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
Structure for Palbociclib (DB09073)
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Advanced breast cancer Regimen in combination with: Fulvestrant (DB00947) •••••••••••• ••••• ••••••••• •••••••• ••••••••••••••• ••••••• Used in combination to treat Metastatic breast cancer Regimen in combination with: Fulvestrant (DB00947) •••••••••••• ••••• ••••••••• •••••••• ••••••••••••••• ••••••• Used in combination to treat Refractory, advanced breast cancer Regimen in combination with: Letrozole (DB01006) •••••••••••• ••••••••••••••• ••••••• Used in combination to treat Refractory, metastatic breast cancer Regimen in combination with: Letrozole (DB01006) •••••••••••• ••••••••••••••• ••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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
Target Actions Organism ACyclin-dependent kinase 4 inhibitorHumans ACyclin-dependent kinase 6 inhibitorHumans - 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
Hover over products below to view reaction partners
- 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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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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Palbociclib can be increased when it is combined with Abametapir. Abatacept The metabolism of Palbociclib can be increased when combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Palbociclib. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Palbociclib. Acalabrutinib The 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Palbociclib isethionate W1NYL2IRDR 827022-33-3 LYYVFHRFIJKPOV-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ibrance Capsule 100 mg/1 Oral U.S. Pharmaceuticals 2017-05-08 Not applicable US 
Ibrance Tablet, film coated 75 mg Oral Pfizer Europe Ma Eeig 2020-12-15 Not applicable EU 
Ibrance Capsule 100 mg Oral Pfizer Europe Ma Eeig 2020-12-15 Not applicable EU Ibrance Capsule 100 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 2015-02-03 Not applicable US Ibrance Capsule 100 mg Oral Pfizer Europe Ma Eeig 2020-12-15 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image REAMPLA® Palbociclib (75 mg) + Palbociclib (100 mg) + Palbociclib (125 mg) Capsule, coated Oral PFIZER MANUFACTURING DEUTSCHLAND GMBH 2018-10-24 Not applicable Colombia 
REAMPLA® Palbociclib (75 mg) + Palbociclib (100 mg) + Palbociclib (125 mg) Capsule, coated Oral PFIZER MANUFACTURING DEUTSCHLAND GMBH 2018-10-24 Not applicable Colombia REAMPLA® Palbociclib (75 mg) + Palbociclib (100 mg) + Palbociclib (125 mg) Capsule, coated Oral PFIZER MANUFACTURING DEUTSCHLAND GMBH 2018-10-24 Not applicable Colombia
Categories
- ATC Codes
- L01EF01 — Palbociclib
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cyclin-dependent kinase (CDK) inhibitors
- Cyclin-Dependent Kinases, antagonists & inhibitors
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Immunosuppressive Agents
- Kinase Inhibitor
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- OCT1 inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Protein Kinase Inhibitors
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- FDA Approved Drug Products: Apadaz (benzhydrocodone and acetaminophen) tablets [Link]
- Pfizer history [Link]
- Canadian cancer society [Link]
- Canadian cancer society [Link]
- Clinical trials [Link]
- FDA Approved Drug Products: Ibrance (palbociclib) capsules for oral administration [Link]
- IBRANCE (palbociclib) BC Cancer monograph [File]
- External Links
- Human Metabolome Database
- HMDB0256084
- KEGG Drug
- D10372
- PubChem Compound
- 5330286
- PubChem Substance
- 310265004
- ChemSpider
- 4487437
- BindingDB
- 6309
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Breast Cancer 1 4 Not Yet Recruiting Treatment Breast Cancer 1 4 Not Yet Recruiting Treatment Breast Carcinoma / Endometrium Carcinoma / Ovarian Carcinoma / Renal Cell Carcinoma (RCC) / Thyroid Carcinoma 1 4 Recruiting Treatment Metastatic Breast Cancer 1 4 Terminated Treatment Breast Neoplasms 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral Capsule Oral 100 mg/1 Capsule Oral 125 mg/1 Capsule Oral 75 mg/1 Tablet Oral 100 mg Tablet Oral 125 mg Tablet Oral 75 mg Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 100 MG Tablet, film coated Oral 125 mg/1 Tablet, film coated Oral 125 MG Tablet, film coated Oral 75 mg/1 Tablet, film coated Oral 75 MG Capsule Oral 100.000 mg Capsule Oral 125.000 mg Capsule Oral 75.000 mg Tablet Oral 75.000 mg Capsule, coated Oral Tablet, coated Oral 75 mg Capsule Oral 100 mg Capsule Oral 125 mg Capsule Oral 75 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7456168 No 2008-11-25 2023-01-16 US US6936612 No 2005-08-30 2023-01-22 US US7208489 No 2007-04-24 2023-01-16 US USRE47739 No 2019-11-26 2023-01-16 US US10723730 No 2020-07-28 2034-02-08 US US11065250 No 2021-07-20 2036-05-24 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 263-266 ºC 'MSDS' boiling point (°C) 711.5 ºC 'MSDS' water solubility 10 mg/ml (isethionate form) 'MSDS' logP 0.99 IBRANCE (palbociclib) monograph pKa 7.4 (the secondary piperazine nitrogen) and 3.9 (the pyridine nitrogen) 'FDA Label' - Predicted Properties
Property Value Source Water Solubility 0.0174 mg/mL ALOGPS logP 2.12 ALOGPS logP 2.77 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 11.34 Chemaxon pKa (Strongest Basic) 8.86 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 103.35 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 127.47 m3·mol-1 Chemaxon Polarizability 49.69 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-0000900000-1234aab98298dbd089a1 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0000900000-ab5bf19f882bd9fd9577 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0532-0000900000-a563ca7ebf6635ac68ab Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0000900000-6f1a6b0f234ffc851d58 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0103-0006900000-3a7cdd2ba77e0c7c0165 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0571-0348900000-9b38623e3c6a0fe387f1 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 205.08873 predictedDeepCCS 1.0 (2019) [M+H]+ 207.44673 predictedDeepCCS 1.0 (2019) [M+Na]+ 214.14618 predictedDeepCCS 1.0 (2019)
Targets
- 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
- 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]
- 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
- 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]
- 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
- SubstrateInhibitor
- 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
- 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
- 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
- IBRANCE (palbociclib) BC Cancer monograph [File]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- 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]
- IBRANCE (palbociclib) FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- 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]
- 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
- IBRANCE (palbociclib) FDA label [File]
Drug created at May 14, 2015 20:03 / Updated at December 05, 2023 12:31