Delving into the Latest Updates on Fenofibrate/Pitavastatin Calcium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fenofibrate/pitavastatin, HL-PIF, Livasupril

+ [2]

Target

HMGCR x PPARα

Action

inhibitors, agonists

Mechanism

HMG-CoA reductase inhibitors(HMG-CoA reductase inhibitors), PPARα agonists(Peroxisome proliferator-activated receptor α agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Hyperlipidemias

Inactive Indication

Complex dyslipidemia

Originator Organization

Hanlim Pharm Co., Ltd.

Active Organization

Hanlim Pharm Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

South Korea (03 Apr 2019),

Hyperlipidemias

Regulation-

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Structure/Sequence

Molecular FormulaC20H21ClO4

InChIKeyYMTINGFKWWXKFG-UHFFFAOYSA-N

CAS Registry49562-28-9

View All Structures (2)

Background/Aims: Pregnancy success requires mandatory maternal tolerance of the semi/ allogeneic embryo involving embryo-derived signals. Expression levels of PreImplantation Factor (PIF), a novel peptide secreted by viable embryos, correlate with embryo development, and its early detection in circulation correlates with a favourable pregnancy outcome. PIF enhances endometrial receptivity to promote embryo implantation. Via the p53 pathway, it increases trophoblast invasion, improving cell survival / immune privilege. PIF also reduces spontaneous and LPS-induced foetal death in immune naïve murine model. We examined PIF effect on gene expression of human leukocyte antigen (HLA-G, -E -F and –C) and the influence of PIF on local progesterone activity in JEG-3 choriocarcinoma cells. Methods: PIF and progesterone (P4) effects on JEG-3 cells surface and intracellular HLA molecules was tested using monoclonal antibodies, flow cytometry, and Western blotting. PIF and IL17 effects on P4 and cytokines secretion was determined by ELISA. PIF and P4 effects on JEG-3 cells proteome was examined using 2D gel staining followed by spot analysis, mass spectrometry and bioinformatic analysis. Results: In cytotrophoblastic JEG-3 cells PIF increased intracellular expression of HLA-G, HLA-F, HLA-E and HLA-C and surface expression of HLA-G, HLA-E and HLA-C in dose and time dependent manner. In case of HLA-E, -F results were confirmed also by Western blot. Proteome analysis confirmed an increase in HLA-G, pro-tolerance FOXP3+ regulatory T cells (Tregs), coagulation factors and complement regulator. In contrast, PIF reduced PRDX2 and HSP70s to negate oxidative stress and protein misfolding. PIF enhanced local progesterone activity, increasing steroid secretion and the receptor protein. It also promoted the secretion of the Th1/Th2 cytokines (IL-10, IL-1β, IL-8, GM-CSF and TGF-β1), resulting in improved maternal signalling. Conclusion: PIF can generate a pro-tolerance milieu by enhancing the expression of HLA molecules and by amplifying endogenous progesterone activity. A Fast-Track clinical trial for autoimmune disease has been satisfactorily completed. The acquired data warrants PIF use for the treatment of early pregnancy disorders.

01 Nov 1979·British journal of pharmacology

Homogenates of rat placenta contain a factor(s) which inhibits uterine arachidonic acid metabolism [proceedings].

Article

Author: Williams, K I ; Harrowing, P D

RSC AdvancesQ3 · CHEMISTRY

The synthesis and properties of isocyanate-based polyimide foam composites containing MWCNTs of various contents and diameters

Q3 · CHEMISTRY

ArticleOA

Author: Zhang, Yudi ; Cao, Jingjing ; Deng, Yuyuan ; Yang, Fukai ; Xu, Xinyu

PIFs were synthesized usingin situpolymerization from PAPI, PMDA, and MWCNTs (0.05, 0.1, 0.2, 0.4, and 0.6 wt%) functionalized with –OH; the diameters were 10–20 nm, 20–30 nm, and >50 nm.

100 Deals associated with Fenofibrate/Pitavastatin Calcium

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