General Information of Drug (ID: DM93VBZ)

Drug Name
LY2835219 Drug Info
Synonyms Abemaciclib; 1231929-97-7; Verzenio; LY-2835219; UNII-60UAB198HK; LY2835219 (free base);
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [1]
Solid tumour/cancer 2A00-2F9Z Phase 3 [2]
Cross-matching ID
PubChem CID
46220502
CAS Number
CAS 1231929-97-7
TTD Drug ID
DM93VBZ
VARIDT Drug ID
DR00097
INTEDE Drug ID
DR0028
ACDINA Drug ID
D00003

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cyclin-dependent kinase 4 (CDK4) TT0PG8F CDK4_HUMAN Modulator [3]
Cyclin-dependent kinase 6 (CDK6) TTO0FDJ CDK6_HUMAN Modulator [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Multidrug and toxin extrusion protein 2 (SLC47A2) DT3TX4H S47A2_HUMAN Approved [4]
Multidrug and toxin extrusion protein 1 (SLC47A1) DTZGT0P S47A1_HUMAN Approved [4]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_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]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Cyclin-dependent kinase 6 (CDK6) DTT CDK6 5.142 3.087 4.307 3.406
Cyclin-dependent kinase 4 (CDK4) DTT CDK4 7.414 7.821 7.812 7.719
Multidrug and toxin extrusion protein 1 (SLC47A1) DTP MATE1 8.272 1.766 7.501 1.202
Organic cation transporter 2 (SLC22A2) DTP `OCT2 3.766 3.548 7.303 3.548
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 Breast cancer
ICD Disease Classification 2C60-2C65
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Cyclin-dependent kinase 4 (CDK4) DTT CDK4 3.30E-72 0.65 2.39
Multidrug and toxin extrusion protein 1 (SLC47A1) DTP MATE1 1.37E-11 -4.84E-01 -6.68E-01
Organic cation transporter 2 (SLC22A2) DTP SLC22A2 6.98E-01 -1.97E-02 -8.16E-02
Multidrug and toxin extrusion protein 2 (SLC47A2) DTP MATE2 1.49E-18 1.67E-01 6.92E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 5.59E-39 -3.76E-01 -1.64E+00
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
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: 7382).
3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
4 Abemaciclib Inhibits Renal Tubular Secretion Without Changing Glomerular Filtration Rate. Clin Pharmacol Ther. 2019 May;105(5):1187-1195.
5 LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]-Abemaciclib.