synovial fluid as a free-drug–driven process
Suppression of cathepsin K biomarker in synovial fluid as a free-drug–driven process Open
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View article: Suppression of cathepsin K biomarker in synovial fluid as a free-drug–driven process
Suppression of cathepsin K biomarker in synovial fluid as a free-drug–driven process Open
Cathepsin K (CatK) inhibitors exhibited chondroprotective and pain-reducing effects in animal models, however, improvements were relatively modest at dose levels achieving maximal suppression of CatK biomarkers in urine. In this report, a …