Once- and Twice-Daily Dosing With Rosiglitazone Improves Glycemic Control in Patients With Type 2 Diabetes

Phillips, Lawrence S.; Grunberger, George; Miller, Elizabeth R.; Patwardhan, Rita; Rappaport, Elizabeth B.; Salzman, Alan

doi:10.2337/diacare.24.2.308

Cited by 280 publications

(189 citation statements)

References 27 publications

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“…Among those, the thiazolidinedione (TZD) class of drugs is currently used for the treatment of type 2 diabetes (28). They normalize glycemia and decrease insulin as well as free fatty acid serum levels in type 2 diabetic rodents and human subjects (29,30) and reduce atherosclerosis in certain mouse models (11).…”

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confidence: 99%

S 26948

et al. 2007

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OBJECTIVE-Rosiglitazone displays powerful antidiabetes benefits but is associated with increased body weight and adipogenesis. Keeping in mind the concept of selective peroxisome proliferator-activated receptor (PPAR)␥ modulator, the aim of this study was to characterize the properties of a new PPAR␥ ligand, S 26948, with special attention in body-weight gain.RESEARCH DESIGN AND METHODS-We used transient transfection and binding assays to characterized the binding characteristics of S 26948 and GST pull-down experiments to investigate its pattern of coactivator recruitment compared with rosiglitazone. We also assessed its adipogenic capacity in vitro using the 3T3-F442A cell line and its in vivo effects in ob/ob mice (for antidiabetes and antiobesity properties), as well as the homozygous human apolipoprotein E2 knockin mice (E2-KI) (for antiatherogenic capacity).RESULTS-S 26948 displayed pharmacological features of a high selective ligand for PPAR␥ with low potency in promoting adipocyte differentiation. It also displayed a different coactivator recruitment profile compared with rosiglitazone, being unable to recruit DRIP205 or PPAR␥ coactivator-1␣. In vivo experiments showed that S 26948 was as efficient in ameliorating glucose and lipid homeostasis as rosiglitazone, but it did not increase body and white adipose tissue weights and improved lipid oxidation in liver. In addition, S 26948 represented one of the few molecules of the PPAR␥ ligand class able to decrease atherosclerotic lesions.CONCLUSIONS-These findings establish S 26948 as a selective PPAR␥ ligand with distinctive coactivator recruitment and gene expression profile, reduced adipogenic effect, and improved biological responses in vivo.

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confidence: 99%

S 26948

et al. 2007

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“…Rosi is a potent antidiabetic drug which improves insulin sensitivity and glycaemic status (Phillips et al, 2001). In addition, it was shown that pretreatment with Rosi and other TZDs leads to the reduction of the adipocyte cell size (Johnson et al, 2007;Velebit et al, 2008).…”

Section: Rosiglitazone Increases the Plasma Membrane Glut4 Density VImentioning

confidence: 99%

Rosiglitazone balances insulin-induced exo- and endocytosis in single 3T3-L1 adipocytes

Velebit

Chowdhury

Kreft

et al. 2011

Molecular and Cellular Endocrinology

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Rosiglitazone (Rosi) improves insulin sensitivity and increases the translocation of glucose transporter 4 (GLUT4) to the plasma membrane (PM). This involves the fusion of membranebound compartments with the plasma membrane, thus increasing the plasma membrane area.However, recent work has shown that in Rosi-pretreated 3T3-L1 adipocytes membrane area did not increase following insulin application, suggesting that the rates of exo-and endocytosis are balanced. Here we examined whether Rosi differentially affects the rates of exo-and endocytosis in 3T3-L1 adipocytes. The immunolabelling of GLUT4 revealed the 3.1-fold increase in PM-resident GLUT4 in Rosi-pretreated, insulin-stimulated cells. By monitoring cumulative exocytosis and endocytosis we found that in Rosi-pretreated cells insulin substantially stimulated the rate of exocytosis and to a similar extent also the rate of endocytosis. We conclude that Rosi-pretreatment balances insulin-stimulated exocytosis and endocytosis, which may prevent insulin-mediated adipocyte cell size increase.

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“…However, with rosiglitazone it should be noted that 4 mg twice daily may be more potent than 8 mg once daily. 32 Lastly, it should be realized that it takes more time for the TZDs to demonstrate full effect than the other oral agents (3 to 4 months vs. several weeks). 32,33,36 Combination agents Within the last 2 years several combination agents have been released for use in the management of type 2 DM.…”

Section: Important Management Issues In Type 2 Dmmentioning

confidence: 99%

“…Interestingly, this alteration of gene transcription takes place in adipocytes and the genes concerned primarily regulate fatty acid metabolism, the net result of which is to decrease serum FFA by approximately 20% to 40%. [32][33][34] This reduction in FFA, in turn, improves insulin action in muscle tissue, thus implicating elevated FFA as a major contributor to insulin resistance. Further-more, this reduction in FFA improves β-cell function by decreasing lipotoxicity, a process whereby increased FFA eventually leads to β-cell death.…”

Section: Thiazolidinediones (Tzd)mentioning

confidence: 99%

“…Perhaps the most noticeable of these non-glycemic effects is the ability of the TZDs to raise high-density lipoprotein (HDL) cholesterol by up to 13%. 32,[39][40][41][42][43]46 Furthermore, there may be a differential effect on HDL subtypes with rosiglitazone, preferentially effecting HDL-2 (the most protective HDL subfraction). 46 The effects on triglycerides and low-density lipoprotein (LDL) levels tend to be more variable and there is mounting evidence that pioglitazone performs consistently better in these regards than rosiglitazone.…”

Section: Thiazolidinediones (Tzd)mentioning

confidence: 99%

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Current Therapeutic Options in Type 2 Diabetes Mellitus: A Practical Approach

Sheehan¹

2003

Clinical Medicine & Research

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The incidence of type 2 diabetes mellitus (DM) in the United States continues to grow rapidly, paralleling the overweight and obesity epidemic. For many years the only therapeutic options for type 2 DM were sulfonylureas and insulin. However, over the last 9 years there has been an explosion of new and exciting agents approved for the treatment of type 2 DM. Some of the treatments target insulin deficiency and others insulin resistance, the hallmarks of the disease. Other drugs delay the intestinal absorption of carbohydrate. Recently several combination agents have been released. With these new drugs has come an overwhelming mountain of information, making it difficult for the busy clinician to know how best to manage the ever-increasing portion of patients with type 2 DM.New questions have arisen: Which agent to start as first line? How much of this drug to use before adding something else? How long for this drug to reach full effect? Which agent to add second? Should a patient uncontrolled on dual therapy begin insulin or start a third oral agent? If insulin therapy is started, what should become of the patient's oral agents? How best to explain the patient's weight gain on therapy? These are not easy questions and no review can fully detail all the therapeutic combinations possible. Instead, the practical approach of reviewing the agents in terms of their mechanism of action and critically comparing their dosing, effect and cost, is undertaken herein. Also addressed is the possible niche some newer classes of agents and combination drugs may or may not hold in the management of type 2 DM. The decision of using insulin versus a third oral agent will be looked at from the standpoint of where the patient is on dual therapy in relation to the hemoglobin A 1c goal. In this way it is hoped that some clarity will be brought to the dizzying array of information that both the physician and patient have to deal with in regard to the management of this prevalent and serious disease.

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Once- and Twice-Daily Dosing With Rosiglitazone Improves Glycemic Control in Patients With Type 2 Diabetes

Cited by 280 publications

References 27 publications

S 26948

S 26948

Rosiglitazone balances insulin-induced exo- and endocytosis in single 3T3-L1 adipocytes

Current Therapeutic Options in Type 2 Diabetes Mellitus: A Practical Approach

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