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

General Information of Drug (ID: DMHZCPO)

Drug Name
Ibrutinib Drug Info
Synonyms PCI-32765; Ibrutinib (BTK inhibitor)
Indication
Disease Entry ICD 11 Status REF
Mantle cell lymphoma 2A85.5 Approved [1]
Small lymphocytic lymphoma 2A82.0 Approved [2]
Waldenstrom macroglobulinemia 2A85.4 Approved [2]
B-cell non-hodgkin lymphoma 2B33.5 Phase 3 [3]
Diffuse large B-cell lymphoma 2A81 Phase 3 [3]
Follicular lymphoma 2A80 Phase 3 [3]
Non-hodgkin lymphoma 2B33.5 Phase 3 [3]
Pancreatic cancer 2C10 Phase 3 [3]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 2 [4]
Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
Cross-matching ID
PubChem CID
24821094
ChEBI ID
CHEBI:76612
CAS Number
CAS 936563-96-1
TTD Drug ID
DMHZCPO
VARIDT Drug ID
DR01270
INTEDE Drug ID
DR0843
ACDINA Drug ID
D01146

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Tyrosine-protein kinase BTK (ATK) TTGM6VW BTK_HUMAN Inhibitor [5]

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

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [7]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [7]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [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
Tyrosine-protein kinase BTK (ATK) DTT BTK 3.838 3.897 5.053 5.897
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
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 Mantle cell lymphoma
ICD Disease Classification 2A85.5
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Tyrosine-protein kinase BTK (ATK) DTT BTK 3.54E-01 0.24 0.56
P-glycoprotein 1 (ABCB1) DTP P-GP 7.45E-02 -1.49E-01 -3.47E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 1.34E-01 -2.79E-01 -7.05E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 1.61E-03 -6.79E-01 -2.18E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 9.81E-01 2.72E-01 6.95E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 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: 6912).
2 Ibrutinib FDA Label
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Ibrutinib for the Treatment of COVID-19 in Patients Requiring Hospitalization
5 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. (Target id: 1948).
6 P-Glycoprotein (MDR1/ABCB1) Restricts Brain Penetration of the Bruton's Tyrosine Kinase Inhibitor Ibrutinib, While Cytochrome P450-3A (CYP3A) Limits Its Oral Bioavailability. Mol Pharm. 2018 Nov 5;15(11):5124-5134.
7 Absorption, metabolism, and excretion of oral 14C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97.