Farglitazar: Antidiabetic, PPARγ agonist

Drugs of the Future

Volumn 26, Issue 4, 2001, Pages 354-363

  Sorbera, L A ^a   Leeson, P A ^a   Martin, L ^a   Castaner J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 [2 (5 TETRAZOLYLMETHYL)BENZYLOXY]PHENOXYMETHYL]QUINOLINE; 5 (2,4 DIOXO 5 THIAZOLIDINYLMETHYL) 2 METHOXY N [4 (TRIFLUOROMETHYL)BENZYL]BENZAMIDE; 5 [4 [2 (1 INDOLYL)ETHOXY]BENZYL] 2,4 THIAZOLIDINEDIONE; ANTIDIABETIC AGENT; DYE; FARGLITAZAR; GLIBENCLAMIDE; N (2 BENZOYLPHENYL) O [2 (METHYL 2 PYRIDINYLAMINO)ETHYL]TYROSINE; NETOGLITAZONE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; REGLITAZAR;

AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG EFFICACY; DRUG HALF LIFE; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SYNTHESIS; DRUG TOLERABILITY; HUMAN; MULTICENTER STUDY; NON INSULIN DEPENDENT DIABETES MELLITUS; RANDOMIZED CONTROLLED TRIAL;

EID: 0034955381     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2001.026.04.617323     Document Type: Article

References (58)

1. N-(2-Benzoylphenyl)-L-tyrosine PPARγ agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents
2. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor γ (PPARγ)
3. 2 is a ligand for the adipocyte determination factor PPARγ
4. A human peroxisome-proliferator-activated receptor-γ is activated by inducers of adipogenesis, including thiazolidinedione drugs
5. Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-γ. Binding and activation correlate with antidiabetic actions in db/db mice
6. Isolation of the human peroxisome proliferator activated receptor γ cDNA: Expression in hematopoietic cells and chromosomal mapping
7. Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators
8. Differential expression and activation of a family of murine peroxisome proliferator-activated receptors
9. Identification of a new member of the steroid hormone receptor superfamily that is activated by a peroxisome proliferator and fatty acids
10. Cloning of a new member of the peroxisome proliferator-activated receptor gene family from mouse liver
11. A unified nomenclature system for the nuclear receptor superfamily
12. The organization, promoter analysis, and expression of the human PPARγ gene
13. Distinct stages in adipogenesis revealed by retinoid inhibition of differentiation after induction of PPARγ
14. PPARγ3 mRNA: A distinct PPARγ mRNA subtype transcribed from an independent promoter
15. Differential activation of peroxisome proliferator-activated receptors by eicosanoids
16. 2 metabolite binds peroxisome proliferator-activated receptor γ and promotes adipocyte differentiation
17. Fatty acids, eicosanoids, and hypolipidemic agents identified as ligands of peroxisome proliferator-activated receptors by coactivator-dependent receptor ligand assay
18. The peroxisome proliferator activated receptor-γ is a negative regulator of macrophage activation
19. Convergence of 9 cis retinoic acid and peroxisome proliferator signalling pathways through heterodimer formation of their receptors
20. The glitazone family of antidiabetic agents
21. The PPARs: From orphan receptors to drug discovery
22. Thiazolidinediones
23. In vitro characterization of the novel, tyrosine-based PPARγ agonist GI262570
24. The novel tyrosine-based PPARγ agonist GI262570 shows preferential binding to PPARγ complexed with RXRα and CBP
25. Asymmetry in the PPARγRXRα crystal structure reveals the molecular basis of heterodimerization among nuclear receptors
26. Antidiabetic efficacy of GI262570 in rodent models of type 2 diabetes
27. GI262570 prevents and reverses the progression of early diabetes in Zucker diabetic rats
28. The PPARγ agonist, GI262570, improves the prediabetic features of the metabolic syndrome X in insulin resistant primates
29. A new antidiabetic drug (GI262570): First time in man study of safety, tolerability, pharmacokinetics and glucodynamics
30. The effect of multiple doses of GI262570 on warfarin (W) pharmacokinetics and pharmacodynamics
31. Effect of multiple doses of GI262570 on digoxin (D) steady state pharmacokinetics (PK)
32. Prospective comparison of clinical trial simulation (CTS) and actual phase II results for GI262570, an antidiabetic compound
33. GI262570, a PPARγ agonist, reduces glucose, insulin, and triglyceride levels throughout the 24 hour profile after two weeks therapy in type 2 diabetics
34. Monotherapy with GI262570, a non-thiazolidinedione PPARγ agonist, improves glycemic control in type 2 diabetes mellitus patients (T2DM)
35. Monotherapy with GI262570, a tyrosine-based non-thiazolidinedione PPARγ agonist, significantly reduces triglyceride and increases HDL-C concentrations in patients with type 2 diabetes mellitus
36. GI262570, a non-thiazolidinedione, tyrosine-based PPARγ agonist improves overall metabolic control in combination with glibenclamide
37. GI262570, a tyrosine-based PPARγ agonist, reduces triglycerides and increases HDL-C concentrations in patients with type 2 diabetes mellitus when combined with glibenclamide treatment
38. PPAR agonists as direct modulators of the vessel wall in cardiovascular disease
39. PPAR agonists for metabolic diseases
40. GI262570, a tyrosine-based PPARγ agonist, reduces triglycerides and increases HDL-C concentrations in patients with type 2 diabetes mellitus when combined with glibenclamide treatment
41. GI262570, a PPARγ agonist, shows rapid onset of metabolic improvement within 2 weeks of therapy in type 2 diabetics
42. Monotherapy with GI262570, a non-thiazolidinedione PPARγ agonist, reduces triglyceride and increases HDL-C in patients with type 2 diabetes
43. GI262570, a non-thiazolidinedione, tyrosine-based PPARγ agonist improves overall metabolic control in combination with glibenclamide
44. GI262570, a nonthiazolidinedione PPARγ agonist, improves metabolic control in patients with type 2 diabetes mellitus when combined with glibenclamide treatment
45. Monotherapy with GI262570, a non-thiazolidinedione PPARγ agonist, reduces triglyceride and increases HDL-C in patients with type 2 diabetes
46. Monotherapy with GI262570, a non-thiazolidinedione PPARγ agonist, improves glycemic control in type 2 diabetes mellitus patients (T2DM)
47. Monotherapy with GI262570, a tyrosine-based non-thiazolidinedione PPARγ agonist, improves metabolic control in type 2 diabetes mellitus patients
48. GI262570, a PPARγ agonist, maintains metabolic improvements throughout 24 hour profiles in type 2 diabetic patients
49. GI262570 prevents and reverses the progression of early diabetes in Zucker diabetic 2fatty rats
50. GI262570 prevents and reverses the progression of early diabetes in Zucker diabetic fatty rats
51. Antidiabetic efficacy of GI262570 in two rodent models of type 2 diabetes
52. Antidiabetic efficacy of GI262570 in rodent models of type 2 diabetes
53. Discovery and in vitro characterization of the novel, tyrosine-based, non-thiazolidinedione PPARγ agonist GI262570
54. Discovery and in vitro characterization of the novel tyrosine-based, non-thiazolidinedione PPARγ agonist GI262570