General Information of Drug (ID: DMJH792)

Drug Name
Pitavastatin Drug Info
Synonyms
Pitavastatin; Itavastatin; Livalo; NK 104; Pitavastatin [INN]; Pitavastatin calcium; UNII-M5681Q5F9P; NK-104; C25H24FNO4; M5681Q5F9P; Zypitamag; Flovas; (3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid; P 872441; P-872441; (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid; ( )-(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-3,5-dihydroxy-6-heptenoic acid; NK 104 (acid); Pitavastatin calcium (JAN)
Indication
Disease Entry ICD 11 Status REF
Hyperlipidemia 5C80.Z Approved [1]
Cross-matching ID
PubChem CID
5282452
ChEBI ID
CHEBI:32020
CAS Number
CAS 147511-69-1
TTD Drug ID
DMJH792
VARIDT Drug ID
DR01545

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTP
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [8]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [9]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [10]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [11]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [12]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [13]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [14]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [15]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [16]
Oxaliplatin DMQNWRD Colorectal cancer 2B91.Z Approved [17]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [18]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [19]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [20]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [21]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [22]
Progesterone DMUY35B Premature labour JB00 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [24]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [23]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [27]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [30]
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [29]
Pravastatin DM6A0X7 Hypercholesterolaemia 5C80.0 Approved [31]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [32]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [33]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [34]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [35]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [36]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [37]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [38]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [4]
Rosuvastatin DMMIQ7G Hypercholesterolaemia 5C80.0 Approved [39]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [40]
Enalapril DMNFUZR Hypertension BA00-BA04 Approved [41]
Cholic acid DM7OKQV Peroxisomal disorder 5C57 Approved [42]
Liothyronine DM6IR3P Hypothyroidism 5A00 Approved [43]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [44]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [45]
Diclofenac DMPIHLS Osteoarthritis FA00-FA05 Approved [46]
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [29]
Pravastatin DM6A0X7 Hypercholesterolaemia 5C80.0 Approved [47]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [32]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [34]
Erythromycin DM4K7GQ Bacterial infection 1A00-1C4Z Approved [7]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [48]
L-glutamic acid DM4PUDW Schizophrenia 6A20 Approved [49]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [50]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [30]
Pravastatin DM6A0X7 Hypercholesterolaemia 5C80.0 Approved [51]
Atorvastatin DMF28YC Cardiovascular disease BA00-BE2Z Approved [52]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [53]
Pitavastatin calcium DM1UJO0 Dyslipidemia 5C80-5C81 Approved [54]
Digoxin DMQCTIH Arrhythmia BC9Z Approved [55]
Rosuvastatin DMMIQ7G Hypercholesterolaemia 5C80.0 Approved [56]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [2]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [3]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Substrate [4]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [5]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [6]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [7]

References

1 Pitavastatin was approved by FDA. The official website of the U.S. Food and Drug Administration. (2019)
2 Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol. 2005 Sep;68(3):800-7.
3 Intestinal absorption of HMG-CoA reductase inhibitor pitavastatin mediated by organic anion transporting polypeptide and P-glycoprotein/multidrug resistance 1. Drug Metab Pharmacokinet. 2011;26(2):171-9.
4 Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005 Oct;57(10):1305-11.
5 ABCG2: a perspective. Adv Drug Deliv Rev. 2009 Jan 31;61(1):3-13.
6 Prediction of the in vivo OATP1B1-mediated drug-drug interaction potential of an investigational drug against a range of statins. Eur J Pharm Sci. 2012 Aug 30;47(1):244-55.
7 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
8 Involvement of the drug transporters p glycoprotein and multidrug resistance-associated protein Mrp2 in telithromycin transport. Antimicrob Agents Chemother. 2006 Jan;50(1):80-7.
9 Dose-dependent disposition of methotrexate in Abcc2 and Abcc3 gene knockout murine models. Drug Metab Dispos. 2011 Nov;39(11):2155-61.
10 Mammalian multidrug-resistance proteins (MRPs). Essays Biochem. 2011 Sep 7;50(1):179-207.
11 Enhancing chemosensitivity in oral squamous cell carcinoma by lentivirus vector-mediated RNA interference targeting EGFR and MRP2. Oncol Lett. 2016 Sep;12(3):2107-2114.
12 Multidrug resistance associated protein 2 mediates transport of prostaglandin E2. Liver Int. 2006 Apr;26(3):362-8.
13 Lentivirus-mediated RNAi silencing targeting ABCC2 increasing the sensitivity of a human nasopharyngeal carcinoma cell line against cisplatin. J Transl Med. 2008 Oct 4;6:55.
14 Effect of acetaminophen on expression and activity of rat liver multidrug resistance-associated protein 2 and P-glycoprotein. Biochem Pharmacol. 2004 Aug 15;68(4):791-8.
15 Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7.
16 Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anion transporter (cMOAT). Drug Metab Dispos. 2002 Apr;30(4):457-63.
17 Multidrug Resistance-Associated Protein 2 (MRP2) Mediated Transport of Oxaliplatin-Derived Platinum in Membrane Vesicles. PLoS One. 2015 Jul 1;10(7):e0130727.
18 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
19 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
20 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
21 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
22 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
23 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
24 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
25 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
26 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
27 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
28 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
29 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
30 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
31 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
32 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
33 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
34 FDA Drug Development and Drug Interactions
35 Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. J Pharmacol Exp Ther. 2006 Aug;318(2):521-9.
36 Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3. Pflugers Arch. 2001 Nov;443(2):188-95.
37 Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011 Jun;89(6):816-20.
38 Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol. 2010 Dec 1;80(11):1746-53.
39 Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806.
40 Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004 Jan 12;1(1):49-56.
41 Uptake of enalapril and expression of organic anion transporting polypeptide 1 in zonal, isolated rat hepatocytes. Drug Metab Dispos. 2000 Jul;28(7):801-6.
42 Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82.
43 Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Endocrinology. 2001 May;142(5):2005-12.
44 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
45 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
46 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
47 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
48 Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60.
49 The Transporter Classification Database (TCDB): recent advances. Nucleic Acids Res. 2016 Jan 4;44(D1):D372-9. (ID: 2.A.60.1.20)
50 Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP. J Pharm Sci. 2017 Sep;106(9):2688-2694.
51 Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45.
52 Human platelets express organic anion-transporting peptide 2B1, an uptake transporter for atorvastatin. Drug Metab Dispos. 2009 May;37(5):1129-37.
53 pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Mol Pharm. 2011 Aug 1;8(4):1303-13.
54 Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos. 2006 Jul;34(7):1229-36.
55 Drug Interactions in Infectious Diseases.
56 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.