General Information of Drug (ID: DM1975O)

Drug Name
Cilnidipine Drug Info
Synonyms
Atelec; Cinaldipine; Cinalong; Siscard; Cilnidipine [INN]; FRC 8653; Atelec (TN); FRC-8653; Cilnidipine (JAN/INN); (+-)-(E)-Cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate; 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl (2E)-3-phenyl-2-propenyl ester; 2-methoxyethyl (2E)-3-phenylprop-2-en-1-yl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate; 3-O-(2-methoxyethyl) 5-O-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Indication
Disease Entry ICD 11 Status REF
High blood pressure BA00 Phase 3 [1]
Cross-matching ID
PubChem CID
5282138
ChEBI ID
CHEMBL452076
CAS Number
CAS 132203-70-4
TTD Drug ID
DM1975O
VARIDT Drug ID
DR01023
INTEDE Drug ID
DR0323

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LOMERIZINE DME0TC8 Migraine 8A80 Approved [5]
Ziconotide DMSLJP4 Pain MG30-MG3Z Approved [6]
Hesperidin DMI5DW1 Vascular purpura 3B60 Approved [7]
Ralfinamide DMUNMY0 Neuropathic pain 8E43.0 Phase 3 [8]
CNV-2197944 DMLT7JV Pain MG30-MG3Z Phase 2 [9]
Ritanserin DM0X36Y Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [10]
CNSB-004 DMHAI0M Pain MG30-MG3Z Preclinical [11]
TH-9229 DMG1MPD Reperfusion injury ND56.Z Terminated [12]
PD-157667 DM61NFD N. A. N. A. Terminated [13]
PD-0204318 DMGKVPH Pain MG30-MG3Z Terminated [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Nifedipine DMSVOZT Angina pectoris BA40 Approved [15]
Clevidipine butyrate DMW4M97 Hypertension BA00-BA04 Approved [16]
Epalrestat DM5OGK0 Diabetic neuropathy 8C0Z Approved [17]
Otilonium bromide DM05968 Gastric motility disorder DA21 Approved [18]
Levamlodipine DM92S6N Hypertension BA00-BA04 Phase 4 [19]
Pinaverium bromide DM7OSHC Irritable bowel syndrome DD91.0 Phase 3 [18]
MEM-1003 DMYZU6G Bipolar disorder 6A60 Phase 2a [20]
Gallopamil DMXBR27 Asthma CA23 Phase 2 [21]
BAY-Y-5959 DMLO18H Cardiovascular disease BA00-BE2Z Phase 2 [22]
Furnidipine DME94QF Nerve injury ND56.4 Discontinued in Phase 3 [23]
⏷ 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 [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [25]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [26]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [27]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [30]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [31]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [25]
Verapamil DMA7PEW Angina pectoris BA40 Approved [32]
⏷ Show the Full List of 10 Drug(s)
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 [33]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [4]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [34]
Quercetin DM3NC4M Obesity 5B81 Approved [35]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [36]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [37]
Nisoldipine DM7ISKJ Hypertension BA00-BA04 Approved [4]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 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
Voltage-gated calcium channel alpha Cav2.2 (CACNA1B) TT4FDG6 CAC1B_HUMAN Blocker [2]
Voltage-gated L-type calcium channel (L-CaC) TTXHYV6 NOUNIPROTAC Blocker [2]

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

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Gene/Protein Processing [4]

References

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2 N- and L-type calcium channel antagonist improves glomerular dynamics, reverses severe nephrosclerosis, and inhibits apoptosis and proliferation in an l-NAME/SHR model. J Hypertens. 2002 May;20(5):993-1000.
3 Metabolism and metabolic inhibition of cilnidipine in human liver microsomes. Acta Pharmacol Sin. 2003 Mar;24(3):263-8.
4 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.
5 Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7.
6 Emerging treatments for traumatic brain injury. Expert Opin Emerg Drugs. 2009 Mar;14(1):67-84.
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8 Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
9 Clinical pipeline report, company report or official report of Convergence Pharmaceuticals Ltd.
10 N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12.
11 CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain. Pain Med. 2010 Feb;11(2):262-73.
12 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008159)
13 Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.
14 US patent application no. 2012,0172,429, Permanently charged sodium and calcium channel blockers as anti- inflammatory agents.
15 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
16 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
17 Recent updates of N-type calcium channel blockers with therapeutic potential for neuropathic pain and stroke. Curr Top Med Chem. 2009;9(4):377-95.
18 Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
19 Effects of (S)-amlodipine and (R)-amlodipine on L-type calcium channel current of rat ventricular myocytes and cytosolic calcium of aortic smooth muscle cells. Pharmazie. 2008 Jun;63(6):470-4.
20 Efficacy of MEM 1003, a novel calcium channel blocker, in delay and trace eyeblink conditioning in older rabbits. Neurobiol Aging. 2007 May;28(5):766-73.
21 Role of apoptosis in the kidney after reperfusion. Orv Hetil. 2008 Feb 17;149(7):305-15.
22 Hemodynamic effects of a calcium channel promoter, BAY y 5959, are preserved after chronic administration in ischemic heart failure in conscious dogs. J Pharmacol Exp Ther. 1998 Aug;286(2):760-6.
23 Q-type Ca2+ channels are located closer to secretory sites than L-type channels: functional evidence in chromaffin cells. Pflugers Arch. 1998 Mar;435(4):472-8.
24 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.
25 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
26 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.
27 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
28 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.
29 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.
30 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
31 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.
32 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.
33 Time series analysis of oxidative stress response patterns in HepG2: a toxicogenomics approach. Toxicology. 2013 Apr 5;306:24-34.
34 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.
35 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.
36 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.
37 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.
38 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.
39 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.