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

General Information of Drug (ID: DMXBR27)

Drug Name
Gallopamil Drug Info
Synonyms
16662-47-8; methoxyverapamil; 5-((3,4-Dimethoxyphenethyl)(methyl)amino)-2-isopropyl-2-(3,4,5-trimethoxyphenyl)pentanenitrile; Galopamilo; Galopamilo [INN-Spanish]; Gallopamillum [INN-Latin]; Gallopamil [INN:BAN]; D600; D 600; C28H40N2O5; CHEBI:34772; (+/-)-Methoxyverapamil hydrochloride; 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-isopropyl-2-(3,4,5-trimethoxyphenyl)valeronitrile; Benzeneacetonitrile, alpha-(3-((2-(3,4-dimethoxyphenyl)ethyl)methylamino)propyl)-3,4,5-trimethoxy-alpha-(1-methylethyl)-; Methoxyverapamil; GSK 796406
Indication
Disease Entry ICD 11 Status REF
Asthma CA23 Phase 2 [1]
Hypertension BA00-BA04 Discontinued in Phase 1 [2]
Cross-matching ID
PubChem CID
1234
ChEBI ID
CHEBI:34772
CAS Number
CAS 16662-47-8
TTD Drug ID
DMXBR27
VARIDT Drug ID
DR00892
INTEDE Drug ID
DR0762

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]
Neutral endopeptidase (MME) TT5TKPM NEP_HUMAN Inhibitor [3]
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2 (ATP2A2) TTE6THL AT2A2_HUMAN Inhibitor [4]
Voltage-gated L-type calcium channel (L-CaC) TTXHYV6 NOUNIPROTAC Blocker [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Phase 2 [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 2 [7]

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
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
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 Asthma
ICD Disease Classification CA23
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
P-glycoprotein 1 (ABCB1) DTP P-GP 7.83E-01 4.69E-02 1.89E-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 ClinicalTrials.gov (NCT00896428) Effects of Gallopamil in Severe Asthma (REMODEL'ASTHME) in University Hospital, Bordeaux.
2 Mechanism of Vasopeptidase Inhibitor-Induced Plasma Extravasation: Comparison of Omapatrilat and the Novel Neutral Endopeptidase 24.11/Angiotensin-Converting Enzyme Inhibitor GW796406. JPET December 2005 vol. 315 no. 3 1306-1313.
3 Mechanism of vasopeptidase inhibitor-induced plasma extravasation: comparison of omapatrilat and the novel neutral endopeptidase 24.11/angiotensin-converting enzyme inhibitor GW796406. J Pharmacol Exp Ther. 2005 Dec;315(3):1306-13.
4 Interaction of D-600 with the transmembrane domain of the sarcoplasmic reticulum Ca(2+)-ATPase. Am J Physiol Cell Physiol. 2000 Jul;279(1):C166-72.
5 Role of apoptosis in the kidney after reperfusion. Orv Hetil. 2008 Feb 17;149(7):305-15.
6 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
7 Identification of human cytochrome P-450 isoforms involved in metabolism of R(+)- and S(-)-gallopamil: utility of in vitro disappearance rate. Drug Metab Dispos. 1999 Nov;27(11):1254-9.