General Information of Drug (ID: DMNFUZR)

Drug Name
Enalapril Drug Info
Synonyms
Vasotec; Enalapril (INN); Enalapril (TN); N-{(1S)-1-[(ethyloxy)carbonyl]-3-phenylpropyl}-L-alanyl-L-proline; N-[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]-L-alanyl-L-proline; (2S)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]pyrrolidine-2-carboxylic acid
Indication
Disease Entry ICD 11 Status REF
Congestive heart failure BD10 Approved [1]
Hypertension BA00-BA04 Approved [2]
Malignant essential hypertension BA00 Approved [1]
Therapeutic Class
Antihypertensive Agents
Cross-matching ID
PubChem CID
5388962
ChEBI ID
CHEBI:4784
CAS Number
CAS 75847-73-3
TTD Drug ID
DMNFUZR
VARIDT Drug ID
DR00010
INTEDE Drug ID
DR0573
ACDINA Drug ID
D00229

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Angiotensin-converting enzyme (ACE) TTL69WB ACE_HUMAN Inhibitor [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Peptide transporter 2 (SLC15A2) DT8QKNP S15A2_HUMAN Approved [4]
Peptide transporter 1 (SLC15A1) DT9G7XN S15A1_HUMAN Approved [5]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Approved [6]
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTE2B1D SO1A2_HUMAN Approved [7]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [8]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Approved [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [9]
Carboxylesterase 1 (CES1) DEB30C5 EST1_HUMAN Approved [10]
Dipeptidase (pepV) DEQMBHW Q84BU9_LACLH Approved [11]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Angiotensin-converting enzyme (ACE) DTT SLC33A1 2.561 2.511 2.379 7.031
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.751 4.17 6.425 6.282
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 4.365 4.466 3.248 2.632
Peptide transporter 1 (SLC15A1) DTP PEPT1 3.807 4.52 5.285 7.133
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.873 2.17 2.485 3.322
Peptide transporter 2 (SLC15A2) DTP PEPT2 2.511 4.129 4.728 4.267
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
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 Congestive heart failure
ICD Disease Classification BD10
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Angiotensin-converting enzyme (ACE) DTT SLC33A1 2.62E-01 -0.01 -0.06
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 1.85E-02 5.14E-02 3.36E-01
Organic anion transporting polypeptide 1A2 (SLCO1A2) DTP OATP1A2 2.28E-01 -5.92E-02 -1.22E-01
Peptide transporter 1 (SLC15A1) DTP PEPT1 6.91E-01 8.30E-03 7.24E-02
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 3.85E-03 1.01E-01 7.72E-01
Peptide transporter 2 (SLC15A2) DTP PEPT2 8.33E-02 -3.63E-02 -1.27E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 8.47E-01 1.14E-02 8.20E-02
Carboxylesterase 1 (CES1) DME CES1 1.24E-01 1.06E-01 4.92E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 6.06E-01 -2.42E-02 -1.64E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Enalapril 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: 6322).
3 Determination of bezafibrate, methotrexate, cyclophosphamide, orlistat and enalapril in waste and surface waters using on-line solid-phase extracti... J Environ Monit. 2009 Apr;11(4):830-8.
4 Ethanol inhibits functional activity of the human intestinal dipeptide transporter hPepT1 expressed in Xenopus oocytes. Alcohol Clin Exp Res. 2008 May;32(5):777-84.
5 The intestinal H+/peptide symporter PEPT1: structure-affinity relationships. Eur J Pharm Sci. 2004 Jan;21(1):53-60.
6 Vectorial transport of enalapril by Oatp1a1/Mrp2 and OATP1B1 and OATP1B3/MRP2 in rat and human livers. J Pharmacol Exp Ther. 2006 Jul;318(1):395-402.
7 Uptake of enalapril and expression of organic anion transporting polypeptide 1 in zonal, isolated rat hepatocytes. Drug Metab Dispos. 2000 Jul;28(7):801-6.
8 The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein. Hepatology. 1998 Nov;28(5):1341-6.
9 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
10 Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: in vitro, in situ intestinal perfusion and portal vein cannulation models. Biopharm Drug Dispos. 2015 Sep;36(6):385-397.
11 Characterization and kinetic analysis of enzyme-substrate recognition by three recombinant lactococcal PepVs. Arch Biochem Biophys. 2006 Oct 15;454(2):137-45.