Source:http://linkedlifedata.com/resource/pubmed/id/14551179
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rdf:type | |
lifeskim:mentions |
umls-concept:C0011860,
umls-concept:C0030705,
umls-concept:C0031327,
umls-concept:C0166415,
umls-concept:C0205314,
umls-concept:C0243192,
umls-concept:C0332307,
umls-concept:C0679622,
umls-concept:C0851347,
umls-concept:C1175029,
umls-concept:C1552644,
umls-concept:C1554184,
umls-concept:C1708335,
umls-concept:C1823153,
umls-concept:C2349976
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pubmed:issue |
11
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pubmed:dateCreated |
2003-10-10
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pubmed:abstractText |
Ragaglitazar is a novel dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist intended to restore insulin sensitivity and correct diabetic dyslipidemia. These studies assessed single-dose pharmacokinetics and tolerability of ragaglitazar in healthy subjects, as well as multiple-dose pharmacokinetics, pharmacodynamics, and tolerability of ragaglitazar in healthy subjects and in patients with type 2 diabetes. Healthy subjects received a single oral dose (1-120 mg), and healthy subjects and type 2 diabetic patients received a loading dose and thereafter once-daily doses (0.5-16 mg) of ragaglitazar for 6 and 20 days, respectively. Ragaglitazar was rapidly absorbed (tmax: 1.5-1.7 h), with mean AUC0-24 h and Cmax proportional to dose after single and multiple dosing; t1/2 was 80 hours following a single dose and 104 hours in healthy subjects and 122 hours in patients after multiple dosing. Administration of 4 mg ragaglitazar to patients (n = 4) for 21 days resulted in mean decreases from baseline in fasting levels of plasma glucose (18%), C-peptide (18%), fructosamine (6%), triglycerides (36%), free fatty acids (49%), total cholesterol (11%), low-density lipoprotein (LDL) cholesterol (21%), and very low-density lipoprotein (VLDL) cholesterol (15%), as well as an increase in high-density lipoprotein (HDL) cholesterol (33%). Overall, ragaglitazar was well tolerated; with multiple dosing, there was a higher incidence of adverse events for patients that, at the highest dose level (16 mg), included peripheral edema and anemia.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Oxazines,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylpropionates,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cytoplasmic and Nuclear,
http://linkedlifedata.com/resource/pubmed/chemical/Transcription Factors,
http://linkedlifedata.com/resource/pubmed/chemical/ragaglitazar
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0091-2700
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1244-56
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:14551179-Adolescent,
pubmed-meshheading:14551179-Adult,
pubmed-meshheading:14551179-Aged,
pubmed-meshheading:14551179-Area Under Curve,
pubmed-meshheading:14551179-Confidence Intervals,
pubmed-meshheading:14551179-Diabetes Mellitus, Type 2,
pubmed-meshheading:14551179-Dose-Response Relationship, Drug,
pubmed-meshheading:14551179-Double-Blind Method,
pubmed-meshheading:14551179-Humans,
pubmed-meshheading:14551179-Linear Models,
pubmed-meshheading:14551179-Male,
pubmed-meshheading:14551179-Middle Aged,
pubmed-meshheading:14551179-Oxazines,
pubmed-meshheading:14551179-Phenylpropionates,
pubmed-meshheading:14551179-Receptors, Cytoplasmic and Nuclear,
pubmed-meshheading:14551179-Transcription Factors
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pubmed:year |
2003
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pubmed:articleTitle |
Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes.
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pubmed:affiliation |
Global Development, Novo Nordisk A/S, Bagsvaerd, Denmark.
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Comparative Study,
Randomized Controlled Trial
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