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Chemical Compound Review

Ragaglitazar     (2S)-2-ethoxy-3-[4-(2- phenoxazin-10...

Synonyms: CHEMBL24038, DRF-2725, NN-622, SureCN4822459, CHEBI:133785, ...
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Disease relevance of Ragaglitazar

  • PPARalpha /gamma ragaglitazar eliminates fatty liver and enhances insulin action in fat-fed rats in the absence of hepatomegaly [1].
  • 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 [2].
  • Ragaglitazar is a novel dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist intended to restore insulin sensitivity and correct diabetic dyslipidemia [2].
  • In summary, our findings showed that in the urothelium of ragaglitazar-treated animals, hypertrophy (increased size and protein content per cell) was an early change, that affected the whole bladder urothelial cell population [3].
  • These data indicates that dual PPARalpha and gamma activator ragaglitazar can be beneficial for the treatment of hypertension and vascular disease commonly associated with type 2 diabetes [4].

High impact information on Ragaglitazar


Biological context of Ragaglitazar


Anatomical context of Ragaglitazar

  • We examined early (precancerous) changes in the bladder urothelium of rats orally dosed with ragaglitazar, using a newly developed flow cytometric method [3].

Associations of Ragaglitazar with other chemical compounds


Gene context of Ragaglitazar


Analytical, diagnostic and therapeutic context of Ragaglitazar


  1. PPARalpha /gamma ragaglitazar eliminates fatty liver and enhances insulin action in fat-fed rats in the absence of hepatomegaly. Ye, J.M., Iglesias, M.A., Watson, D.G., Ellis, B., Wood, L., Jensen, P.B., Sørensen, R.V., Larsen, P.J., Cooney, G.J., Wassermann, K., Kraegen, E.W. Am. J. Physiol. Endocrinol. Metab. (2003) [Pubmed]
  2. Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. Skrumsager, B.K., Nielsen, K.K., Müller, M., Pabst, G., Drake, P.G., Edsberg, B. Journal of clinical pharmacology. (2003) [Pubmed]
  3. Generalized cellular hypertrophy is induced by a dual-acting PPAR agonist in rat urinary bladder urothelium in vivo. Oleksiewicz, M.B., Thorup, I., Nielsen, H.S., Andersen, H.V., Hegelund, A.C., Iversen, L., Guldberg, T.S., Brinck, P.R., Sjogren, I., Thinggaard, U.K., Jørgensen, L., Jensen, M.B. Toxicologic pathology. (2005) [Pubmed]
  4. Antihypertensive effect of ragaglitazar: a novel PPARalpha and gamma dual activator. Mamnoor, P.K., Hegde, P., Datla, S.R., Damarla, R.K., Rajagopalan, R., Chakrabarti, R. Pharmacol. Res. (2006) [Pubmed]
  5. Differential influences of peroxisome proliferator-activated receptors gamma and -alpha on food intake and energy homeostasis. Larsen, P.J., Jensen, P.B., Sørensen, R.V., Larsen, L.K., Vrang, N., Wulff, E.M., Wassermann, K. Diabetes (2003) [Pubmed]
  6. Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar. Ebdrup, S., Pettersson, I., Rasmussen, H.B., Deussen, H.J., Frost Jensen, A., Mortensen, S.B., Fleckner, J., Pridal, L., Nygaard, L., Sauerberg, P. J. Med. Chem. (2003) [Pubmed]
  7. Ragaglitazar: a novel PPAR alpha PPAR gamma agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Chakrabarti, R., Vikramadithyan, R.K., Misra, P., Hiriyan, J., Raichur, S., Damarla, R.K., Gershome, C., Suresh, J., Rajagopalan, R. Br. J. Pharmacol. (2003) [Pubmed]
  8. Biomarkers for early effects of carcinogenic dual-acting PPAR agonists in rat urinary bladder urothelium in vivo. Egerod, F.L., Nielsen, H.S., Iversen, L., Thorup, I., Storgaard, T., Oleksiewicz, M.B. Biomarkers (2005) [Pubmed]
  9. Intravenous pharmacokinetics, oral bioavailability and dose proportionality of ragaglitazar, a novel PPAR-dual activator in rats. Jagannath, K., Chaluvadi, M.R., Mullangi, R., Mamidi, N.V., Srinivas, N.R. Biopharmaceutics & drug disposition. (2004) [Pubmed]
  10. Development and validation of a high-resolution capillary electrophoresis method for multi-analysis of ragaglitazar and arginine in active pharmaceutical ingredients and low-dose tablets. Jamali, B., Lehmann, S. Journal of pharmaceutical and biomedical analysis. (2004) [Pubmed]
  11. Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: the bezafibrate lessons. Tenenbaum, A., Motro, M., Fisman, E.Z. Cardiovascular diabetology [electronic resource]. (2005) [Pubmed]
  12. Development and validation of a high-precision capillary electrophoresis method for main component assay of ragaglitazar. Lehmann, S.V., Bergholdt, A.B. Journal of chromatography. A. (2003) [Pubmed]
  13. Quantitative determination of ragaglitazar in rat plasma by HPLC: validation and application in pharmacokinetic study. Kota, J., Mullangi, R., Mamidi, R.N., Rajagopalan, R. Biomed. Chromatogr. (2002) [Pubmed]
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