Gene/Protein Disease Symptom Drug Enzyme Compound
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 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Liraglutide is a once-daily glucagon-like peptide-1 analogue being developed for the treatment of type 2 diabetes. The aim of this study was to investigate the effect of age and gender on the pharmacokinetics of liraglutide. Eight male and 8 female subjects were recruited from an 18- to 45-year-old group and an over-65-year-old group, respectively. All subjects received a single subcutaneous dose of 1.0 mg liraglutide. The area under the liraglutide plasma concentration curve from time 0 to last quantifiable concentration adjusted for body weight (significant covariate; P = .001) was found to be equivalent in young and elderly subjects (primary end point), with an estimated ratio of 0.94 (90% confidence interval, 0.84-1.06; P = .39). No significant impact of gender was observed (P = .38; estimated ratio, 1.08; 90% confidence interval, 0.93-1.26). Adverse events were of mild or moderate severity. The most frequently reported events were headache, vomiting, and nausea. When adjusted for body weight, no effect of gender or age was found on the pharmacokinetics of liraglutide.
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PMID:An open-label, parallel group study investigating the effects of age and gender on the pharmacokinetics of the once-daily glucagon-like peptide-1 analogue liraglutide. 1670 10

The incretin hormones are intestinal peptides that enhance insulin secretion following ingestion of nutrients. Liraglutide is a glucagon-like peptide-1 receptor analogue, which is obtained by derivatising glucagon-like peptide-1 with a fatty acid, providing a compound with pharmacokinetic properties that are suitable for once-daily dosing. Liraglutide has demonstrated lasting improvement of HbA(1c )levels, weight reduction and improved beta-cell function in patients with Type 2 diabetes mellitus. Liraglutide is well tolerated; the adverse events that are most frequently reported being transient nausea and diarrhoea. This article reviews the mechanisms of action and efficacy of liraglutide for the treatment of Type 2 diabetes mellitus. This agent is presently in Phase III clinical development.
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PMID:Liraglutide: a once-daily GLP-1 analogue for the treatment of type 2 diabetes mellitus. 1724 43

Liraglutide is a novel glucagon-like peptide-1 (GLP-1) receptor agonist with 97% amino acid sequence identity to native GLP-1. An amino acid substitution and fatty acid side chain enable a more protracted pharmacokinetic profile of over 24 hours. These modifications make liraglutide suitable for once-daily dosing. Liraglutide use exploits the incretin effect to glucose-dependently stimulate insulin secretion. The LEAD (Liraglutide Effect and Action Diabetes) program evaluated the safety and efficacy of liraglutide and demonstrated an improved level of glycemic control relative to currently used oral antidiabetic drugs, including other GLP-1-based therapies. In these trials, liraglutide was shown to enable many patients to achieve hemoglobin A1c (HbA1c) targets and to improve several morbidities commonly associated with type 2 diabetes; liraglutide induced weight loss, reduced systolic blood pressure and improved beta-cell function. Liraglutide was well tolerated, although an increased incidence of mild nausea was observed. Since liraglutide mimics the glucose-sensitive action of native GLP-1, it does not induce hypoglycemia. Liraglutide offers an interesting alternative therapy to control blood glucose levels in patients with type 2 diabetes, who commonly present with hypertension and overweight. It is expected to be approved by the U.S. Food and Drug Administration and the European Medicines Agency in Europe for use in 2009.
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PMID:Liraglutide: a new treatment for type 2 diabetes. 1934 30

Liraglutide is a long-acting analog of GLP-1, being developed by Novo Nordisk and currently undergoing regulatory review for the treatment of type 2 diabetes. Upon injection, liraglutide binds non-covalently to albumin, giving it a pharmacokinetic profile suitable for once-daily administration. In clinical trials of up to 1 year duration, liraglutide has been demonstrated to have beneficial effects on islet cell function, leading to improvements in glycemic control. Both fasting and postprandial glucose concentrations are lowered, and are associated with lasting reductions in HbA1c levels. Liraglutide is effective as monotherapy and in combination therapy with oral antidiabetic drugs, and reduces HbA1c by up to approximately 1.5% from baseline (8.2%-8.4%). Because of the glucose-dependency of its action, there is a low incidence of hypoglycemia. Liraglutide is associated with body weight loss, and reductions in systolic blood pressure have been observed throughout the clinical trials. The most common adverse events reported with liraglutide are gastrointestinal (nausea, vomiting and diarrhea). These tend to be most pronounced during the initial period of therapy and decline with time. Further clinical experience with liraglutide will reveal its long-term durability, safety and efficacy.
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PMID:Potential of liraglutide in the treatment of patients with type 2 diabetes. 1943 48

Liraglutide (Victoza) is an acylated analogue of glucagon-like peptide-1 (GLP-1) indicated for the treatment of type 2 diabetes mellitus. In phase III studies, once-daily subcutaneous liraglutide improved glycaemic control compared with placebo or active comparator in adult patients with type 2 diabetes, both as monotherapy and in combination with one or two oral antidiabetic drugs such as metformin, sulfonylureas or thiazolidinediones. Liraglutide provided significantly better glycaemic control than rosiglitazone or insulin glargine in combination trials. At appropriate dosages, liraglutide was noninferior to glimepiride with respect to glycaemic control in a combination trial, but provided significantly better control than glimepiride or glibenclamide in monotherapy trials. Liraglutide improved pancreatic beta-cell function, generally led to weight loss, and was associated with a low risk of hypoglycaemia. Liraglutide was generally well tolerated, with the most common adverse events being gastrointestinal events, such as nausea, which decreased over time. Thus, liraglutide is an effective treatment option for use in patients with type 2 diabetes mellitus.
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PMID:Liraglutide: a review of its use in type 2 diabetes mellitus. 1974 13

Recently, the European Medicines Agency (EMEA) Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion, recommending to grant a marketing authorization for liraglutide for the treatment of type 2 diabetes mellitus. Liraglutide is the first human glucagon-like peptide-1 (GLP-1) analog, based on the structure of native GLP-1, with pharmacokinetic properties suitable for once-daily dosing. In the phase III Liraglutide Effect and Action in Diabetes (LEAD) program, liraglutide has been shown to lower glycated hemoglobin to the same extent or more than other antidiabetic drugs including insulin. Liraglutide determines favorable changes in the global cardiovascular risk profile because its use is associated with weight loss, blood pressure reduction, as well as improvements of several cardiovascular risk biomarkers. Liraglutide is generally well tolerated, the most frequently reported adverse effect is transient nausea, and it does not seems to have significant interactions with medications commonly used for cardiovascular prevention. This article reviews, for the practicing cardiologist, the results of the LEAD program and explores liraglutide potentials for cardiovascular prevention in type 2 diabetes mellitus.
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PMID:[Drug therapy of type 2 diabetes and cardiovascular prevention: potentials for liraglutide]. 1976 Nov 1

Liraglutide is a new glucagon-like peptide-1 (GLP-1) receptor agonist and a true GLP-1 analogue. After successful phase 2 studies, liraglutide was assessed in a series of phase 3 trials [(Liraglutide Effect and Action in Diabetes (LEAD)] designed to demonstrate efficacy and safety across the continuum of type 2 diabetes antihyperglycaemic care, both as monotherapy and in combination with commonly used oral antidiabetic drugs (OADs). The LEAD programme also compared liraglutide with other OADs. As a monotherapy, liraglutide demonstrated significant improvements in glycaemic control in comparison with glimepiride. When combined with one or two OADs, reductions in haemoglobin A1c, fasting plasma glucose and postprandial glucose were generally greater with liraglutide than with comparators. Throughout the trials, liraglutide was associated with weight reduction; in most instances, the reduction from baseline was significantly greater than that seen with comparators. Improvements in assessments of beta-cell function were consistently shown with liraglutide treatment across all trials. Furthermore, reductions in systolic blood pressure were reported. Liraglutide was associated with a low risk of hypoglycaemia and was generally well tolerated. The majority of adverse effects were gastrointestinal, the most frequent of which was nausea.
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PMID:The safety and efficacy of liraglutide with or without oral antidiabetic drug therapy in type 2 diabetes: an overview of the LEAD 1-5 studies. 1987 59

Liraglutide, a new glucagon-like peptide-1 (GLP-1)-receptor agonist with 97% homology to human GLP-1, can be administered once/day independent of meals in patients with type 2 diabetes mellitus. Clinical trials have demonstrated its efficacy in controlling hyperglycemia, helping patients achieve hemoglobin A(1c) level goals; in facilitating weight loss, and in improving indexes of beta-cell function when used alone or in combination with metformin, glimepiride, or rosiglitazone. These studies also suggest that liraglutide may be associated with modest improvements in systolic blood pressure. Data from a comparative trial of liraglutide and insulin glargine have suggested that liraglutide provides greater glycemic control with less weight gain, and another study demonstrated that liraglutide provides greater improvements in glycemic control with less hypoglycemia than exenatide and with comparable weight loss. Although liraglutide is well tolerated and is associated with low rates of hypoglycemia, transient and mild nausea can occur when therapy is initiated. However, rates of hypoglycemia appear to be lower and nausea appears to be less persistent with liraglutide than with exenatide. Even though data on the long-term use of liraglutide are still needed, this drug may provide a useful treatment option in patients poorly controlled with dietary modification and exercise and in those whose diabetes is inadequately controlled by oral antidiabetic agents.
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PMID:Clinical studies of liraglutide, a novel, once-daily human glucagon-like peptide-1 analog for improved management of type 2 diabetes mellitus. 1994 16

When patients with type 2 diabetes fail to achieve strict HbA1c control with oral glucose-lowering drugs, insulin is the standard recourse. Exenatide, an injectable incretin analogue, should only be used when weight gain is a major problem. Liraglutide is another injectable incretin analogue recently authorised for use in this setting. Two randomised unblinded trials, one versus insulin glargine in 581 patients and the other versus exenatide in 464 patients, suggest that liraglutide has a slightly more potent effect on glycaemia. Weight loss was similar in the liraglutide and exenatide groups. In a trial including 1091 patients, liraglutide was not more or less effective than glimepiride on glycaemia. Like exenatide, liraglutide can cause pancreatitis. In the trial comparing liraglutide versus exenatide, one-quarter of patients experienced nausea. There is more evidence of a risk of thyroid cancer with liraglutide than with exenatide. Liraglutide is administered as a single daily subcutaneous injection, whereas exenatide requires two daily injections. In practice, when prescribing an incretin analogue seems justified, it is more prudent to continue using exenatide, while closely monitoring patients for adverse effects.
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PMID:Liraglutide. Type 2 diabetes: more prudent to continue using exenatide. 2073 33

Liraglutide (Victoza) is a peptide produced by DNA recombinant technology, which presents 97% homology with human glucagon-like peptide-1 (GLP-1) but is resistant to dipeptidylpeptidase-4, the enzyme that degrades the natural hormone. It actives the GLP-1 receptor and exerts an incretin mimetic effect during at least 24 hours after a single subcutaneous injection. Besides a glucose-dependent stimulatory effect of insulin secretion, liraglutide inhibits glucagon secretion and retards gastric emptying. In patients with type 2 diabetes, it reduces glycated haemoglobin by at least 1%, without inducing hypoglycaemia. It also induces a moderate weight loss and a mild reduction in blood pressure. Gastrointestinal adverse events (nausea, vomiting) may occur during the initial phase of treatment, but rarely impose the interruption of the medication and usually diminish with time.Although indicated in combination with other glucose-lowering agents, liraglutide is currently reimbursed in Belgium only if administered in patients with type 2 diabetes not sufficiently controlled with a combination of metformin plus sulfonylurea or metformin plus a thiazolidinedione. Victoza is presented in prefilled pens and is injected subcutaneously once a day. Treatment will be initiated with 0.6 mg to improve digestive tolerance and the daily dose will be increased to 1.2 mg (usual dose) after at least one week, and up to 1.8 mg (maximal dose) if necessary.
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PMID:[Liraglutide (Victoza): human glucagon-like peptide-1 used in once daily injection for the treatment of type 2 diabetes]. 2085 6


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