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

General Information of Drug (ID: DMD7L94)

Drug Name
Palbociclib Drug Info
Synonyms
571190-30-2; PD0332991; PD-0332991; Ibrance; PD 0332991; UNII-G9ZF61LE7G; Palbociclib(PD0332991); 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazin-1-yl)pyridin-2-yl]amino]-8H-pyrido[2,3-d]pyrimidin-7-one; 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one; G9ZF61LE7G; PD 332991; 6-ACETYL-8-CYCLOPENTYL-5-METHYL-2-[(5-PIPERAZIN-1-YLPYRIDIN-2-YL)AMINO]PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE; LQQ; PD 332991, PD 0332991, PD0332991; 6-Acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-ylpyridin-2-ylamino)-8H-pyrido(2,3-d)pyrimidin-7-one; 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one; HMR-2934
Indication
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Approved [1]
Solid tumour/cancer 2A00-2F9Z Phase 2 [2] , [3]
Schizophrenia 6A20 Terminated [4]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
5330286
ChEBI ID
CHEBI:85993
CAS Number
CAS 571190-30-2
TTD Drug ID
DMD7L94
VARIDT Drug ID
DR01288
INTEDE Drug ID
DR1229
ACDINA Drug ID
D00504

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 [1]
Cyclin-dependent kinase 6 (CDK6) TTO0FDJ CDK6_HUMAN Modulator [1]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [5]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [6]

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
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
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
P-glycoprotein 1 (ABCB1) DTP P-GP 3.12E-33 -8.30E-01 -1.04E+00
Breast cancer resistance protein (ABCG2) DTP BCRP 3.87E-47 -1.28E+00 -1.63E+00
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 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
2 ClinicalTrials.gov (NCT01723774) PD 0332991 and Anastrozole for Stage 2 or 3 Estrogen Receptor Positive and HER2 Negative Breast Cancer. U.S. National Institutes of Health.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
5 Efflux transporters at the blood-brain barrier limit delivery and efficacy of cyclin-dependent kinase 4/6 inhibitor palbociclib (PD-0332991) in an orthotopic brain tumor model. J Pharmacol Exp Ther. 2015 Nov;355(2):264-71.
6 Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105.