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The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans
TLDR
The results indicate that SB‐705498, at a clinically safe and well‐tolerated dose, has target‐specific pharmacodynamic activity in humans, and provide the first clinical evidence that a TRPV1 antagonist may alleviate pain and hyperalgesia associated with inflammation and tissue injury.
Safety, Pharmacokinetic, and Functional Effects of the Nogo-A Monoclonal Antibody in Amyotrophic Lateral Sclerosis: A Randomized, First-In-Human Clinical Trial
TLDR
Safety, pharmacokinetics, and functional effects of ozanezumab, a humanized monoclonal antibody against Nogo-A were well tolerated and co-localization at the site of action was demonstrated, supporting future studies with ozaneZumab in ALS.
A Randomized, Controlled Study to Investigate the Analgesic Efficacy of Single Doses of the Cannabinoid Receptor-2 Agonist GW842166, Ibuprofen or Placebo in Patients With Acute Pain Following Third
TLDR
Ibuprofen was significantly more effective than placebo across all endpoints and there was no evidence for any beneficial adjunctive effect after coadministration of rescue analgesia with GW842166.
Systemic Pharmacokinetics, Safety, and Preliminary Efficacy of Topical AhR Agonist Tapinarof: Results of a Phase 1 Study
TLDR
The 1% cream was selected as the concentration for use in future studies because of its lower AE incidence and efficacy comparable to the 2% cream, and the efficacy and safety of 1% tapinarof support results of previous positive studies that used a different formulation.
Analgesic efficacy and safety of the novel p38 MAP kinase inhibitor, losmapimod, in patients with neuropathic pain following peripheral nerve injury: a double‐blind, placebo‐controlled study
TLDR
A double‐blind, placebo‐controlled study was undertaken to evaluate the analgesic efficacy of losmapimod (GW856553), a novel p38α/β inhibitor, in subjects with neuropathic pain following traumatic peripheral nerve injury.
Pharmacokinetics and tolerability of lamotrigine and olanzapine coadministered to healthy subjects.
TLDR
Lamotrigine and olanzapine coadministration in patients who may benefit from the combination was supported by this study, and the possibility exists that the lamotigine dose for some patients may need adjustment to optimize treatment when olanZapine is added to or withdrawn from a regimen including lamotrigines.
Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers
TLDR
The results confirm that the new formulation of sumatriptan and sum atriptan conventional tablets are bioequivalent as demonstrated by the finding that the 90% confidence intervals for the sumatripan area under the concentration time curve to infinity and to the last evaluable time point and maximum plasma concentration fell within the predetermined bounds defining bioequivalence.
Human microdose evaluation of the novel EP1 receptor antagonist GSK269984A.
TLDR
For drug development programmes characterized by inconsistencies between pre-clinical in vitro metabolic and in vivo PK data, and where uncertainty exists with respect to allometric predictions of the human PK profile, these data support the early application of a human microdose study to facilitate the selection of compounds for further clinical development.
A hypersensitivity of glycogen phosphorylase activation in hearts of diabetic rats.
TLDR
Data from this study are consistent with a diabetes-related unmasking of an alpha effect on cardiac phosphorylase activation and an unexplained increase in the sensitivity of phosphory lase kinase activation by protein kinase.
Safety and efficacy of ozanezumab in patients with amyotrophic lateral sclerosis: a randomised, double-blind, placebo-controlled, phase 2 trial
TLDR
Ozanezumab did not show efficacy compared with placebo in patients with ALS, and Nogo-A does not seem to be an effective therapeutic target in ALS.
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