Palbociclib

Identification

Summary

Palbociclib is an endocrine-based chemotherapeutic agent used in combination with other antineoplastic agents to treat HER2-negative and HR-positive advanced or metastatic breast cancer.

Brand Names
Ibrance
Generic Name
Palbociclib
DrugBank Accession Number
DB09073
Background

Palbociclib is a piperazine pyridopyrimidine3 that acts in the cell cycle machinery. It is a second generation cyclin-dependent kinase inhibitor4 selected from a group of pyridopyrimidine compounds due to its favorable physical and pharmaceutical properties.5

Palbociclib was developed by Pfizer Inc after the discovery that identified the cyclin-dependent kinases as key regulators of cell growth.8 It was originally FDA approved on March 2015 for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer and its indications were updated in April 2019 to include male patients based on findings from postmarketing reports and electronic health records demonstrating safety and clinical efficacy.7

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 447.5328
Monoisotopic: 447.238273207
Chemical Formula
C24H29N7O2
Synonyms
  • 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one
  • Palbociclib
External IDs
  • PD 0332991
  • PD 332991
  • PD-0332991
  • PD-332991
  • PD0332991
  • PD332991

Pharmacology

Indication

Palbociclib is indicated in combination with letrozole as initial endocrine-based therapy for the treatment of human epidermal growth factor receptor type 2 (HER2)-negative and hormone receptor(HR)-positive tumors in adult patients with advanced/metastatic breast cancer. It is as well approved in combination with fulvestrant in patients with disease progression with prior endocrine therapy.1

In the official labeling, the use of palbociclib should be accompanied with either an aromatase inhibition, no restricted to letrozole, as initial endocrine-based therapy in postmenopausal women or in man.12

The breast cancer starts as a group of cancer cells that grow into and destroy the nearby breast tissue. This growth can spread into other parts of the body which is called metastasis. According to the location of the cancer cells, it can be categorized in ductal carcinoma and lobular carcinoma. However, other types of breast cancer include inflammatory breast cancer, Paget disease of the breast, triple negative breast cancer non-Hodgkin lymphoma and soft tissue sarcoma.9 In males, breast cancer is usually treated as the cases of postmenopausal women and almost all the cases are ductal carcinoma.10

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAdvanced breast cancerRegimen in combination with: Fulvestrant (DB00947)••••••••••••••••• ••••••••• •••••••• ••••••••••••••••••••••
Used in combination to treatMetastatic breast cancerRegimen in combination with: Fulvestrant (DB00947)••••••••••••••••• ••••••••• •••••••• ••••••••••••••••••••••
Used in combination to treatRefractory, advanced breast cancerRegimen in combination with: Letrozole (DB01006)••••••••••••••••••••••••••••••••••
Used in combination to treatRefractory, metastatic breast cancerRegimen in combination with: Letrozole (DB01006)••••••••••••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Due to its mechanism of action, palbociclib inhibits cell growth and suppresses DNA replication in retinoblastoma tumor suppressor gene (RB) proficient cancer cells. As expected, these RB cells present a significant increase in the proportion of cells in G1 state and the presence of palbociclib produces effective dephosphorylation of RB, reduce proliferation and induce senescence causing cell-cycle arrest.5

In vitro studies showed the potential for palbociclib to reduce cellular proliferation of estrogen receptor-positive breast cancer cell lines through the inhibition of the cell-cycle progression from G1 to S phase. In this study, it was demonstrated that the sensitivity of the cells significantly increased with the expression of RB1 and CCND1 and low expression of CDKN2A. As well, palbociclib, combined with antiestrogens, enhanced in vivo antitumor activity in estrogen receptor-positive breast cancer mouse models.3

In clinical trials, palbociclib, in combination with letrozole, was shown to significantly increase the progression-free survival (PFS) in patients with metastatic breast cancer without prior endocrine treatment. In the results, the PFS increased from 4.5 to 9.5 months with an overall response rate (ORR) of 24.6%.2

Mechanism of action

Palbociclib is a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor1 that acts by binding to the ATP pocket with an IC50 in the range of 9-15 nmol/L. It is important to consider that it presents low to absent activity against other kinases.4

The CDK4/6 kinase is involved, with coregulatory partner cyclin D, in the G1-S transition. Hence, inhibition of this step prevents cell cycle progression in cells in whose this pathway is functioning. This step includes the pathways of the phosphorylation of retinoblastoma protein and the E2F family of transcription factors.4

TargetActionsOrganism
ACyclin-dependent kinase 4
inhibitor
Humans
ACyclin-dependent kinase 6
inhibitor
Humans
Absorption

Palbociclib presents a linear pharmacokinetic profile and its peak plasma concentration was observed 6-12 hours after oral administration. The oral bioavailability is reported to be of 46% with a steady-state reached after 8 days and a median accumulation ratio of 2.4.3

The absorption of palbociclib is significantly reduced under fasting conditions and hence, food intake is recommended when this drug is administered.3

Volume of distribution

The mean apparent distribution of palbociclib is 2583 L which suggests that palbociclib penetrates extensively into peripheral tissues.11

Protein binding

Binding of palbociclib to human plasma proteins in vitro accounts for approximately 85% of the administered dose.13

Metabolism

Palbociclib is mainly hepatically transformed.3 the metabolism is mainly performed by the activities of the cytochrome P450 isoenzyme 3A and the sulfotransferase 2A1.4 The metabolism of palbociclib is represented mainly by reactions of oxidation and sulfonation followed by acylation and glucuronidation as minor reactions. After its metabolism, palbociclib forms mainly inactive glucuronide and sulfamic acid conjugates. The major circulating metabolite, accounting for 1.5% of the dose in excreta is is the glucuronide conjugate.13

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Route of elimination

The main route of elimination of palbociclib is through feces after hepatic metabolism while renal clearance seems to play a minor role accounting only for 17.5% of the eliminated dose.3

Half-life

The mean plasma elimination half-life of palbociclib is 29 hours.3

Clearance

The mean apparent oral clearance of palbociclib is of 63.1 L/h.3

Adverse Effects
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Toxicity

The reported oral Ld50 is of 100 mg/kg.MSDS In cases of overdosage, only supportive measures are considered.Label

Palbociclib was showed to present clastogenic activities in in vitro and in vivo assays. As well, it has been reported to produce fetal harm due to its mechanism of action.3 Lastly, it was shown to increase the incidence of microglial cell tumors in the central nervous system at high doses.Label

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Palbociclib can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Palbociclib can be increased when combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Palbociclib.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Palbociclib.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Palbociclib.
Food Interactions
  • Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of palbociclib, which may increase its serum concentration.
  • Avoid St. John's Wort. This herb induces the CYP3A metabolism of palbociclib and may reduce its serum concentration.
  • Take at the same time every day. This applies to both palbociclib capsules and tablets.
  • Take with food. Palbociclib capsules should be taken with food. Some subjects have reduced bioavailability of palbociclib when in a fasted state, therefore taking with food makes the bioavailability more consistent.
  • Take with or without food. Palbociclib tablets may be taken with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Palbociclib isethionateW1NYL2IRDR827022-33-3LYYVFHRFIJKPOV-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IbranceCapsule100 mg/1OralPfizer Laboratories Div Pfizer Inc2015-02-03Not applicableUS flag
IbranceCapsule75 mgOralPfizer Europe Ma Eeig2020-12-15Not applicableEU flag
IbranceTablet, film coated100 mgOralPfizer Europe Ma Eeig2020-12-15Not applicableEU flag
IbranceTablet75 mgOralPfizer Canada Ulc2020-09-21Not applicableCanada flag
IbranceCapsule125 mgOralPfizer Europe Ma Eeig2020-12-15Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
REAMPLA®Palbociclib (75 mg) + Palbociclib (100 mg) + Palbociclib (125 mg)Capsule, coatedOralPFIZER MANUFACTURING DEUTSCHLAND GMBH2018-10-24Not applicableColombia flag
REAMPLA®Palbociclib (75 mg) + Palbociclib (100 mg) + Palbociclib (125 mg)Capsule, coatedOralPFIZER MANUFACTURING DEUTSCHLAND GMBH2018-10-24Not applicableColombia flag
REAMPLA®Palbociclib (75 mg) + Palbociclib (100 mg) + Palbociclib (125 mg)Capsule, coatedOralPFIZER MANUFACTURING DEUTSCHLAND GMBH2018-10-24Not applicableColombia flag

Categories

ATC Codes
L01EF01 — Palbociclib
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pyridinylpiperazines. These are compounds containing a pyridinylpiperazine skeleton, which consists of a pyridine linked (not fused) to a piperazine by a bond by a single bond that is not part of a ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Pyridinylpiperazines
Alternative Parents
N-arylpiperazines / Pyrido[2,3-d]pyrimidines / Aryl alkyl ketones / Dialkylarylamines / Pyridinones / Aminopyridines and derivatives / Aminopyrimidines and derivatives / Methylpyridines / Imidolactams / Vinylogous amides
show 7 more
Substituents
Amine / Aminopyridine / Aminopyrimidine / Aromatic heteropolycyclic compound / Aryl alkyl ketone / Aryl ketone / Azacycle / Dialkylarylamine / Heteroaromatic compound / Hydrocarbon derivative
show 22 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
piperidines, tertiary amino compound, secondary amino compound, ring assembly, aromatic ketone, cyclopentanes, pyridopyrimidine, aminopyridine (CHEBI:85993)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
G9ZF61LE7G
CAS number
571190-30-2
InChI Key
AHJRHEGDXFFMBM-UHFFFAOYSA-N
InChI
InChI=1S/C24H29N7O2/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29)
IUPAC Name
6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one
SMILES
CC(=O)C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N3CCNCC3)N=C2N(C2CCCC2)C1=O

References

General References
  1. Wilson FR, Varu A, Mitra D, Cameron C, Iyer S: Systematic review and network meta-analysis comparing palbociclib with chemotherapy agents for the treatment of postmenopausal women with HR-positive and HER2-negative advanced/metastatic breast cancer. Breast Cancer Res Treat. 2017 Nov;166(1):167-177. doi: 10.1007/s10549-017-4404-4. Epub 2017 Jul 27. [Article]
  2. Nathan MR, Schmid P: A Review of Fulvestrant in Breast Cancer. Oncol Ther. 2017;5(1):17-29. doi: 10.1007/s40487-017-0046-2. Epub 2017 May 8. [Article]
  3. Beaver JA, Amiri-Kordestani L, Charlab R, Chen W, Palmby T, Tilley A, Zirkelbach JF, Yu J, Liu Q, Zhao L, Crich J, Chen XH, Hughes M, Bloomquist E, Tang S, Sridhara R, Kluetz PG, Kim G, Ibrahim A, Pazdur R, Cortazar P: FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer. Clin Cancer Res. 2015 Nov 1;21(21):4760-6. doi: 10.1158/1078-0432.CCR-15-1185. Epub 2015 Aug 31. [Article]
  4. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]
  5. Cadoo KA, Gucalp A, Traina TA: Palbociclib: an evidence-based review of its potential in the treatment of breast cancer. Breast Cancer (Dove Med Press). 2014 Aug 4;6:123-33. doi: 10.2147/BCTT.S46725. eCollection 2014. [Article]
  6. Schmidt M: Palbociclib - from Bench to Bedside and Beyond. Breast Care (Basel). 2016 Jun;11(3):177-81. doi: 10.1159/000447001. Epub 2016 Jun 22. [Article]
  7. FDA Approved Drug Products: Apadaz (benzhydrocodone and acetaminophen) tablets [Link]
  8. Pfizer history [Link]
  9. Canadian cancer society [Link]
  10. Canadian cancer society [Link]
  11. Clinical trials [Link]
  12. FDA Approved Drug Products: Ibrance (palbociclib) capsules for oral administration [Link]
  13. IBRANCE (palbociclib) BC Cancer monograph [File]
Human Metabolome Database
HMDB0256084
KEGG Drug
D10372
PubChem Compound
5330286
PubChem Substance
310265004
ChemSpider
4487437
BindingDB
6309
RxNav
1601374
ChEBI
85993
ChEMBL
CHEMBL189963
ZINC
ZINC000003938686
PharmGKB
PA166153469
PDBe Ligand
LQQ
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Palbociclib
PDB Entries
2euf / 5l2i / 7n7o
FDA label
Download (694 KB)
MSDS
Download (266 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentBreast Cancer1
4Not Yet RecruitingTreatmentBreast Cancer1
4Not Yet RecruitingTreatmentBreast Carcinoma / Endometrium Carcinoma / Ovarian Carcinoma / Renal Cell Carcinoma (RCC) / Thyroid Carcinoma1
4RecruitingTreatmentMetastatic Breast Cancer1
4TerminatedTreatmentBreast Neoplasms1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral
CapsuleOral100 mg/1
CapsuleOral125 mg/1
CapsuleOral75 mg/1
TabletOral100 mg
TabletOral125 mg
TabletOral75 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral100 MG
Tablet, film coatedOral125 mg/1
Tablet, film coatedOral125 MG
Tablet, film coatedOral75 mg/1
Tablet, film coatedOral75 MG
CapsuleOral100.000 mg
CapsuleOral125.000 mg
CapsuleOral75.000 mg
TabletOral75.000 mg
Capsule, coatedOral
Tablet, coatedOral75 mg
CapsuleOral100 mg
CapsuleOral125 mg
CapsuleOral75 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US7456168No2008-11-252023-01-16US flag
US6936612No2005-08-302023-01-22US flag
US7208489No2007-04-242023-01-16US flag
USRE47739No2019-11-262023-01-16US flag
US10723730No2020-07-282034-02-08US flag
US11065250No2021-07-202036-05-24US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)263-266 ºC'MSDS'
boiling point (°C)711.5 ºC'MSDS'
water solubility10 mg/ml (isethionate form)'MSDS'
logP0.99IBRANCE (palbociclib) monograph
pKa7.4 (the secondary piperazine nitrogen) and 3.9 (the pyridine nitrogen)'FDA Label'
Predicted Properties
PropertyValueSource
Water Solubility0.0174 mg/mLALOGPS
logP2.12ALOGPS
logP2.77Chemaxon
logS-4.4ALOGPS
pKa (Strongest Acidic)11.34Chemaxon
pKa (Strongest Basic)8.86Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count8Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area103.35 Å2Chemaxon
Rotatable Bond Count5Chemaxon
Refractivity127.47 m3·mol-1Chemaxon
Polarizability49.69 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0000900000-1234aab98298dbd089a1
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0002-0000900000-ab5bf19f882bd9fd9577
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0532-0000900000-a563ca7ebf6635ac68ab
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0002-0000900000-6f1a6b0f234ffc851d58
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0103-0006900000-3a7cdd2ba77e0c7c0165
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0571-0348900000-9b38623e3c6a0fe387f1
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-205.08873
predicted
DeepCCS 1.0 (2019)
[M+H]+207.44673
predicted
DeepCCS 1.0 (2019)
[M+Na]+214.14618
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Cyclin-dependent protein serine/threonine kinase regulator activity
Specific Function
Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S tra...
Gene Name
CDK4
Uniprot ID
P11802
Uniprot Name
Cyclin-dependent kinase 4
Molecular Weight
33729.55 Da
References
  1. Fry DW, Harvey PJ, Keller PR, Elliott WL, Meade M, Trachet E, Albassam M, Zheng X, Leopold WR, Pryer NK, Toogood PL: Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Article]
  2. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Cyclin-dependent protein serine/threonine kinase activity
Specific Function
Serine/threonine-protein kinase involved in the control of the cell cycle and differentiation; promotes G1/S transition. Phosphorylates pRB/RB1 and NPM1. Interacts with D-type G1 cyclins during int...
Gene Name
CDK6
Uniprot ID
Q00534
Uniprot Name
Cyclin-dependent kinase 6
Molecular Weight
36938.025 Da
References
  1. Fry DW, Harvey PJ, Keller PR, Elliott WL, Meade M, Trachet E, Albassam M, Zheng X, Leopold WR, Pryer NK, Toogood PL: Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Article]
  2. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands.
Gene Name
SULT2A1
Uniprot ID
Q06520
Uniprot Name
Bile salt sulfotransferase
Molecular Weight
33779.57 Da
References
  1. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. IBRANCE (palbociclib) BC Cancer monograph [File]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]
  2. IBRANCE (palbociclib) FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21. [Article]
  2. IBRANCE (palbociclib) FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. IBRANCE (palbociclib) FDA label [File]

Drug created at May 14, 2015 20:03 / Updated at December 05, 2023 12:31