General Information of Drug (ID: DMBY31K)

Drug Name
Rivoglitazone Drug Info
Synonyms CS-011; DE-101; Rivoglitazone (ophthalmic); Rivoglitazone (ophthalmic), Santen; CS-011 (ophthalmic), Santen
Indication
Disease Entry ICD 11 Status REF
Ocular inflammation 9C61.24 Phase 3 [1]
Cross-matching ID
PubChem CID
3055168
CAS Number
CAS 185428-18-6
TTD Drug ID
DMBY31K
INTEDE Drug ID
DR1432

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [5]
Progesterone DMUY35B Premature labour JB00 Approved [6]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [7]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [8]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [9]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [10]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [11]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [12]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [6]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [14]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [15]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [15]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [16]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [17]
Diclofenac DMPIHLS Osteoarthritis FA00-FA05 Approved [18]
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [19]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [15]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [20]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [23]
Diclofenac DMPIHLS Osteoarthritis FA00-FA05 Approved [13]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [24]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [20]
Ibuprofen DM8VCBE Pain MG30-MG3Z Approved [13]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [25]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [26]
Ezetimibe DM7A8TW Hypercholesterolaemia 5C80.0 Approved [27]
Simvastatin DM30SGU Hypercholesterolaemia 5C80.0 Approved [28]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Diclofenac DMPIHLS Osteoarthritis FA00-FA05 Approved [29]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [30]
Ibuprofen DM8VCBE Pain MG30-MG3Z Approved [13]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [31]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [32]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [25]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [26]
Ezetimibe DM7A8TW Hypercholesterolaemia 5C80.0 Approved [33]
Simvastatin DM30SGU Hypercholesterolaemia 5C80.0 Approved [28]
Losartan DM72JXH Hypertension BA00-BA04 Approved [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [34]
Pioglitazone DMKJ485 Diabetic complication 5A2Y Approved [35]
Lobeglitazone DMHY3IP Type-2 diabetes 5A11 Approved [36]
Rosiglitazone XR DMT45MU Type-2 diabetes 5A11 Approved [37]
Thiazolidinedione DMC1NBW Alzheimer disease 8A20 Approved [35]
Glitazone DMDN4A1 N. A. N. A. Phase 4 [38]
Muraglitazar DMG3NFZ N. A. N. A. Phase 3 [39]
Rosiglitazone + metformin DMPIDXT Diabetic complication 5A2Y Phase 3 [37]
Balaglitazone DMXBHR6 Type-1 diabetes 5A10 Phase 3 [40]
Ragaglitazar DMFSHEM Type-1 diabetes 5A10 Phase 3 [41]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Peroxisome proliferator-activated receptor gamma (PPAR-gamma) TTZMAO3 PPARG_HUMAN Agonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [4]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Substrate [4]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Substrate [4]

References

1 ClinicalTrials.gov (NCT00571519) Randomized, Double-blind, Active-controlled, Study of Rivoglitazone in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
2 A randomized-controlled trial to investigate the effects of rivoglitazone, a novel PPAR gamma agonist on glucose-lipid control in type 2 diabetes. Diabetes Obes Metab. 2011 Sep;13(9):806-13.
3 Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics of pioglitazone. Clin Pharmacol Ther. 2005 May;77(5):404-14.
4 In vitro metabolism of rivoglitazone, a novel peroxisome proliferator-activated receptor gama agonist, in rat, monkey, and human liver microsomes and freshly isolated hepatocytes. Drug Metab Dispos. 2011 Jul;39(7):1311-9.
5 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
6 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
7 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
8 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
9 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
10 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
11 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
12 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
13 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
14 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
15 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
16 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
17 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
18 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
19 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
20 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
21 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
22 Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22.
23 Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90.
24 Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600.
25 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
26 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
27 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
28 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
29 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
30 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
31 UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.
32 Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
33 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.
34 Expression of peroxisome proliferator-activated receptors (PPARs) in human urinary bladder carcinoma and growth inhibition by its agonists. Int J Cancer. 2003 May 1;104(5):597-602.
35 Functional PPAR-gamma receptor is a novel therapeutic target for ACTH-secreting pituitary adenomas. Nat Med. 2002 Nov;8(11):1281-7.
36 Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-gamma agonist, after a single oral administration in healthy female subjects. Clin Drug Investig. 2014 Jul;34(7):467-74.
37 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
38 Peroxisome proliferator-activated receptor alpha activators improve insulin sensitivity and reduce adiposity. J Biol Chem. 2000 Jun 2;275(22):16638-42.
39 Muraglitazar, a dual (alpha/gamma) PPAR activator: a randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with... Clin Ther. 2005 Aug;27(8):1181-95.
40 Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma () agonist.Mini Rev Med Chem.2012 Feb;12(2):87-97.
41 Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. J Clin Pharmacol. 2003 Nov;43(11):1244-56.