General Information of Drug Combination (ID: DC1ZBMR)

Drug Combination Name
Felodipine Felodipine
Indication
Disease Entry Status REF
Hypertension Phase 4 [1]
Component Drugs Felodipine   DMOSW35 Felodipine   DMOSW35
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Felodipine
Disease Entry ICD 11 Status REF
Hypertension BA00-BA04 Approved [2]
Felodipine Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Calcium channel unspecific (CaC) TT5HONZ NOUNIPROTAC Blocker [3]
------------------------------------------------------------------------------------
Felodipine Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]
------------------------------------------------------------------------------------
Felodipine Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [5]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [6]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [6]
------------------------------------------------------------------------------------
Felodipine Interacts with 18 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Expression [7]
Cytochrome P450 2C8 (CYP2C8) OTHCWT42 CP2C8_HUMAN Decreases Activity [8]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [9]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Increases Activity [7]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Expression [7]
Cytochrome P450 1A2 (CYP1A2) OTLLBX48 CP1A2_HUMAN Increases Expression [7]
Cytochrome P450 2A6 (CYP2A6) OT52TWG3 CP2A6_HUMAN Increases Expression [7]
Cytochrome P450 2C9 (CYP2C9) OTGLBN29 CP2C9_HUMAN Decreases Activity [7]
Cytochrome P450 2B6 (CYP2B6) OTOYO4S7 CP2B6_HUMAN Increases Expression [7]
Aryl hydrocarbon receptor (AHR) OTFE4EYE AHR_HUMAN Increases Activity [7]
Cytochrome P450 2J2 (CYP2J2) OTJBTEH8 CP2J2_HUMAN Decreases Activity [10]
Aurora kinase A (AURKA) OTMX0HYT AURKA_HUMAN Affects Binding [11]
Natriuretic peptides A (NPPA) OTMQNTNX ANF_HUMAN Affects Expression [12]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Increases Activity [13]
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Increases Activity [13]
Peroxisome proliferator-activated receptor delta (PPARD) OTI4WTOP PPARD_HUMAN Increases Activity [13]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [14]
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Increases Activity [13]
------------------------------------------------------------------------------------
⏷ Show the Full List of 18 DOT(s)
Indication(s) of Felodipine
Disease Entry ICD 11 Status REF
Hypertension BA00-BA04 Approved [2]
Felodipine Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Calcium channel unspecific (CaC) TT5HONZ NOUNIPROTAC Blocker [3]
------------------------------------------------------------------------------------
Felodipine Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]
------------------------------------------------------------------------------------
Felodipine Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [5]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [6]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Metabolism [6]
------------------------------------------------------------------------------------
Felodipine Interacts with 18 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Expression [7]
Cytochrome P450 2C8 (CYP2C8) OTHCWT42 CP2C8_HUMAN Decreases Activity [8]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [9]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Increases Activity [7]
Cytochrome P450 1A1 (CYP1A1) OTE4EFH8 CP1A1_HUMAN Increases Expression [7]
Cytochrome P450 1A2 (CYP1A2) OTLLBX48 CP1A2_HUMAN Increases Expression [7]
Cytochrome P450 2A6 (CYP2A6) OT52TWG3 CP2A6_HUMAN Increases Expression [7]
Cytochrome P450 2C9 (CYP2C9) OTGLBN29 CP2C9_HUMAN Decreases Activity [7]
Cytochrome P450 2B6 (CYP2B6) OTOYO4S7 CP2B6_HUMAN Increases Expression [7]
Aryl hydrocarbon receptor (AHR) OTFE4EYE AHR_HUMAN Increases Activity [7]
Cytochrome P450 2J2 (CYP2J2) OTJBTEH8 CP2J2_HUMAN Decreases Activity [10]
Aurora kinase A (AURKA) OTMX0HYT AURKA_HUMAN Affects Binding [11]
Natriuretic peptides A (NPPA) OTMQNTNX ANF_HUMAN Affects Expression [12]
Estrogen receptor (ESR1) OTKLU61J ESR1_HUMAN Increases Activity [13]
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Increases Activity [13]
Peroxisome proliferator-activated receptor delta (PPARD) OTI4WTOP PPARD_HUMAN Increases Activity [13]
Cytochrome P450 1B1 (CYP1B1) OTYXFLSD CP1B1_HUMAN Decreases Activity [14]
Bile acid receptor (NR1H4) OTWZLPTB NR1H4_HUMAN Increases Activity [13]
------------------------------------------------------------------------------------
⏷ Show the Full List of 18 DOT(s)

References

1 ClinicalTrials.gov (NCT00348686) Candesartan Effectiveness Study in Pro-B Type Natriuretic Peptides (BNP). U.S. National Institutes of Health.
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: 4190).
3 Molecular pharmacology of human Cav3.2 T-type Ca2+ channels: block by antihypertensives, antiarrhythmics, and their analogs. J Pharmacol Exp Ther. 2009 Feb;328(2):621-7.
4 The influence of CYP3A5*3 and BCRPC421A genetic polymorphisms on the pharmacokinetics of felodipine in healthy Chinese volunteers. J Clin Pharm Ther. 2017 Jun;42(3):345-349.
5 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
6 Drug Interactions Flockhart Table
7 Optical isomers of dihydropyridine calcium channel blockers display enantiospecific effects on the expression and enzyme activities of human xenobiotics-metabolizing cytochromes P450. Toxicol Lett. 2016 Nov 16;262:173-186.
8 Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78.
9 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
10 Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine. Chem Biol Interact. 2019 Jun 1;306:1-9.
11 A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition. Chem Biol Drug Des. 2016 Jun;87(6):958-67. doi: 10.1111/cbdd.12728. Epub 2016 Mar 21.
12 Effect of the calcium antagonist felodipine as supplementary vasodilator therapy in patients with chronic heart failure treated with enalapril: V-HeFT III. Vasodilator-Heart Failure Trial (V-HeFT) Study Group. Circulation. 1997 Aug 5;96(3):856-63. doi: 10.1161/01.cir.96.3.856.
13 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.
14 Association of CYP1A1 and CYP1B1 inhibition in in vitro assays with drug-induced liver injury. J Toxicol Sci. 2021;46(4):167-176. doi: 10.2131/jts.46.167.