General Information of Drug (ID: DMLZIT2)

Drug Name
Dexniguldipine Drug Info
Synonyms Dexniguldipine hydrochloride; BY-935; B-8509-035; B-859-35
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [1] , [2]
Cross-matching ID
PubChem CID
6918097
ChEBI ID
CHEBI:103932
CAS Number
CAS 120054-86-6
TTD Drug ID
DMLZIT2
VARIDT Drug ID
DR01387
INTEDE Drug ID
DR0473

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Investigative Drug(s)
Clinical Trial Drug(s)
Discontinued 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 [7]
Progesterone DMUY35B Premature labour JB00 Approved [8]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [10]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [11]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [12]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [13]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [14]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [8]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [16]
Aminophenazone DMY2AH1 Anaesthesia 9A78.6 Phase 4 [17]
Sodium Phosphate, Dibasic, Anhydrous DM1G4S9 Discovery agent N.A. Investigative [18]
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Bacterial infection 1A00-1C4Z Approved [19]
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [20]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [21]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [22]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [21]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [21]
Progesterone DMUY35B Premature labour JB00 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [21]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Encequidar DMM8Z3Q Metastatic breast cancer 2C6Y Phase 2 [26]
LY335979 DM2KITF Acute myeloid leukaemia 2A60 Discontinued in Phase 3 [27]
Dofequidar fumarate DMWMHU7 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 3 [28]
LANIQUIDAR DM3YABD Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 2 [29]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Multidrug resistance protein 3 (ABCB4) TTJUXV6 MDR3_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [5]
Steroid 17-alpha-monooxygenase (CYP17A1) DEX2KIA CP17A_HUMAN Substrate [6]

References

1 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: 463).
2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002528)
3 Mechanism of action of dexniguldipine-HCl (B8509-035), a new potent modulator of multidrug resistance. Biochem Pharmacol. 1995 Mar 1;49(5):603-9.
4 Fingerprint-based in silico models for the prediction of P-glycoprotein substrates and inhibitors. Bioorg Med Chem. 2012 Sep 15;20(18):5388-95.
5 Integrated analysis on the physicochemical properties of dihydropyridine calcium channel blockers in grapefruit juice interactions. Curr Pharm Biotechnol. 2012 Jul;13(9):1705-17.
6 In vitro metabolism of dexamethasone (DEX) in human liver and kidney: the involvement of CYP3A4 and CYP17 (17,20 LYASE) and molecular modelling studies. Biochem Pharmacol. 1997 Sep 1;54(5):605-11.
7 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.
8 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
9 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.
10 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
11 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.
12 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.
13 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
14 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.
15 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.
16 Identifying susceptibility genes for prostate cancer--a family-based association study of polymorphisms in CYP17, CYP19, CYP11A1, and LH-beta. Cancer Epidemiol Biomarkers Prev. 2005 Aug;14(8):2035-9.
17 Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93.
18 Transcriptional complexes at the CYP17 CRS. Endocr Res. 2002 Nov;28(4):551-8.
19 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
20 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
21 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.
22 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
23 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
24 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
25 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.
26 Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor. J Med Chem. 2021 Apr 8;64(7):3677-3693.
27 A Phase I trial of a potent P-glycoprotein inhibitor, zosuquidar trihydrochloride (LY335979), administered intravenously in combination with doxoru... Clin Cancer Res. 2004 May 15;10(10):3265-72.
28 Reversal of multidrug resistance by a novel quinoline derivative, MS-209. Cancer Chemother Pharmacol. 1995;35(4):271-7.
29 Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats. Nucl Med Biol. 2009 Aug;36(6):643-9.