General Information of Drug (ID: DM0C9IL)

Drug Name
Ranolazine Drug Info
Synonyms
RANOLAZINE; 95635-55-5; Ranexa; N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide; CVT-303; (-)-Ranolazine; Ranolazine (Ranexa); Ranolazine 2HCl; RS-43285-003; 142387-99-3; N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide; CHEBI:87690; N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide; C24H33N3O4; NCGC00015897-02; DSSTox_RID_80743; DSSTox_CID_25196; DSSTox_GSID_45196; Ran4; CVT 303; Latixa; RAN D; Latixa; Ranolazine dihydrochloride; KEG-1295; RS-43285; Ranexa (TN); Ranexa, Ranolazine; Ranolazine (USAN/INN); Ranolazine extended-release; Ranolazine/Dronedarone Fixed-Dose Combination
Indication
Disease Entry ICD 11 Status REF
Acute coronary syndrome BA41 Approved [1]
Angina pectoris BA40 Approved [1]
Chronic/stable angina BA40.1 Approved [2]
Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [1]
Paroxysmal atrial fibrillation BC81.30 Phase 2 [3]
Therapeutic Class
Analgesics
Cross-matching ID
PubChem CID
56959
ChEBI ID
CHEBI:87690
CAS Number
CAS 95635-55-5
TTD Drug ID
DM0C9IL
VARIDT Drug ID
DR00246
INTEDE Drug ID
DR1394
ACDINA Drug ID
D00584

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting Plasminogen (PLG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aminocaproic Acid DMFGND4 Bleeding disorder GA20-GA21 Approved [7]
Streptokinase DM5JQ0D Pulmonary embolism BB00 Approved [8]
Tranexamic Acid DMFI8A7 Excessive bleeding GA30.02 Approved [9]
Alteplase DMRJ3YX Acute myocardial infarction BA41 Approved [10]
Tenecteplase DMJYN25 Acute myocardial infarction BA41 Approved [10]
Anistreplase DM6Q4B0 Acute coronary syndrome BA41 Approved [11]
Reteplase DML0D1P Heart attack BA41 Approved [12]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [13]
Desmoteplase DMDLU4Z Ischemic stroke 8B11.5Z Phase 3 [14]
Plasminogen DM0EFQS Alzheimer disease 8A20 Phase 2/3 [15]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [16]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [17]
Methotrexate DM2TEOL Anterior urethra cancer Approved [18]
Folic Acid DMEMBJC Colorectal carcinoma Approved [19]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [18]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [18]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [20]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [18]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [21]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [23]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [26]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [27]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [28]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [29]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [30]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [24]
Verapamil DMA7PEW Angina pectoris BA40 Approved [31]
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Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [32]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [33]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [34]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [27]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [31]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [35]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [36]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [37]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [38]
Propranolol DM79NTF Angina pectoris BA40 Approved [39]
⏷ 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
Plasminogen (PLG) TTP86E2 PLMN_HUMAN Modulator [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [6]

References

1 Ranolazine FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7291).
3 Clinical pipeline report, company report or official report of Gilead.
4 Tranexamic acid in trauma: how should we use it. J Trauma Acute Care Surg. 2013 Jun;74(6):1575-86.
5 Ranolazine-tacrolimus interaction. Ann Pharmacother. 2010 Nov;44(11):1844-9.
6 Ranolazine: a contemporary review. J Am Heart Assoc. 2016 Mar 15;5(3):e003196.
7 The blockage of the high-affinity lysine binding sites of plasminogen by EACA significantly inhibits prourokinase-induced plasminogen activation. Biochim Biophys Acta. 2002 Apr 29;1596(2):182-92.
8 Acute anuric renal failure with streptokinase therapy in a patient with acute venous thromboembolic disease and the review of renal side effects of streptokinase. Tuberk Toraks. 2008;56(4):456-61.
9 Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8.
10 Thrombolytic therapies: the current state of affairs. J Endovasc Ther. 2005 Apr;12(2):224-32.
11 Evaluation of thrombolytic agents. Drugs. 1997;54 Suppl 3:11-6; discussion 16-7.
12 Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.
13 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
14 Vampire bat salivary plasminogen activator (desmoteplase): a unique fibrinolytic enzyme that does not promote neurodegeneration. Stroke. 2003 Feb;34(2):537-43.
15 Structure and function of the plasminogen/plasmin system. Thromb Haemost. 2005 Apr;93(4):647-54.
16 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
17 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
18 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
19 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
20 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
21 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
22 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
23 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.
24 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
25 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.
26 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
27 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.
28 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.
29 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
30 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.
31 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.
32 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
33 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
34 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
35 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
36 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
37 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
38 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
39 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.