scholarly journals An open‐label clinical trial of the effects of age and gender on the pharmacodynamics, pharmacokinetics and safety of the ghrelin receptor agonist anamorelin

2015 ◽  
Vol 4 (2) ◽  
pp. 112-120 ◽  
Author(s):  
Philip T. Leese ◽  
John M. Trang ◽  
Robert A. Blum ◽  
Eleanor de Groot
Keyword(s):  
Clinical Trial ◽  
Receptor Agonist ◽  
Open Label ◽  
Age And Gender ◽  
Ghrelin Receptor ◽  
Ghrelin Receptor Agonist ◽  
And Gender

Integrated Approach to Early Detection of Cardiovascular Toxicity Induced by a Ghrelin Receptor Agonist

2015 ◽  
Vol 34 (2) ◽  
pp. 151-161 ◽  
Author(s):  
Alan H. Stokes ◽  
J. Greg Falls ◽  
Lawrence Yoon ◽  
Neal Cariello ◽  
Brenda Faiola ◽  
...  
Keyword(s):  
Cardiac Troponin ◽  
Receptor Agonist ◽  
Troponin I ◽  
Troponin T ◽  
Heart Weight ◽  
Repeat Dose ◽  
End Points ◽  
Fatty Acid Binding ◽  
Ghrelin Receptor ◽  
Ghrelin Receptor Agonist

Cardiovascular (CV) safety concerns are among the leading causes of compound attrition in drug development. This work describes a strategy of applying novel end points to a 7-day rodent study to increase the opportunity to detect and characterize CV injury observed in a longer term (ie, 28 days) study. Using a ghrelin receptor agonist (GSK894281), a compound that produces myocardial degeneration/necrosis in rats after 28 days at doses of 0.3, 1, 10, or 60 mg/kg/d, we dosed rats across a range of similar doses (0, 0.3, 60, or 150 mg/kg/d) for 7 days to determine whether CV toxicity could be detected in a shorter study. End points included light and electron microscopies of the heart; heart weight; serum concentrations of fatty acid-binding protein 3 (FABP3), cardiac troponin I (cTnI), cardiac troponin T (cTnT), and N-terminal proatrial natriuretic peptide (NT-proANP); and a targeted transcriptional assessment of heart tissue. Histologic evaluation revealed a minimal increase in the incidence and/or severity of cardiac necrosis in animals administered 150 mg/kg/d. Ultrastructurally, mitochondrial membrane whorls and mitochondrial degeneration were observed in rats given 60 or 150 mg/kg/d. The FABP3 was elevated in rats given 150 mg/kg/d. Cardiac transcriptomics revealed evidence of mitochondrial dysfunction coincident with histologic lesions in the heart, and along with the ultrastructural results support a mechanism of mitochondrial injury. There were no changes in cTnI, cTnT, NT-proANP, or heart weight. In summary, enhancing a study design with novel end points provides a more integrated evaluation in short-term repeat dose studies, potentially leading to earlier nonclinical detection of structural CV toxicity.

Failure of Demonstrated Clinical Efficacy of Antibiotic-Bonded Continuous Ambulatory Peritoneal Dialysis (CAPD) Catheters

1990 ◽  
Vol 10 (1) ◽  
pp. 57-59 ◽  
Author(s):  
Stanley Z. Trooskin ◽  
Richard A. Harvey ◽  
T. w. J. Lennard ◽  
Ralph S. Greco
Keyword(s):  
Clinical Trial ◽  
Peritoneal Dialysis ◽  
Continuous Ambulatory Peritoneal Dialysis ◽  
Infectious Complications ◽  
Clinical Report ◽  
Age And Gender ◽  
And Gender ◽  
To Receive

Previous in vitro, in vivo, and a preliminary clinical report have demonstrated efficacy of noncovalently bonding antibiotics to the surface of continuous ambulatory peritoneal dialysis (CAPO) catheters in decreasing infectious complications. A larger prospective randomized clinical trial was completed. Eighty-six patients with chronic renal failure were enrolled in the study and randomized to receive either a surfactant treated or untreated control catheter. All catheters were soaked in cefoxitin at the time of insertion. Groups were comparable in terms of pre-existing illnesses, age, and gender. No differences were shown in the incidence of cathetertract infections, peritonitis or mechanical complications. There was also no differences in microbiologic culture results. Therefore, it is concluded that this clinical trial did not demonstrate a reduction in catheter-related infectious complications by antibiotic bonding.

scholarly journals Population pharmacokinetics (PPK) of anamorelin (ANAM), an oral selective ghrelin receptor agonist

2018 ◽  
Vol 29 ◽  
pp. viii616-viii617 ◽  
Author(s):  
A. Bernareggi ◽  
S. Kaasa ◽  
M. Fallon ◽  
R.J.E. Skipworth ◽  
D. Currow
Keyword(s):  
Population Pharmacokinetics ◽  
Receptor Agonist ◽  
Ghrelin Receptor ◽  
Ghrelin Receptor Agonist

scholarly journals Effects of ghrelin receptor agonist, relamorelin, on gastric motor functions and satiation in healthy volunteers

2016 ◽  
Vol 28 (11) ◽  
pp. 1705-1713 ◽  
Author(s):  
A. D. Nelson ◽  
M. Camilleri ◽  
A. Acosta ◽  
I. Busciglio ◽  
S. Linker Nord ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Receptor Agonist ◽  
Motor Functions ◽  
Ghrelin Receptor ◽  
Ghrelin Receptor Agonist

Investigation of the effectiveness of a ghrelin receptor agonist to stimulate the defecation centre in spinal cord injured rats

2011 ◽  
Vol 163 (1-2) ◽  
pp. 58
Author(s):  
J.B. Furness ◽  
D.M. Ferens ◽  
M.D. Habgood ◽  
N.R. Saunders ◽  
D.J. Brown ◽  
...  
Keyword(s):  
Spinal Cord ◽  
Receptor Agonist ◽  
Ghrelin Receptor ◽  
Ghrelin Receptor Agonist ◽  
Spinal Cord Injured

Ghrelin receptor agonist, GHRP-2, produces antinociceptive effects at the supraspinal level via the opioid receptor in mice

Peptides ◽  
2014 ◽  
Vol 55 ◽  
pp. 103-109 ◽  
Author(s):  
Ping Zeng ◽  
Shu Li ◽  
Yue-hui Zheng ◽  
Fu-Yan Liu ◽  
Jing-lei Wang ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Ghrelin Receptor ◽  
Antinociceptive Effects ◽  
Ghrelin Receptor Agonist
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