Details
Stereochemistry | RACEMIC |
Molecular Formula | C18H19N3O3S |
Molecular Weight | 357.427 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(CCOC1=CC=C(CC2SC(=O)NC2=O)C=C1)C3=CC=CC=N3
InChI
InChIKey=YASAKCUCGLMORW-UHFFFAOYSA-N
InChI=1S/C18H19N3O3S/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15/h2-9,15H,10-12H2,1H3,(H,20,22,23)
Molecular Formula | C18H19N3O3S |
Molecular Weight | 357.427 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/rosiglitazone.html
http://www.rxlist.com/avandia-drug.htm
http://www.wikidoc.org/index.php/Rosiglitazone
Curator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/rosiglitazone.html
http://www.rxlist.com/avandia-drug.htm
http://www.wikidoc.org/index.php/Rosiglitazone
Rosiglitazone acts as a highly selective and potent agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. It is FDA approved for the treatment of as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Inhibitors of CYP2C8 (e.g., gemfibrozil) may increase rosiglitazone levels; inducers of CYP2C8 (e.g., rifampin) may decrease rosiglitazone levels. Common adverse reactions include edema, weight gain, and headache.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
40.0 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | AVANDIA Approved UseAfter consultation with a healthcare professional who has considered and advised the patient of the risks and benefits of rosiglitazone, AVANDAMET® is indicated as an adjunct to diet and exercise to improve glycemic control when treatment with both rosiglitazone and metformin is appropriate in adults with type 2 diabetes mellitus who either are: already taking rosiglitazone, or not already taking rosiglitazone and unable to achieve glycemic control on other diabetes medications and, in consultation with their healthcare provider, have decided not to take pioglitazone (ACTOS®) or pioglitazone-containing products (ACTOPLUS MET®, ACTOPLUS MET XR®, DUETACT®) for medical reasons. Other Important Limitations of Use: Due to its mechanism of action, rosiglitazone is active only in the presence of endogenous insulin. Therefore, AVANDAMET should not be used in patients with type 1 diabetes. Coadministration of AVANDAMET with insulin is not recommended [see Warnings and Precautions (5.2, 5.3) Launch Date1999 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
432 ng/mL DRUG LABEL https://www.fda.gov/media/75754/download |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
ROSIGLITAZONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
598 ng/mL DRUG LABEL https://www.fda.gov/media/75754/download |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
ROSIGLITAZONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2890 ng × h/mL DRUG LABEL https://www.fda.gov/media/75754/download |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
ROSIGLITAZONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
2971 ng × h/mL DRUG LABEL https://www.fda.gov/media/75754/download |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
ROSIGLITAZONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.59 h DRUG LABEL https://www.fda.gov/media/75754/download |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
ROSIGLITAZONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FED |
|
3.37 h DRUG LABEL https://www.fda.gov/media/75754/download |
8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered: |
ROSIGLITAZONE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.105 |
unhealthy, 53.1 n = 32 Health Status: unhealthy Condition: Nonalcoholic steatohepatitis Age Group: 53.1 Sex: M+F Population Size: 32 Sources: Page: p.105 |
DLT: Headache, Malaise... Disc. AE: Pain in leg... Dose limiting toxicities: Headache (3.1%) AEs leading toMalaise (3.1%) Oedema legs (9.4%) discontinuation/dose reduction: Pain in leg (3.1%) Sources: Page: p.105 |
20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: Page: p.73,74 |
unhealthy, 60 n = 1 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 60 Sex: M Population Size: 1 Sources: Page: p.73,74 |
Disc. AE: Macular edema... AEs leading to discontinuation/dose reduction: Macular edema Sources: Page: p.73,74 |
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Disc. AE: Congestive heart failure, Myocardial ischemia... AEs leading to discontinuation/dose reduction: Congestive heart failure Sources: Page: p.1Myocardial ischemia (2%) Fluid retention Edema Weight gain Anemia Macular edema Fracture bone |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Headache | 3.1% DLT |
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.105 |
unhealthy, 53.1 n = 32 Health Status: unhealthy Condition: Nonalcoholic steatohepatitis Age Group: 53.1 Sex: M+F Population Size: 32 Sources: Page: p.105 |
Malaise | 3.1% DLT |
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.105 |
unhealthy, 53.1 n = 32 Health Status: unhealthy Condition: Nonalcoholic steatohepatitis Age Group: 53.1 Sex: M+F Population Size: 32 Sources: Page: p.105 |
Pain in leg | 3.1% Disc. AE |
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.105 |
unhealthy, 53.1 n = 32 Health Status: unhealthy Condition: Nonalcoholic steatohepatitis Age Group: 53.1 Sex: M+F Population Size: 32 Sources: Page: p.105 |
Oedema legs | 9.4% DLT |
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.105 |
unhealthy, 53.1 n = 32 Health Status: unhealthy Condition: Nonalcoholic steatohepatitis Age Group: 53.1 Sex: M+F Population Size: 32 Sources: Page: p.105 |
Macular edema | Disc. AE | 20 mg single, oral Overdose Dose: 20 mg Route: oral Route: single Dose: 20 mg Sources: Page: p.73,74 |
unhealthy, 60 n = 1 Health Status: unhealthy Condition: Type 2 diabetes mellitus Age Group: 60 Sex: M Population Size: 1 Sources: Page: p.73,74 |
Myocardial ischemia | 2% Disc. AE |
8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Anemia | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Congestive heart failure | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Edema | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Fluid retention | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Fracture bone | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Macular edema | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
Weight gain | Disc. AE | 8 mg 1 times / day multiple, oral Recommended Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Type 2 diabetes mellitus Sources: Page: p.1 |
PubMed
Title | Date | PubMed |
---|---|---|
Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors. | 2000 Mar |
|
Troglitazone inhibits mitogenic signaling by insulin in vascular smooth muscle cells. | 2000 May |
|
Activation of peroxisome proliferator-activated receptor gamma suppresses nuclear factor kappa B-mediated apoptosis induced by Helicobacter pylori in gastric epithelial cells. | 2001 Aug 17 |
|
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight. | 2001 Dec 17 |
|
Troglitazone and rosiglitazone induce apoptosis of vascular smooth muscle cells through an extracellular signal-regulated kinase-independent pathway. | 2001 Feb |
|
Fatty-acyl-CoA thioesters inhibit recruitment of steroid receptor co-activator 1 to alpha and gamma isoforms of peroxisome-proliferator-activated receptors by competing with agonists. | 2001 Jan 15 |
|
Troglitazone treatment increases plasma vascular endothelial growth factor in diabetic patients and its mRNA in 3T3-L1 adipocytes. | 2001 May |
|
Novel genes regulated by the insulin sensitizer rosiglitazone during adipocyte differentiation. | 2002 Apr |
|
Unique ability of troglitazone to up-regulate peroxisome proliferator-activated receptor-gamma expression in hepatocytes. | 2002 Jan |
|
Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB. | 2002 Jan 11 |
|
Troglitazone inhibits both post-glutamate neurotoxicity and low-potassium-induced apoptosis in cerebellar granule neurons. | 2002 Jan 11 |
|
Ligands of the peroxisome proliferator-activated receptors (PPAR-gamma and PPAR-alpha) reduce myocardial infarct size. | 2002 Jul |
|
Peroxisome proliferator-activated receptor agonists inhibit inflammatory edema and hyperalgesia. | 2002 Jun |
|
Comparative effects of thiazolidinediones on in vitro P450 enzyme induction and inhibition. | 2003 Apr |
|
Essential requirements for substrate binding affinity and selectivity toward human CYP2 family enzymes. | 2003 Jan 1 |
|
A yeast two-hybrid technology-based system for the discovery of PPARgamma agonist and antagonist. | 2004 Dec 15 |
|
Reduction of intracellular cholesterol accumulation in THP-1 macrophages by a combination of rosiglitazone and atorvastatin. | 2004 Jul 1 |
|
PPAR(gamma) agonist rosiglitazone improves vascular function and lowers blood pressure in hypertensive transgenic mice. | 2004 Mar |
|
Rosiglitazone improves insulin sensitivity, glucose tolerance and ambulatory blood pressure in subjects with impaired glucose tolerance. | 2004 May |
|
Hepatic lipase mRNA, protein, and plasma enzyme activity is increased in the insulin-resistant, fructose-fed Syrian golden hamster and is partially normalized by the insulin sensitizer rosiglitazone. | 2004 Nov |
|
Comparison of the effects of pioglitazone and rosiglitazone on macrophage foam cell formation. | 2004 Oct 22 |
|
Rosiglitazone treatment improves insulin regulation and dyslipidemia in type 2 diabetic cynomolgus monkeys. | 2004 Sep |
|
Altered adipokine response in murine 3T3-F442A adipocytes treated with protease inhibitors and nucleoside reverse transcriptase inhibitors. | 2005 |
|
The antidiabetic agent rosiglitazone upregulates SERCA2 and enhances TNF-alpha- and LPS-induced NF-kappaB-dependent transcription and TNF-alpha-induced IL-6 secretion in ventricular myocytes. | 2005 |
|
Effect of rosiglitazone and 15-deoxy-Delta12,14-prostaglandin J2 on bleomycin-induced lung injury. | 2005 Feb |
|
Mechanism of the anti-inflammatory effect of thiazolidinediones: relationship with the glucocorticoid pathway. | 2005 May |
|
Trialkyltin compounds bind retinoid X receptor to alter human placental endocrine functions. | 2005 Oct |
Sample Use Guides
Start at 4 mg daily in single or divided doses; do not exceed 8 mg daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18039959
Rosiglitazone treatment (5 uM) prevents NO and prostacyclin overproduction by inhibiting microparticles-induced iNOS and COX-2 expression.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:18:29 GMT 2023
by
admin
on
Fri Dec 15 16:18:29 GMT 2023
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Record UNII |
05V02F2KDG
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C98241
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N0000011272
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A10BD03
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NBK548114
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N0000180190
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A10BD04
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QA10BG02
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N0000175374
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C1934
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QA10BD04
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A10BG02
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N0000170119
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N0000011272
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QA10BD03
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N0000180186
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N0000170119
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N0000011272
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Rosiglitazone
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ROSIGLITAZONE
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PRIMARY | RxNorm |
Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
Binding Assay
IC50
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SALT/SOLVATE -> PARENT | |||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT | |||
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ENANTIOMER -> RACEMATE | |||
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BINDER->LIGAND |
BINDING
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> INHIBITOR |
SUBSTRATE USED: Bromsulphthalein (BSP)
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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ENANTIOMER -> RACEMATE |
Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT |
MINOR
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METABOLITE ACTIVE -> PARENT |
MAJOR
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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