A Contemporary Overview of PPARα/γ Dual Agonists for the Management of Diabetic Dyslipidemia

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BACKGROUND: Diabetes mellitus and concomitant dyslipidemia, being referred to as 'diabetic dyslipidemia', are the foremost detrimental factors documented to play a pivotal role in cardiovascular illness. Diabetic dyslipidemia is associated with insulin resistance, high plasma triglyceride levels, low HDL-cholesterol concentration and elevated small dense LDL-cholesterol particles. Maintaining an optimal glucose and lipid levels in patients afflicted with diabetic dyslipidemia could be a major task that might require a well-planned diet-management system and regular physical activity, or otherwise an intake of combined antidiabetic and antihyperlipidemic medications. Synchronized treatment which efficiently controls insulin resistance-associated diabetes mellitus and co-existing dyslipidemia could indeed be a fascinating therapeutic option in the management of diabetic dyslipidemia. Peroxisome proliferator-activated receptors α/γ (PPARα/γ) dual agonists are such kind of drugs which possess therapeutic potentials to treat diabetic dyslipidemia. Nevertheless, PPARα/γ dual agonists like muraglitazar, naveglitazar, tesaglitazar, ragaglitazar and aleglitazar have been reported to have undesirable adverse effects, and their developments have been halted at various stages. On the other hand, a recently introduced PPARα/γ dual agonist, saroglitazar is an emerging therapeutic agent of glitazar class approved in India for the management of diabetic dyslipidemia, and its treatment has been reported to be generally safe and well tolerated.

CONCLUSION: Some additional and new compounds, at initial and preclinical stages, have been recently reported to possess PPARα/γ dual agonistic potentials with considerable therapeutic efficacy and reduced adverse profile. This review sheds light on the current status of various PPARα/γ dual agonists for the management of diabetic dyslipidemia.

Medienart:

E-Artikel

Erscheinungsjahr:

2019

Erschienen:

2019

Enthalten in:

Zur Gesamtaufnahme - volume:12

Enthalten in:

Current molecular pharmacology - 12(2019), 3 vom: 22., Seite 195-201

Sprache:

Englisch

Beteiligte Personen:

Balakumar, Pitchai [VerfasserIn]
Mahadevan, Nanjaian [VerfasserIn]
Sambathkumar, Ramanathan [VerfasserIn]

Links:

Volltext

Themen:

Adverse effects
Cardiovascular events
Diabetic dyslipidemia
E0YMX3S4JD
Insulin resistance
Journal Article
Oedema.
PPARα/γ dual agonists
PPAR alpha
PPAR gamma
Phenylpropionates
Pyrroles
Review
Saroglitazar

Anmerkungen:

Date Completed 26.03.2020

Date Revised 26.02.2021

published: Print

Citation Status MEDLINE

doi:

10.2174/1874467212666190111165015

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM292647654