Peringatan Keamanan

Lobeglitazone showed a similar adverse effect profile to pioglitazone, another thiazolidinedione medication from the same class. The most concerning side effects found were edema and weight gain, with no severe adverse effects. Notably, there were no observable changes to patients with heart failure, which is a concern associated with other medications of the same class A19751.

Lobeglitazone

DB09198

small molecule experimental

Deskripsi

Lobeglitazone is an antidiabetic medication from the thiazolidinedione class of drugs. It primarily functions as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By activating PPAR-gamma and promoting the binding of insulin at fat cells, lobeglitazone thereby has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles A19748. Unlike DB01132, which is a dual PPAR agonist at PPAR-alpha and PPAR-gamma, Lobeglitazone is a pure PPAR-alpha agonist.

Lobeglitazone was approved by the Ministry of Food and Drug Safety (South Korea) in 2013, and is being monitored by postmarketing surveillance until 2019. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.

Struktur Molekul 2D

Berat 480.54
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following an intravenous dosage of 1 mg/kg, the half life was found to be 110 min [A19749].
Volume Distribusi The steady state volume of distribution (Vss) of lobeglitazone was found to be 189–276 mL/kg. Vss was not found to vary statistically with the dose, suggesting that lobeglitazone follows linear kinetics [A19749].
Klirens (Clearance) In rat studies, systemic clearance was found to be between 1.95 and 2.19 mL/min/kg regardless of dosage [A19749].

Absorpsi

In rat studies, the AUC for the doses 0.5, 1, and 2 mg/kg, AUC values were determined to be 459, 514, and 481 ug min/mL respectively. Absoprtion occurs rapidly after administration, with Tmax of 67.5 and 48.8 min and a Cmax of 0.962 and 0.4.94 ug/mL following doses of 0.5 and 2 mg/kg, respectively. Absolute bioavailability after oral administration was nearly complete and apparently not affected by the dosage; 92.1% following a 0.5 mg/kg dose and 99.0% following a 2 mg/kg dose. Furthermore, the extent of LB remaining in the GI tract at 24 h was found to be negligible, with values less than 0.2% of the oral dose, suggesting that the intestinal absorption is complete in rats at the dose range studied A19749.

Metabolisme

Rat studies with lobeglitazone have suggested that it is primarily metabolized by cytochrome P450 (CYP) isozymes A19749, however the exact enzymes involved in its metabolism have yet to be elucidated. The structure of Lobeglitazone's five major metabolites have been characterized along with their pharmacokinetic parameters, and can be seen in the metabolism section below. In rat studies, demethylation and hydroxylation appear to be the primary metabolic pathways. The most abundant metabolite found in these studies was confirmed in vivo as M1, a demethylated derivative of lobeglitazone; its rate of formation was found to be approximately 0.216 ? 0.252 mL/min/kg, representing approximately 9.76% of the total lobeglitazone elimination in vivo in rats A19756.

Rute Eliminasi

It has been reported that the combined extent of the excretion of lobeglitazone to the bile, urine and intestine is low (less than 10% of total dose), suggesting that the major route of elimination for the drug involves its metabolism A19749.

Interaksi Obat

1064 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Lobeglitazone.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Lobeglitazone.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Lobeglitazone.
Mifepristone The serum concentration of Lobeglitazone can be increased when it is combined with Mifepristone.
Pregabalin The risk or severity of weight gain and edema formation can be increased when Pregabalin is combined with Lobeglitazone.
Agomelatine The serum concentration of Agomelatine can be increased when it is combined with Lobeglitazone.
Pirfenidone The metabolism of Pirfenidone can be decreased when combined with Lobeglitazone.
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Lobeglitazone.
Lipoic acid The risk or severity of hypoglycemia can be increased when Lipoic acid is combined with Lobeglitazone.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Lobeglitazone.
Moxifloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Moxifloxacin.
Grepafloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Grepafloxacin.
Enoxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Enoxacin.
Pefloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Pefloxacin.
Ciprofloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Ciprofloxacin.
Trovafloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Trovafloxacin.
Nalidixic acid The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Nalidixic acid.
Rosoxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Rosoxacin.
Cinoxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Cinoxacin.
Lomefloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Lomefloxacin.
Gatifloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Gatifloxacin.
Norfloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Norfloxacin.
Levofloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Levofloxacin.
Gemifloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Gemifloxacin.
Ofloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Ofloxacin.
Sparfloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Sparfloxacin.
Temafloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Temafloxacin.
Fleroxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Fleroxacin.
Technetium Tc-99m ciprofloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Technetium Tc-99m ciprofloxacin.
Garenoxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Garenoxacin.
Nemonoxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Nemonoxacin.
Flumequine The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Flumequine.
Enrofloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Enrofloxacin.
Orbifloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Orbifloxacin.
Sarafloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Sarafloxacin.
Difloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Difloxacin.
Pazufloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Pazufloxacin.
Prulifloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Prulifloxacin.
Delafloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Delafloxacin.
Sitafloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Sitafloxacin.
Oxolinic acid The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Oxolinic acid.
Rufloxacin The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Rufloxacin.
Pipemidic acid The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Pipemidic acid.
Methyclothiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Methyclothiazide.
Chlorthalidone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Chlorthalidone.
Bendroflumethiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Bendroflumethiazide.
Metolazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Metolazone.
Benzthiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Benzthiazide.
Hydroflumethiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Hydroflumethiazide.
Indapamide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Indapamide.
Chlorothiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Chlorothiazide.
Hydrochlorothiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Hydrochlorothiazide.
Trichlormethiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Trichlormethiazide.
Polythiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Polythiazide.
Quinethazone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Quinethazone.
Cyclopenthiazide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Cyclopenthiazide.
Epitizide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Epitizide.
Protriptyline Protriptyline may decrease the hypoglycemic activities of Lobeglitazone.
Amoxapine Amoxapine may decrease the hypoglycemic activities of Lobeglitazone.
Amineptine Amineptine may decrease the hypoglycemic activities of Lobeglitazone.
Dimetacrine Dimetacrine may decrease the hypoglycemic activities of Lobeglitazone.
Butriptyline Butriptyline may decrease the hypoglycemic activities of Lobeglitazone.
Dosulepin Dosulepin may decrease the hypoglycemic activities of Lobeglitazone.
Oxaprotiline Oxaprotiline may decrease the hypoglycemic activities of Lobeglitazone.
Opipramol Opipramol may decrease the hypoglycemic activities of Lobeglitazone.
Amitriptylinoxide Amitriptylinoxide may decrease the hypoglycemic activities of Lobeglitazone.
Dibenzepin Dibenzepin may decrease the hypoglycemic activities of Lobeglitazone.
Quinupramine Quinupramine may decrease the hypoglycemic activities of Lobeglitazone.
Melitracen Melitracen may decrease the hypoglycemic activities of Lobeglitazone.
Lofepramine Lofepramine may decrease the hypoglycemic activities of Lobeglitazone.
Iprindole Iprindole may decrease the hypoglycemic activities of Lobeglitazone.
Imipramine oxide Imipramine oxide may decrease the hypoglycemic activities of Lobeglitazone.
Tianeptine Tianeptine may decrease the hypoglycemic activities of Lobeglitazone.
Nortriptyline Nortriptyline may decrease the hypoglycemic activities of Lobeglitazone.
Desipramine Desipramine may decrease the hypoglycemic activities of Lobeglitazone.
Tolbutamide The therapeutic efficacy of Tolbutamide can be increased when used in combination with Lobeglitazone.
Glimepiride The therapeutic efficacy of Glimepiride can be increased when used in combination with Lobeglitazone.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Lobeglitazone.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Lobeglitazone.
Tolazamide The therapeutic efficacy of Tolazamide can be increased when used in combination with Lobeglitazone.
Glyburide The therapeutic efficacy of Glyburide can be increased when used in combination with Lobeglitazone.
Glipizide The therapeutic efficacy of Glipizide can be increased when used in combination with Lobeglitazone.
Gliclazide The therapeutic efficacy of Gliclazide can be increased when used in combination with Lobeglitazone.
Gliquidone The therapeutic efficacy of Gliquidone can be increased when used in combination with Lobeglitazone.
Glisoxepide The therapeutic efficacy of Glisoxepide can be increased when used in combination with Lobeglitazone.
Glibornuride The therapeutic efficacy of Glibornuride can be increased when used in combination with Lobeglitazone.
Carbutamide The therapeutic efficacy of Carbutamide can be increased when used in combination with Lobeglitazone.
Metahexamide The therapeutic efficacy of Metahexamide can be increased when used in combination with Lobeglitazone.
Canagliflozin Canagliflozin may increase the hypoglycemic activities of Lobeglitazone.
Leuprolide The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Leuprolide.
Goserelin The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Goserelin.
Ziprasidone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Ziprasidone.
Etonogestrel The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Etonogestrel.
Desogestrel The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Desogestrel.
Megestrol acetate The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Megestrol acetate.
Clozapine The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Clozapine.
Levonorgestrel The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Levonorgestrel.
Progesterone The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Progesterone.
Piperazine The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Piperazine.
Niacin The therapeutic efficacy of Lobeglitazone can be decreased when used in combination with Niacin.

Target Protein

Peroxisome proliferator-activated receptor alpha PPARA
Peroxisome proliferator-activated receptor gamma PPARG

Referensi & Sumber

Synthesis reference: Kim BY, Ahn JB, Lee HW, Kang SK, Lee JH, Shin JS, Ahn SK, Hong CI, Yoon SS: Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione. Eur J Med Chem. 2004 May;39(5):433-47.
Artikel (PubMed)
  • PMID: 27914133
    Lee YH, Kim JH, Kim SR, Jin HY, Rhee EJ, Cho YM, Lee BW: Lobeglitazone, a Novel Thiazolidinedione, Improves Non-Alcoholic Fatty Liver Disease in Type 2 Diabetes: Its Efficacy and Predictive Factors Related to Responsiveness. J Korean Med Sci. 2017 Jan;32(1):60-69. doi: 10.3346/jkms.2017.32.1.60.
  • PMID: 25648999
    Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ: Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3.
  • PMID: 25580775
    Jin SM, Park CY, Cho YM, Ku BJ, Ahn CW, Cha BS, Min KW, Sung YA, Baik SH, Lee KW, Yoon KH, Lee MK, Park SW: Lobeglitazone and pioglitazone as add-ons to metformin for patients with type 2 diabetes: a 24-week, multicentre, randomized, double-blind, parallel-group, active-controlled, phase III clinical trial with a 28-week extension. Diabetes Obes Metab. 2015 Jun;17(6):599-602. doi: 10.1111/dom.12435. Epub 2015 Feb 8.
  • PMID: 15110969
    Kim BY, Ahn JB, Lee HW, Kang SK, Lee JH, Shin JS, Ahn SK, Hong CI, Yoon SS: Synthesis and biological activity of novel substituted pyridines and purines containing 2,4-thiazolidinedione. Eur J Med Chem. 2004 May;39(5):433-47.
  • PMID: 26275726
    Lee JH, Ahn SH, Maeng HJ, Lee W, Kim DD, Chung SJ: The identification of lobeglitazone metabolites in rat liver microsomes and the kinetics of the in vivo formation of the major metabolite M1 in rats. J Pharm Biomed Anal. 2015 Nov 10;115:375-82. doi: 10.1016/j.jpba.2015.07.040. Epub 2015 Jul 30.

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