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-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [7]
Progesterone DMUY35B Premature labour JB00 Approved [8]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [10]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [11]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [12]
Etoposide DMNH3PG Solid tumour/cancer 2A00-2F9Z Approved [13]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [14]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [8]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [15]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Bacterial infection 1A00-1C4Z Approved [16]
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [17]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [18]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [19]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [18]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [18]
Progesterone DMUY35B Premature labour JB00 Approved [20]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [18]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [21]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [23]
Methotrexate DM2TEOL leukaemia 2A60-2B33 Approved [24]
Folic acid DMEMBJC Folate-deficiency anemia 3A02.Y Approved [25]
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [26]
Cisplatin DMRHGI9 Solid tumour/cancer 2A00-2F9Z Approved [27]
Progesterone DMUY35B Premature labour JB00 Approved [28]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [29]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [28]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [30]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [32]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [33]
Ribociclib succinate DM9CIUW Breast cancer 2C60-2C65 Approved [34]
Trilaciclib DMP5A4T Small-cell lung cancer 2C25.Y Approved [35]
LEE011 DMMX75K Breast cancer 2C60-2C65 Phase 3 [36]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [37]
P276-00 DM9DJL2 Mantle cell lymphoma 2A85.5 Phase 2 [38]
P-276 DMMJUHD Breast cancer 2C60-2C65 Phase 2 [39]
G1T38 DMQO2IT Breast cancer 2C60-2C65 Phase 2 [3]
GLR2007 DM7DWLY Glioblastoma of brain 2A00.00 Phase 1/2 [40]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [32]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [33]
Ribociclib succinate DM9CIUW Breast cancer 2C60-2C65 Approved [34]
Trilaciclib DMP5A4T Small-cell lung cancer 2C25.Y Approved [35]
LEE011 DMMX75K Breast cancer 2C60-2C65 Phase 3 [36]
G1T38 DMQO2IT Breast cancer 2C60-2C65 Phase 2 [3]
GLR2007 DM7DWLY Glioblastoma of brain 2A00.00 Phase 1/2 [40]
FCN-437 DMQ8VUW Breast cancer 2C60-2C65 Phase 1/2 [41]
FN-1501 DM7BMD6 Solid tumour/cancer 2A00-2F9Z Phase 1 [42]
G1T28-1 DML028U Solid tumour/cancer 2A00-2F9Z Phase 1 [33]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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 MOA REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [5]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]

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.
7 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
8 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
9 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
10 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
11 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
12 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
13 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
14 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
15 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
16 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
17 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
18 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
19 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
20 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
21 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
22 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
23 Doxorubicin transport by RALBP1 and ABCG2 in lung and breast cancer. Int J Oncol. 2007 Mar;30(3):717-25.
24 Wild-type breast cancer resistance protein (BCRP/ABCG2) is a methotrexate polyglutamate transporter. Cancer Res. 2003 Sep 1;63(17):5538-43.
25 The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. Mol Pharmacol. 2007 Jan;71(1):240-9.
26 Role of BCRP as a biomarker for predicting resistance to 5-fluorouracil in breast cancer. Cancer Chemother Pharmacol. 2009 May;63(6):1103-10.
27 Inhibiting the function of ABCB1 and ABCG2 by the EGFR tyrosine kinase inhibitor AG1478. Biochem Pharmacol. 2009 Mar 1;77(5):781-93.
28 Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51.
29 The phytoestrogen genistein enhances multidrug resistance in breast cancer cell lines by translational regulation of ABC transporters. Cancer Lett. 2016 Jun 28;376(1):165-72.
30 Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009 Feb;26(2):480-7.
31 Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. Blood. 2004 Nov 1;104(9):2940-2.
32 Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
33 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
34 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
35 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
36 Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
37 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
38 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
39 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.
40 Clinical pipeline report, company report or official report of Gan & Lee Pharmaceuticals.
41 Clinical pipeline report, company report or official report of Fochon Pharmaceuticals.
42 Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia. J Med Chem. 2018 Feb 22;61(4):1499-1518.