sodelglitazar

{{Short description|Chemical compound}}

{{Drugbox

| verifiedrevid =

| IUPAC_name = [4-[[[2-[2-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methyl]sulfanyl]-2-methylphenoxy]-2-methylpropanoic acid

{{cite patent | country = US | number = 7105551 | status = abandoned | title = Thiazole derivatives for treating ppar related disorders | assign1 = SmithKlineBeecham | inventor = Rodolfo C, Marie GR, Hurst III LM, Lawrence SM | pubdate = 1 April 2004 }}

| image = Sodelglitazar skeletal.svg

| width = 275

| tradename =

| MedlinePlus =

| pregnancy_category = N/A

| legal_status = Investigational

| routes_of_administration =

| bioavailability =

| protein_bound =

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| CAS_number = 447406-78-2

| ATC_prefix = None

| ATC_suffix =

| PubChem = 9805950

| IUPHAR_ligand =

| DrugBank =

| UNII = 6G973E04VI

| KEGG = D06647

| ChEMBL = 2104984

| ChemSpiderID = 7981710

| C=23 | H=21 | F=4 | N=1 | O=3 | S=2

| molecular_weight =

| smiles = CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=C(C=C(C=C3)C(F)(F)F)F)C)OC(C)(C)C(=O)O

| StdInChI = 1S/C23H21F4NO3S2/c1-12-9-15(6-8-18(12)31-22(3,4)21(29)30)32-11-19-13(2)28-20(33-19)16-7-5-14(10-17(16)24)23(25,26)27/h5-10H,11H2,1-4H3,(H,29,30)

| StdInChIKey = ZUGQWAYOWCBWGM-UHFFFAOYSA-N

}}

Sodelglitazar, formerly known as GW 677954, is a thiazole PPARδ receptor agonist developed by GlaxoSmithKline.{{cite journal | vauthors = Liu XY, Wang RL, Xu WR, Tang LD, Wang SQ, Chou KC | title = Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar | journal = Protein and Peptide Letters | volume = 18 | issue = 10 | pages = 1021–7 | date = October 2011 | pmid = 21592078 | doi = 10.2174/092986611796378701 }} While it is primarily active at the PPARδ receptor, it is considered a pan agonist with activity at PPARα and PPARγ receptors.{{cite book| vauthors = Ottow E, Weinmann H |title=Nuclear Receptors as Drug Targets |url= https://books.google.com/books?id=iATfLbPgRugC&pg=PA380 |access-date=2 April 2013|year=2008|publisher=Wiley|isbn=978-3-527-31872-8|pages=380–}}

Safety

Phase 2 studies were terminated prior to completion due to safety findings in rodent studies.{{cite web|url= http://download.gsk-clinicalstudyregister.com/files/20459.pdf | archive-url = https://web.archive.org/web/20170306040626/http://download.gsk-clinicalstudyregister.com/files/20459.pdf | archive-date = 6 March 2017 |title= A randomised, double-blind, parallel group, placebo-controlled, multicentre study to evaluate the safety, tolerability and efficacy of oral GW677954 capsules 2.5mg, 5mg, 10mg and 20mg a day for 24 weeks in overweight dyslipidaemic subjects |publisher=GlaxoSmithKline|date=2013-09-01}}

See also

References