Stuart Mair

Quotient Clinical (United Kingdom)

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Stuart Wood

Pharmaron (United Kingdom)

Iain Shaw

Quotient Clinical (United Kingdom)

Gill Ford

Quotient Clinical (United Kingdom)

Lloyd Stevens

Quotient Clinical (United Kingdom)

Tamás Jordán

IMGENEX India (India)

John McDermott

Manchester University NHS Foundation Trust

Réka Angi

IMGENEX India (India)

László Molnár

University of Sopron

Miguel H. Bronchud

Hospital Universitario Dexeus

Rodeina Challand

BioFactura (United States)

Cooperative Institutions

Quotient Clinical (United Kingdom)

Bristol-Myers Squibb (United States)

AstraZeneca (United Kingdom)

IMGENEX India (India)

University of Florida

Mitsubishi Tanabe Pharma Corporation

Mitsubishi Group (Japan)

BioCryst Pharmaceuticals (United States)

Pfizer (United States)

Ibero American University

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Pemafibrate Has High Bioavailability and is Principally Excreted via the Liver

Atherosclerosis Supplements (2018)

Neil Hounslow Stuart Mair Hideki Suganami Mitsumasa Nakamura

Aliskiren

Renin inhibitor

10.1016/j.atherosclerosissup.2018.04.475

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Citations (16)

Absorption, disposition and metabolic pathway of amiselimod (MT-1303) in healthy volunteers in a mass balance study

Xenobiotica (2018)

Takayuki Kifuji Shinsuke Inoue Megumi Furukawa Begonya Perez Madera Takahiro Goto

The absorption, metabolism and excretion of MT-1303 were investigated in healthy male subjects after a single oral dose of 0.4 mg [14C]-MT-1303 (ClinicalTrials.gov NCT02293967). The MT-1303 concentration in the plasma reached a maximum at 12 h after administration. Thereafter, the concentration declined with a half-life of 451 h. At the final assessment on Day 57, 91.16% of the administered radioactivity was excreted, and the cumulative excretion in the urine and faeces was 35.32% and 55.84%, respectively. The most abundant metabolite in plasma was MT-1303-P, which accounted for 42.6% of the area under the plasma concentration-time curve (AUC) of the total radioactivity. The major component excreted in urine was Human Urine (HU)4 (3066434), accounting for 28.1% of radioactivity in the sample (4.05% of the dose), whereas MT-1303 was a major component in the faeces, accounting for 89.8% of radioactivity in the sample (25.49% of the dose) up to 240 h after administration. This study indicates that multiple metabolic pathways are involved in the elimination of MT-1303 from the human body and the excretion of MT-1303 and MT-1303-P via the kidney is low. Therefore, MT-1303 is unlikely to cause conspicuous drug interactions or alter pharmacokinetics in patients with renal impairment.

10.1080/00498254.2018.1525508

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Citations (7)

The Association for Human Pharmacology in the Pharmaceutical Industry London Meeting 2018: Brexit and Other Challenges in Early Phase Drug Development

Frontiers in Pharmacology (2018)

Susan Reijntjes Muna Albayaty James Bush Joseph Cheriyan Anthea Cromie

The Association for Human Pharmacology in the Pharmaceutical Industry (AHPPI) annual meeting focused on the changing face of early phase drug development and opened with a keynote speech concerning the revolution in pharmaceutical medicine over the last 30 years. Examples were presented of how translational pharmaceutics is being used to tackle the high drug candidate failure rate and is improving productivity when moving drug candidates from the laboratory through to clinical proof of concept. The EU Medicines Agency revised 2007 Risk Mitigation guideline on first in human (FIH) clinical trials was discussed. The focus of the revised guideline, which came into force in February 2018, is on risk mitigation and promotion of safety and will assist drug sponsors with the design and performance of early clinical studies. The use of integrated adaptive protocol designs in early clinical development was discussed in relation to the challenges involved when running early phase clinical trials in patients. The Health Regulatory Authority presented its strategies to ensure that the UK remains an attractive place to conduct Phase I trials. They confirmed that in the event of a 'no deal' Brexit, it is well placed to implement and influence many provisions of the new EU CTR. The meeting provided an opportunity to discuss the changing regulatory environment and the opportunities and challenges facing the UK following Brexit with invited speakers from a range of disciplines including drug development, clinical trials and research organizations, government science policy and regulatory agencies.

Drug Development

Guideline

Promotion (chess)

10.3389/fphar.2018.01301

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Citations (2)

The effects of ulimorelin, a ghrelin agonist, on liquid gastric emptying and colonic transit in humans

Neurogastroenterology & Motility (2020)

J S James Stuart Mair W Döll Erik P. Sandefer David F. Wurtman

Abstract Background Ulimorelin, a small molecule ghrelin agonist and prokinetic agent, was effective in animal models of gastroparesis and delayed transit. However, employing once daily administration, it failed in clinical trials of postoperative ileus (POI), a condition in which colonic motility recovers last. The aim of this study was to evaluate drug dosing and regional differences in drug activity between stomach and colon. Methods Gastric emptying was assessed by scintigraphy in healthy adults at single doses of 600‐1200 µg kg −1 and multiple doses of 80‐600 µg kg −1 Q8H for 7 days. Colonic motility was assessed by 7‐region scintigraphic analysis at a dose of 600 µg kg −1 for 2 days. The primary endpoints were percent change in time to 50% (∆ t 50 ) liquid gastric emptying on Days 1, 4, and 6 and the geometric mean center of colonic transit at 24 hours (GC 24 ). Plasma concentrations of free and total ulimorelin were measured for pharmacokinetic and exposure‐response modeling. Key Results Ulimorelin 150‐600 µg kg −1 every 8 hours resulted in statistically significant improvements (∆ t 50 = 23% to 46% ( P < .05)) in gastric emptying from baseline that were sustained through Day 6. However, no effects on GC 24 were observed. Pharmacokinetic analyses suggested that the free concentrations of ulimorelin achieved in POI trials and dosing frequency may have been inadequate. Conclusions and Inferences Ulimorelin is a potent gastric prokinetic but lacks evidence of activity in the human colon, pointing to the stomach as the predominant site of action of ghrelin in humans; ClinicalTrials.gov NCT02993055.

Prokinetic agent

Gastroparesis

Metoclopramide

Pharmacodynamics

10.1111/nmo.13784

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Citations (10)

Adme Study of [14c] Netupitant Administered as an oral 300 Mg Suspension to Healthy Male Subjects

Annals of Oncology (2012)

Claudio Giuliano Selma Calcagnile Stuart Mair Lloyd Stevens Ian C. T. Nisbet

ADME

10.1016/s0923-7534(20)34121-1

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Citations (0)

Comparison of the pharmacodynamic profiles of a biosimilar filgrastim and Amgen filgrastim: results from a randomized, phase I trial

Annals of Hematology (2010)

Cornelius F. Waller Miguel H. Bronchud Stuart Mair Rodeina Challand

Further to the patent expiry of Neupogen® (Amgen filgrastim), Hospira has developed a biosimilar filgrastim (Nivestim™) that may offer a clinically effective alternative for multiple hematologic and oncologic indications. Here results are reported from a phase I trial, primarily designed to compare the pharmacodynamic profiles of Hospira filgrastim and Amgen filgrastim. A phase I, single-center, double-blind, randomized trial was undertaken to demonstrate equivalence of the pharmacodynamic characteristics of Hospira filgrastim and Amgen filgrastim. Fifty healthy volunteers were randomized to receive 5 or 10 µg/kg dosing, before further randomization to treatment sequence. All volunteers received five daily subcutaneous doses of Hospira filgrastim or Neupogen, with subsequent crossover to the alternative treatment. Bioequivalence was evaluated by analysis of variance; if the estimated 90% confidence intervals (CIs) for the ratio of 'test' to 'reference' treatment means were within the conventional equivalence limits of 0.80–1.25, then bioequivalence was concluded. Forty-eight volunteers completed the study. Geometric mean absolute neutrophil count area under the curve from time 0 to the last time point at day 5 (primary endpoint) was comparable in volunteers given Hospira filgrastim or Amgen filgrastim at 5 µg/kg (ratio of means, 0.98; 90% CI, 0.92–1.05) or 10 µg/kg (ratio, 0.97; 90% CI, 0.93–1.01); 90% CIs were within the predefined range necessary to demonstrate bioequivalence. Hospira filgrastim was well tolerated with no additional safety concerns over Amgen filgrastim. Hospira filgrastim is bioequivalent with Amgen filgrastim with regard to its pharmacodynamic characteristics.

Biosimilar

Bioequivalence

Pharmacodynamics

10.1007/s00277-010-0973-6

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Citations (39)

Pharmacokinetic profiles of a biosimilar filgrastim and Amgen filgrastim: results from a randomized, phase I trial

Annals of Hematology (2010)

Cornelius F. Waller Miguel H. Bronchud Stuart Mair Rodeina Challand

Recombinant human granulocyte colony-stimulating factor (filgrastim) has multiple hematologic and oncologic indications as Neupogen® (Amgen filgrastim). Hospira has developed a biosimilar filgrastim (Nivestim™). Here, results are reported from a phase I trial, primarily designed to compare the pharmacokinetic profiles of Hospira filgrastim and Amgen filgrastim. A phase I, single-center, open-label, randomized trial was undertaken to demonstrate equivalence of the pharmacokinetic characteristics of Hospira filgrastim and Amgen filgrastim. Forty-eight healthy volunteers were randomized to receive intravenous (i.v.) or subcutaneous (s.c.) dosing and then further randomized to order of treatment. Volunteers in each of the two dosing groups received a single 10µg/kg dose of Hospira filgrastim or Amgen filgrastim, with subsequent crossover. Bioequivalence was evaluated by analysis of variance; if the estimated 90% confidence intervals (CIs) for the ratio of 'test' to 'reference' treatment means were within the conventional equivalence limits of 0.80–1.25, then bioequivalence was concluded. Forty-six volunteers completed the study. Geometric mean area under the curve from time 0 to the last time point (primary endpoint) was similar in volunteers given Hospira filgrastim or Amgen filgrastim following i.v. (ratio of means: 0.96; 90% CI: 0.90–1.02) or s.c. (ratio of means: 1.02; 90% CI: 0.95–1.09) dosing; 90% CIs were within the predefined range necessary to demonstrate bioequivalence. Hospira filgrastim was well tolerated with no additional safety concerns over Amgen filgrastim. Hospira filgrastim is bioequivalent with Amgen filgrastim in terms of its pharmacokinetic properties and may provide a clinically effective alternative.

Biosimilar

Bioequivalence

10.1007/s00277-010-0961-x

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Citations (37)

BCX9930, an Oral Factor D Inhibitor, for the Potential Treatment of Alternative Pathway Mediated Diseases: Interim Results of a Phase 1 Study in Healthy Subjects

Blood (2020)

Matthew Davidson Amanda Mathis Stuart Mair Diane Gesty‐Palmer Melanie Cornpropst

Paroxysmal nocturnal hemoglobinuria

Tolerability

Eculizumab

Pharmacodynamics