Drug Details

General Information of the Drug (ID: DR0019)
Name
Pemafibrate
Synonyms
Pemafibrate; 848259-27-8; UNII-17VGG92R23; (R)-2-(3-((benzo[d]oxazol-2-yl(3-(4-methoxyphenoxy)propyl)amino)methyl)phenoxy)butanoic acid; CHEMBL247951; (R)-K-13675; 17VGG92R23; K-13675, (R)-; 848259-27-8 (free acid); CAS#848259-27-8; (2~{R})-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid; (2R)-2-[3-[[1,3-benzoxazol-2-yl-[3-(4-methoxyphenoxy)propyl]amino]methyl]phenoxy]butanoic acid; Pemafibrate [INN]; Parmodia (TN); P7F; Pemafibrate (JAN); (R)-K 13675; SCHEMBL2766188; DTXSID00233891; BCP20864; EX-A1919; BDBM50214899; CS-6084; DB15212; SB19229; HY-17618; D10711; Q27251943; K-877; (R)-K 13675; CS-2768; K-877; K877; K 877; (R)-K 13675; (R)-K13675; (R)K-13675; (R)-2-[3-[N-(benzoxazol-2-yl)-N-(3-(4-methoxyphenoxy)propyl)aminomethyl]phenoxy]butyric acid
    Click to Show/Hide
Molecular Type
Small molecule
Disease Hypertriglyceridaemia [ICD-11: 5C80] Approved [1]
Structure
Click to Download Mol
2D MOL

3D MOL

    Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product
Formula
C28H30N2O6
PubChem CID
11526038
Canonical SMILES
CCC(C(=O)O)OC1=CC=CC(=C1)CN(CCCOC2=CC=C(C=C2)OC)C3=NC4=CC=CC=C4O3
InChI
1S/C28H30N2O6/c1-3-25(27(31)32)35-23-9-6-8-20(18-23)19-30(28-29-24-10-4-5-11-26(24)36-28)16-7-17-34-22-14-12-21(33-2)13-15-22/h4-6,8-15,18,25H,3,7,16-17,19H2,1-2H3,(H,31,32)/t25-/m1/s1
InChIKey
ZHKNLJLMDFQVHJ-RUZDIDTESA-N
CAS Number
CAS 848259-27-8
TTD Drug ID
D04QIE
DrugBank ID
DB15212
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Pitavastatin      Homo sapiens     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Up-regulation Expression NOS3  Molecule Info 
Pathway MAP
                    In-vivo Model For a xenograft model, seven-week-old male Dahl salt-sensitive (DS) rats were fed a normal diet (ND; 0.3% NaCl and 4.5% fat) or a high-salt and high-fat diet (HD; 8% NaCl and 29.4% fat).
                    Experimental
                    Result(s)		 Combination therapy with pitavastatin and pemafibrate improved lipid profiles including TG and cholesterol levels and ameliorated endothelial dysfunction.
Target and Pathway
Target(s) PPAR-alpha (PPARA)  Molecule Info  [1]
KEGG Pathway PPAR signaling pathway Click to Show/Hide
2 cAMP signaling pathway
3 Adipocytokine signaling pathway
4 Glucagon signaling pathway
5 Non-alcoholic fatty liver disease (NAFLD)
6 Hepatitis C
Pathway Interaction Database RXR and RAR heterodimerization with other nuclear receptor Click to Show/Hide
Reactome RORA activates gene expression Click to Show/Hide
2 BMAL1:CLOCK,NPAS2 activates circadian gene expression
3 PPARA activates gene expression
4 YAP1- and WWTR1 (TAZ)-stimulated gene expression
5 Transcriptional activation of mitochondrial biogenesis
6 Activation of gene expression by SREBF (SREBP)
7 Transcriptional regulation of white adipocyte differentiation
8 Nuclear Receptor transcription pathway
9 Regulation of lipid metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
10 Circadian Clock
WikiPathways Nuclear Receptors in Lipid Metabolism and Toxicity Click to Show/Hide
2 Nuclear Receptors Meta-Pathway
3 Estrogen Receptor Pathway
4 PPAR Alpha Pathway
5 Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
6 Transcriptional Regulation of White Adipocyte Differentiation
7 YAP1- and WWTR1 (TAZ)-stimulated gene expression
8 Activation of Gene Expression by SREBP (SREBF)
9 Adipogenesis
10 SREBF and miR33 in cholesterol and lipid homeostasis
11 Circadian Clock
12 Nuclear Receptors
References
Reference 1 Pemafibrate: First Global Approval. Drugs. 2017 Oct;77(16):1805-1810.
Reference 2 Combination therapy with pemafibrate (K-877) and pitavastatin improves vascular endothelial dysfunction in dahl/salt-sensitive rats fed a high-salt and high-fat diet. Cardiovasc Diabetol. 2020 Sep 26;19(1):149.
 Download Picture         KEGG Link