Lobeglitazone (trade name Duvie,
Chong Kun Dang) is an
antidiabetic drug
Drugs used in diabetes treat diabetes mellitus by altering the glucose level in the blood. With the exceptions of insulin, most GLP receptor agonists ( liraglutide, exenatide, and others), and pramlintide, all are administered orally and are t ...
in the
thiazolidinedione
The thiazolidinediones , abbreviated as TZD, also known as glitazones after the prototypical drug ciglitazone, are a class of heterocyclic compounds consisting of a five-membered C3NS ring. The term usually refers to a family of drugs used i ...
class of drugs. As an
agonist for both
PPARα
Peroxisome proliferator-activated receptor alpha (PPAR-α), also known as NR1C1 (nuclear receptor subfamily 1, group C, member 1), is a nuclear receptor protein functioning as a transcription factor that in humans is encoded by the ''PPARA'' gen ...
and
PPARγ
Peroxisome proliferator- activated receptor gamma (PPAR-γ or PPARG), also known as the glitazone reverse insulin resistance
receptor, or NR1C3 (nuclear receptor subfamily 1, group C, member 3) is a type II nuclear receptor functioning as a tran ...
, it works as an
insulin sensitizer by binding to the
PPAR receptors in fat cells and making the cells more responsive to insulin.
Medical uses
Lobeglitazone is used to assist regulation of blood glucose level of diabetes mellitus type 2 patients. It can be used alone or in combination with metformin.
Lobeglitazone was approved by the Ministry of Food and Drug Safety (Korea) in 2013, and the
postmarketing surveillance Postmarketing surveillance (PMS), also known as post market surveillance, is the practice of monitoring the safety of a pharmaceutical drug or medical device after it has been released on the market and is an important part of the science of phar ...
is on progress until 2019.
Pharmacokinetics
The absolute bioavailability of lobeglitazone is about 95% in rat.
In human, the mean steady state clearance (CL
ss/F) was 1.13 L/h across in 1 to 4 mg dose range. In the dose range, the mean half-life was 10.3 h.
Urine excretion was negligible amount in elimination of lobeglitazone in rat and human.
The plasma protein binding of the drug is over 99%.
The average blood-to-plasma concentration ratio was 0.636. The unbound fraction of lobeglitazone in microsomal incubation medium was 0.479.
Lobeglitazone was primarily distributed to the liver with tissue-to-plasma concentration ratio as 5.59, and less to heart, lung, and fat. The tissue to plasma concentration ratios were ranged from about 0.25 to 4.0 for major tissues, in rat.
Among six major membrane transporters recommended by the United States Food and Drug Administration, lobeglitazone interacts with OATP1B1, OAT3, and MDR1.
In vitro, lobeglitazone was a substrate of rodent OATP1B2.
Lobeglitazone interacted with CYP1A2, 2C9 and 2C19.
Distribution to liver of lobeglitazone was inhibited by atorvastatin, in rats.
References
{{portal bar , Medicine
Anti-diabetic drugs
Pyrimidines
Thiazolidinediones