Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMAI7ZV)

Drug Name
Diltiazem Drug Info
Synonyms
Acalix; Adizem; Aldizem; Anoheal; Cardil; Cardizem; Citizem; Dilacor; Dilcontin; Dilren; Diltia; Diltiazemum; Dilticard; Diltzac; Dilzen; Endrydil; Viazem; Cardizen LA; Incoril AP; Tiazac Tildiem; Tiazac XC; Adizem (TN); Altiazem (TN); Angiozem (TN); Angizem (TN); Angizem CD (TN); Apo-Diltiaz; Cardizem (Hydrochloride); Cardizem (TN); Cartia XT (TN); Dilacor-XR; Dilatam (TN); Dilatem (TN); Dilcardia (TN); Dilcontin SR (TN); Dilt-cd; Dilta-Hexal; Diltelan (TN); Diltiazem (INN); Diltiazem [INN:BAN]; Diltiazemum [INN-Latin]; Diltime (TN); Dilzem (TN); Dyalec (TN); Filazem (TN); Herben (TN); Nu-Diltiaz; Progor (TN); RG 83606 (Hydrochloride); Surazem (TN); Tiamate (TN); Tiazac (TN); Tiazac XC (TN); Tildiem (TN); Vasmulax (TN); Viazem (TN); Zandil (TN); Zemtrial (TN); D-cis-Diltiazem; MK-793 (Malate); [(2S,3S)-5-(2-dimethylaminoethyl)-2-(4-methoxyphenyl)-4-oxo-2,3-dihydro-1,5-benzothiazepin-3-yl] acetate; Acetic acid (2S,3S)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester; (+)-cis-5-[2-(dimethylamino)ethyl]-2,3-dihydro-3-hydroxy-2-(p-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one acetate ester; (2S,3S)-5-(2-(dimethylamino)ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate; (2S,3S)-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate; (2S,3S)-5-[2-(dimethylamino)ethyl]-2-[4-(methyloxy)phenyl]-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate; (2S-cis)-3-(acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one
Indication
Disease Entry ICD 11 Status REF
Angina pectoris BA40 Approved [1]
Atrial fibrillation BC81.3 Approved [1]
Hypertension BA00-BA04 Approved [2]
Malignant essential hypertension BA00 Approved [1]
Therapeutic Class
Antihypertensive Agents
Cross-matching ID
PubChem CID
39186
ChEBI ID
CHEBI:101278
CAS Number
CAS 56209-45-1
TTD Drug ID
DMAI7ZV
VARIDT Drug ID
DR00656
INTEDE Drug ID
DR0509
ACDINA Drug ID
D00200

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1) TTFK1JQ CA2D1_HUMAN Blocker [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [6]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [6]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [7]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [8]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [9]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [10]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1) DTT CACNA2D1 5.083 4.833 5.343 2.536
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Angina pectoris
ICD Disease Classification BA40
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1) DTT CACNA2D1 9.36E-01 -0.03 -0.13
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1) DTT CACNA2D1 2.81E-05 -0.15 -0.68
P-glycoprotein 1 (ABCB1) DTP P-GP 1.24E-01 -4.12E-01 -4.68E-01
P-glycoprotein 1 (ABCB1) DTP P-GP 3.00E-02 -1.09E-02 -7.37E-02
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 2.41E-01 3.17E-02 2.29E-01
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 5.67E-01 5.11E-02 1.35E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 6.74E-01 5.99E-02 7.30E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.51E-01 1.59E-01 2.09E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.79E-03 1.32E-01 7.85E-01
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 1.82E-01 -1.71E-02 -9.86E-02
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 8.01E-02 6.73E-02 3.36E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 2.91E-04 1.41E-01 6.14E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 7.33E-02 5.59E-02 2.99E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 5.65E-03 -7.28E-02 -1.24E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 2.13E-01 4.03E-02 2.50E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 8.21E-02 8.17E-02 4.35E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Diltiazem 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: 2298).
3 Egr-1, the potential target of calcium channel blockers in cardioprotection with ischemia/reperfusion injury in rats. Cell Physiol Biochem. 2009;24(1-2):17-24.
4 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.
5 Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos. 2002 Aug;30(8):883-91.
6 Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
7 Effects of CYP3A4 inhibition by diltiazem on pharmacokinetics and dynamics of diazepam in relation to CYP2C19 genotype status. Drug Metab Dispos. 2001 Oct;29(10):1284-9.
8 Significant impacts of CYP3A4*1G and CYP3A5*3 genetic polymorphisms on the pharmacokinetics of diltiazem and its main metabolites in Chinese adult kidney transplant patients. J Clin Pharm Ther. 2016 Jun;41(3):341-7.
9 Role of CYP3A4 in human hepatic diltiazem N-demethylation: inhibition of CYP3A4 activity by oxidized diltiazem metabolites. J Pharmacol Exp Ther. 1997 Jul;282(1):294-300.
10 FDA Drug Development and Drug Interactions