General Information of Drug (ID: DMQP5I3)

Drug Name
Lacidipine Drug Info
Synonyms
Lacidipine; Lacidipine (Lacipil, Motens); Lacidipino; Lacidipino [Spanish]; Lacidipinum [Latin]; Lacimen; Lacipil; Motens; trans Lacidipine; 103890-78-4; 260080034N; 4-(o-((E)-2-Carboxyvinyl)phenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid, 4-tert-butyl diethyl ester; C26H33NO6; DSSTox_CID_26429; DSSTox_GSID_46429; DSSTox_RID_81607; GR 43659 X; GR 43659X; GR-43659X; GX-1048; UNII-260080034N; diethyl 2,6-dimethyl-4-[2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate
Cross-matching ID
PubChem CID
5311217
ChEBI ID
CHEBI:94480
CAS Number
CAS 103890-78-4
TTD Drug ID
DMQP5I3
INTEDE Drug ID
DR0910

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DME
DOT
Drug Status:
Approved 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 [3]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [4]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [6]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [7]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [8]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [9]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [10]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [4]
Verapamil DMA7PEW Angina pectoris BA40 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Estrogen receptor (ESR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [12]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [13]
Gefitinib DM15F0X Colon adenocarcinoma Approved [14]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [15]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [16]
Liraglutide DM3FXPS Non-insulin dependent diabetes 5A11 Approved [17]
Quercetin DM3NC4M Obesity 5B81 Approved [18]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [19]
Procaine DM4LSNE Anaesthesia 9A78.6 Approved [15]
Estrone DM5T6US Acne vulgaris ED80 Approved [20]
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Drug(s) Affected By Androgen receptor (AR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [21]
Nilutamide DMFN07X Prostate cancer 2C82.0 Approved [21]
Hydroxyflutamide DMGIZF5 Prostate cancer 2C82.0 Approved [21]
Enzalutamide DMGL19D Prostate cancer 2C82.0 Approved [22]
Bicalutamide DMZMSPF Prostate cancer 2C82.0 Approved [23]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [24]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [25]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [2]
Selenium DM25CGV N. A. N. A. Approved [26]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [28]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [29]
Quercetin DM3NC4M Obesity 5B81 Approved [30]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [31]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [32]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [33]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [34]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [35]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [36]
Stavudine DM6DEK9 Human immunodeficiency virus infection 1C62 Approved [37]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [38]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [39]
Methotrexate DM2TEOL Anterior urethra cancer Approved [40]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [41]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [42]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [43]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [44]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [45]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [46]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [47]
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Drug(s) Affected By Bile acid receptor (NR1H4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [48]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [2]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [49]
Quercetin DM3NC4M Obesity 5B81 Approved [50]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [51]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [52]
Nisoldipine DM7ISKJ Hypertension BA00-BA04 Approved [2]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [49]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [53]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [46]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Gene/Protein Processing [2]
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Gene/Protein Processing [2]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Gene/Protein Processing [2]
Peroxisome proliferator-activated receptor delta (PPARD) OTI4WTOP PPARD_HUMAN Gene/Protein Processing [2]
Peroxisome proliferator-activated receptor gamma (PPARG) OTHMARHO PPARG_HUMAN Gene/Protein Processing [2]
Vitamin D3 receptor OTFC7K35 VDR_HUMAN Gene/Protein Processing [2]

References

1 The effects of lacidipine on the steady/state plasma concentrations of simvastatin in healthy subjects. Br J Clin Pharmacol. 2001 Feb;51(2):147-52.
2 Quantitative high-throughput profiling of environmental chemicals and drugs that modulate farnesoid X receptor. Sci Rep. 2014 Sep 26;4:6437. doi: 10.1038/srep06437.
3 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.
4 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
5 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.
6 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
7 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.
8 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.
9 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
10 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.
11 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.
12 Estrogen-like activity of metals in MCF-7 breast cancer cells. Endocrinology. 2003 Jun;144(6):2425-36. doi: 10.1210/en.2002-221054.
13 Cross-talk between non-genomic and genomic signalling pathways--distinct effect profiles of environmental estrogens. Toxicol Appl Pharmacol. 2010 Jun 1;245(2):160-70. doi: 10.1016/j.taap.2010.02.015. Epub 2010 Mar 4.
14 Bidirectional cross talk between ERalpha and EGFR signalling pathways regulates tamoxifen-resistant growth. Breast Cancer Res Treat. 2006 Mar;96(2):131-46. doi: 10.1007/s10549-005-9070-2. Epub 2005 Oct 27.
15 Sensitivity of human dental pulp cells to eighteen chemical agents used for endodontic treatments in dentistry. Odontology. 2013 Jan;101(1):43-51.
16 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
17 Antitumoral activity of liraglutide, a new DNMT inhibitor in breast cancer cells in vitro and in vivo. Chem Biol Interact. 2021 Nov 1;349:109641. doi: 10.1016/j.cbi.2021.109641. Epub 2021 Sep 14.
18 Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on human breast cancer cells. Mol Pharmacol. 2001 Sep;60(3):595-602.
19 Novel retinoic acid metabolism blocking agents have potent inhibitory activities on human breast cancer cells and tumour growth. Br J Cancer. 2007 Apr 23;96(8):1204-15. doi: 10.1038/sj.bjc.6603705. Epub 2007 Mar 27.
20 Prediction of the combined effects of multiple estrogenic chemicals on MCF-7 human breast cancer cells and a preliminary molecular exploration of the estrogenic proliferative effects and related gene expression. Ecotoxicol Environ Saf. 2018 Sep 30;160:1-9. doi: 10.1016/j.ecoenv.2018.05.025. Epub 2018 May 21.
21 TBECH, 1,2-dibromo-4-(1,2 dibromoethyl) cyclohexane, alters androgen receptor regulation in response to mutations associated with prostate cancer. Toxicol Appl Pharmacol. 2016 Sep 15;307:91-101. doi: 10.1016/j.taap.2016.07.018. Epub 2016 Jul 27.
22 Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies. Nucleic Acids Res. 2015 Jul 13;43(12):5880-97. doi: 10.1093/nar/gkv262. Epub 2015 Apr 23.
23 Possible role of adaptive mutation in resistance to antiandrogen in prostate cancer cells. Prostate. 2005 Nov 1;65(3):268-75. doi: 10.1002/pros.20282.
24 Effects of the environmental estrogens bisphenol A, o,p'-DDT, p-tert-octylphenol and coumestrol on apoptosis induction, cell proliferation and the expression of estrogen sensitive molecular parameters in the human breast cancer cell line MCF-7. J Steroid Biochem Mol Biol. 2002 Jan;80(1):61-70. doi: 10.1016/s0960-0760(01)00173-x.
25 Identifying environmental chemicals as agonists of the androgen receptor by using a quantitative high-throughput screening platform. Toxicology. 2017 Jun 15;385:48-58. doi: 10.1016/j.tox.2017.05.001. Epub 2017 May 4.
26 Prostate specific antigen expression is down-regulated by selenium through disruption of androgen receptor signaling. Cancer Res. 2004 Jan 1;64(1):19-22. doi: 10.1158/0008-5472.can-03-2789.
27 Comparison of the Hershberger assay and androgen receptor binding assay of twelve chemicals. Toxicology. 2004 Feb 15;195(2-3):177-86. doi: 10.1016/j.tox.2003.09.012.
28 COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
29 Protective effects of myricitrin against osteoporosis via reducing reactive oxygen species and bone-resorbing cytokines. Toxicol Appl Pharmacol. 2014 Nov 1;280(3):550-60.
30 The effect of quercetin and kaempferol aglycones and glucuronides on peroxisome proliferator-activated receptor-gamma (PPAR-). Food Funct. 2015 Apr;6(4):1098-107. doi: 10.1039/c5fo00076a.
31 Induction of solid tumor differentiation by the peroxisome proliferator-activated receptor-gamma ligand troglitazone in patients with liposarcoma. Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):3951-6. doi: 10.1073/pnas.96.7.3951.
32 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
33 Glucosamine sulfate reduces prostaglandin E(2) production in osteoarthritic chondrocytes through inhibition of microsomal PGE synthase-1. J Rheumatol. 2012 Mar;39(3):635-44. doi: 10.3899/jrheum.110621. Epub 2011 Nov 15.
34 Isoniazid suppresses antioxidant response element activities and impairs adipogenesis in mouse and human preadipocytes. Toxicol Appl Pharmacol. 2013 Dec 15;273(3):435-41. doi: 10.1016/j.taap.2013.10.005. Epub 2013 Oct 12.
35 Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
36 Aspirin inhibits MMP-9 mRNA expression and release via the PPARalpha/gamma and COX-2/mPGES-1-mediated pathways in macrophages derived from THP-1 cells. Biomed Pharmacother. 2010 Feb;64(2):118-23. doi: 10.1016/j.biopha.2009.04.033. Epub 2009 Oct 17.
37 Mitochondrial proliferation, DNA depletion and adipocyte differentiation in subcutaneous adipose tissue of HIV-positive HAART recipients. Antivir Ther. 2003 Aug;8(4):323-31.
38 Cannabidiol induces antioxidant pathways in keratinocytes by targeting BACH1. Redox Biol. 2020 Jan;28:101321. doi: 10.1016/j.redox.2019.101321. Epub 2019 Sep 5.
39 Functional characterization of peroxisome proliferator-activated receptor-/ expression in colon cancer. Mol Carcinog. 2011 Nov;50(11):884-900. doi: 10.1002/mc.20757. Epub 2011 Mar 11.
40 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
41 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
42 Aspirin-induced apoptosis in jurkat cells is not mediated by peroxisome proliferator-activated receptor delta. Mol Cell Biochem. 2004 Nov;266(1-2):57-63. doi: 10.1023/b:mcbi.0000049138.67699.7b.
43 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
44 (9)-Tetrahydrocannabinol upregulates fatty acid 2-hydroxylase (FA2H) via PPAR induction: A possible evidence for the cancellation of PPAR/-mediated inhibition of PPAR in MDA-MB-231?cells. Arch Biochem Biophys. 2019 Feb 15;662:219-225. doi: 10.1016/j.abb.2018.12.011. Epub 2018 Dec 13.
45 Cross-talk between vitamin D receptor (VDR)- and peroxisome proliferator-activated receptor (PPAR)-signaling in melanoma cells. Anticancer Res. 2009 Sep;29(9):3647-58.
46 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
47 Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
48 Time series analysis of oxidative stress response patterns in HepG2: a toxicogenomics approach. Toxicology. 2013 Apr 5;306:24-34.
49 Potency of individual bile acids to regulate bile acid synthesis and transport genes in primary human hepatocyte cultures. Toxicol Sci. 2014 Oct;141(2):538-46. doi: 10.1093/toxsci/kfu151. Epub 2014 Jul 23.
50 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
51 The farnesoid X receptor FXRalpha/NR1H4 acquired ligand specificity for bile salts late in vertebrate evolution. Am J Physiol Regul Integr Comp Physiol. 2007 Sep;293(3):R1400-9. doi: 10.1152/ajpregu.00781.2006. Epub 2007 Jun 13.
52 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
53 Investigation of imatinib and other approved drugs as starting points for antidiabetic drug discovery with FXR modulating activity. Biochem Pharmacol. 2012 Jun 15;83(12):1674-81. doi: 10.1016/j.bcp.2012.02.027. Epub 2012 Mar 7.