Identification

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Name
Palbociclib
Accession Number
DB09073
Type
Small Molecule
Groups
Approved, Investigational
Description

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

Structure
Thumb
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
Product Ingredients
IngredientUNIICASInChI Key
Palbociclib isethionateW1NYL2IRDR827022-33-3LYYVFHRFIJKPOV-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
IbranceCapsule100 mg/1OralU.S. Pharmaceuticals2017-05-08Not applicableUs
IbranceCapsule125 mg/1OralU.S. Pharmaceuticals2015-02-03Not applicableUs
IbranceCapsule125 mg/1OralPfizer Laboratories Div Pfizer Inc2015-02-03Not applicableUs
IbranceCapsule125 mgOralPfizer2016-04-19Not applicableCanada
IbranceCapsule100 mg/1OralPfizer Laboratories Div Pfizer Inc2015-02-03Not applicableUs
IbranceCapsule100 mgOralPfizer2016-04-19Not applicableCanada
IbranceCapsule75 mg/1OralU.S. Pharmaceuticals2017-05-08Not applicableUs
IbranceCapsule75 mg/1OralPfizer Laboratories Div Pfizer Inc2015-02-03Not applicableUs
IbranceCapsule75 mgOralPfizer2016-04-20Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
G9ZF61LE7G
CAS number
571190-30-2
Weight
Average: 447.5328
Monoisotopic: 447.238273207
Chemical Formula
C24H29N7O2
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

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.Label

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

Associated Conditions
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
Additional Data Available
Adverse Effects

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Contraindications

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Blackbox Warnings

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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.12

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.12

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

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

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe serum concentration of (R)-warfarin can be increased when it is combined with Palbociclib.
(S)-WarfarinThe serum concentration of (S)-Warfarin can be increased when it is combined with Palbociclib.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Palbociclib.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Palbociclib.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Palbociclib.
5-androstenedioneThe metabolism of Palbociclib can be decreased when combined with 5-androstenedione.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Palbociclib.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Palbociclib is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Palbociclib.
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Palbociclib.
Additional Data Available
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    Severity

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  • Evidence Level
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  • Action
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Food Interactions
Not Available

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. [PubMed:28752187]
  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. [PubMed:28680952]
  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. [PubMed:26324739]
  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. [PubMed:28203301]
  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. [PubMed:25177151]
  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. [PubMed:27493617]
  7. FDA approvals [Link]
  8. Pfizer history [Link]
  9. Canadian cancer society [Link]
  10. Canadian cancer society [Link]
  11. Clinical trials [Link]
  12. IBRANCE (palbociclib) BC Cancer monograph [File]
External Links
KEGG Drug
D10372
PubChem Compound
5330286
PubChem Substance
310265004
ChemSpider
4487437
BindingDB
6309
ChEBI
85993
ChEMBL
CHEMBL189963
PharmGKB
PA166153469
HET
LQQ
Wikipedia
Palbociclib
ATC Codes
L01XE33 — Palbociclib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
2euf / 5l2i
FDA label
Download (694 KB)
MSDS
Download (266 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingOtherAdvanced Breast Cancer1
1Active Not RecruitingTreatmentAdvanced Solid Tumor Malignancies1
1Active Not RecruitingTreatmentAdvanced and Metastatic Breast Cancer1
1Active Not RecruitingTreatmentCCND1 Positive / Recurrent Mantle Cell Lymphoma / T(11;14)1
1Active Not RecruitingTreatmentCancer, Breast1
1Active Not RecruitingTreatmentMantle Cell Lymphoma (MCL)1
1CompletedBasic ScienceHealthy Volunteers11
1CompletedBasic ScienceHealthy, Hepatic Insufficiency1
1CompletedBasic ScienceImpaired Renal Function1
1CompletedTreatmentMalignancies1
1CompletedTreatmentMantle Cell Lymphoma (MCL)1
1CompletedTreatmentMetastatic Pancreatic Ductal Adenocarcinoma1
1CompletedTreatmentNeoplasms / Non-Hodgkin's Lymphoma (NHL)1
1Not Yet RecruitingTreatmentAcute Myelogenous Leukaemia (AML) / Cancer, Breast / Malignant Neoplasm of Pancreas / Prostate Cancer1
1Not Yet RecruitingTreatmentAdvanced Breast Cancer / BRCA1 Mutations / BRCA2 Mutation / Locally Advanced Breast Cancer (LABC) / Metastatic Breast Cancer (MBC)1
1Not Yet RecruitingTreatmentBreast Neoplasm Female1
1Not Yet RecruitingTreatmentCancer, Breast1
1RecruitingTreatmentAcute Lymphoblastic Leukaemia Recurrent / Acute Lymphoblastic Leukaemias (ALL) / Acute, recurrent Myeloid Leukemia / Hematopoietic/Lymphoid Cancer / Leukemia Acute Myeloid Leukemia (AML) / Refractory Acute Lymphoblastic Leukemia / Refractory Acute Myeloid Leukemia1
1RecruitingTreatmentAcute Lymphoblastic Leukemia With Failed Remission / Acute Lymphoblastic Leukemia, in Relapse1
1RecruitingTreatmentAdvanced Breast Cancer1
1RecruitingTreatmentAdvanced Solid Tumours / Cancer, Breast1
1RecruitingTreatmentBladder Cancers / Cancer of the Ovary / Cancer of Unknown Primary / Colorectal Cancers / Head and Neck Carcinoma / Sarcomas / Solid Neoplasms / Stage III Pancreatic Cancer / Stage IIIA Breast Cancer / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIB Breast Cancer / Stage IIIb Non-small Cell Lung Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer / Stage IV Non-Small Cell Lung Cancer / Stage IVA Pancreatic Cancer / Stage IVB Pancreatic Cancer1
1RecruitingTreatmentCancer, Breast5
1RecruitingTreatmentCancer, Breast / Tumors, Solid1
1RecruitingTreatmentCastration Resistant Prostate Cancer (CRPC) / Hormone Receptor Positive Advanced Breast Cancer / Human Epidermal Receptor 2 Negative Advanced Breast Cancer / Metastatic Breast Cancer (MBC)1
1RecruitingTreatmentEwing's Sarcoma (ES) / Medulloblastomas / Neuroblastomas / Rhabdoid Tumors / Rhabdomyosarcomas / Tumors, Solid1
1RecruitingTreatmentHead & Neck Cancer / Lung Cancer Squamous Cell / Malignant Neoplasm of Pancreas / Tumors, Solid1
1RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
1RecruitingTreatmentHormone Receptor Positive Breast Cancer / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast / Metastatic Breast Cancer (MBC)1
1RecruitingTreatmentLeukemia, Acute / Leukemia, Lymphocytic / Leukemia, T-Cell / Lymphoma, Lymphoblastic / Recurrent Disease / T-Cell Lymphomas1
1RecruitingTreatmentMalignant Neoplasm of Breast / Malignant Neoplasms of Digestive Organs / Malignant Neoplasms of Female Genital Organs / Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites / Malignant Neoplasms of Independent (Primary) Multiple Sites / Malignant Neoplasms of Lip Oral Cavity and Pharynx / Malignant Neoplasms of Mesothelial and Soft Tissue / Malignant Neoplasms of Respiratory and Intrathoracic Organs / Malignant Neoplasms of Thyroid and Other Endocrine Glands / Malignant Neoplasms of Urinary Tract / Neoplasms of Uncertain or Unknown Behavior1
1RecruitingTreatmentMalignant Neoplasm of Pancreas / Tumors, Solid1
1RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1RecruitingTreatmentRecurrent B Acute Lymphoblastic Leukemia / Refractory B Acute Lymphoblastic Leukemia1
1TerminatedTreatmentChildhood Choroid Plexus Tumor / Childhood Ependymoblastoma / Childhood Grade III Meningioma / Childhood High-grade Cerebellar Astrocytoma / Childhood High-grade Cerebral Astrocytoma / Childhood Medulloepithelioma / Recurrent Childhood Anaplastic Astrocytoma / Recurrent Childhood Anaplastic Oligoastrocytoma / Recurrent Childhood Anaplastic Oligodendroglioma / Recurrent Childhood Brain Stem Glioma / Recurrent Childhood Cerebellar Astrocytoma / Recurrent Childhood Cerebral Astrocytoma / Recurrent Childhood Giant Cell Glioblastoma / Recurrent Childhood Glioblastoma / Recurrent Childhood Gliomatosis Cerebri / Recurrent Childhood Gliosarcoma / Recurrent Childhood Medulloblastoma / Recurrent Childhood Pineoblastoma / Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor1
1TerminatedTreatmentAcute, relapsed Leukemia / High-Risk Myelodysplasia / Refractory Acute Leukemia1
1TerminatedTreatmentMultiple Myeloma (MM)1
1, 2Active Not RecruitingTreatmentBreast Cancer Metastatic / Metastatic Invasive Breast Cancer / Unresectable Locally Advanced Invasive Breast Cancer1
1, 2Active Not RecruitingTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentKRAS Mutant Non-Small Cell Lung Cancer / Tumors, Solid1
1, 2Not Yet RecruitingTreatmentCRC / KRAS Gene Mutation / Lung Cancer Non-Small Cell Cancer (NSCLC) / Tumors, Solid1
1, 2Not Yet RecruitingTreatmentHead and Neck Carcinoma / Locally Advanced / Unresectable1
1, 2Not Yet RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Leukemia Acute Myeloid Leukemia (AML)1
1, 2RecruitingTreatmentAnatomic Stage I Breast Cancer AJCC v8 / Anatomic Stage IA Breast Cancer AJCC v8 / Anatomic Stage IB Breast Cancer AJCC v8 / Anatomic Stage II Breast Cancer AJCC v8 / Anatomic Stage IIA Breast Cancer AJCC v8 / Anatomic Stage IIB Breast Cancer AJCC v8 / Anatomic Stage III Breast Cancer AJCC v8 / Anatomic Stage IIIA Breast Cancer AJCC v8 / Anatomic Stage IIIB Breast Cancer AJCC v8 / Anatomic Stage IIIC Breast Cancer AJCC v8 / Anatomic Stage IV Breast Cancer AJCC v8 / Estrogen Receptor Positive / HER2/Neu Negative / MKI67 Positive / One to five years postmenopausal / Prognostic Stage I Breast Cancer AJCC v8 / Prognostic Stage IA Breast Cancer AJCC v8 / Prognostic Stage IB Breast Cancer AJCC v8 / Prognostic Stage IIA Breast Cancer AJCC v8 / Prognostic Stage IIB Breast Cancer AJCC v8 / Prognostic Stage III Breast Cancer AJCC v8 / Prognostic Stage IIIA Breast Cancer AJCC v8 / Prognostic Stage IIIB Breast Cancer AJCC v8 / Prognostic Stage IIIC Breast Cancer AJCC v8 / Prognostic Stage IV Breast Cancer AJCC v81
1, 2RecruitingTreatmentBreast Cancer Metastatic / Her2-Positive Breast Cancer1
1, 2RecruitingTreatmentBreast Diseases / Neoplasms, Breast1
1, 2RecruitingTreatmentCDNKN2A Loss Defined / Melanoma BRAF V600E/K Mutated1
1, 2RecruitingTreatmentCancer, Breast2
1, 2RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck1
1, 2RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Negative / Invasive Breast Carcinoma / Multifocal Breast Carcinoma / One to five years postmenopausal / Progesterone Receptor Positive / Stage I Breast Carcinoma / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage II Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage III Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1, 2RecruitingTreatmentGlioblastoma, Adult1
1, 2RecruitingTreatmentHormone Receptor (HR)-Positive Breast Cancer / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
1, 2RecruitingTreatmentLung Cancers1
1, 2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1, 2RecruitingTreatmentMetastatic Non-Small Cell Lung Cancer / Non-Small Cell Lung Cancer Stage IIIB1
2Active Not RecruitingBasic ScienceCancer, Breast1
2Active Not RecruitingOtherNeoplasms, Breast1
2Active Not RecruitingTreatmentAdvanced Gastrointestinal Stromal Tumors1
2Active Not RecruitingTreatmentAdvanced Hepatocellular Carcinoma / HCC / Liver Cancer1
2Active Not RecruitingTreatmentBreast Carcinoma Metastatic in the Brain / Estrogen Receptor Negative / HER2/Neu Negative / HER2/Neu Positive / Progesterone Receptor Negative / Recurrent Breast Carcinoma / Stage IV Breast Cancer / Triple-Negative Breast Carcinoma1
2Active Not RecruitingTreatmentCancer, Breast3
2Active Not RecruitingTreatmentCancer, Breast / Carcinoma, Breast / Tumors, Breast1
2Active Not RecruitingTreatmentCancer, Breast / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
2Active Not RecruitingTreatmentHormone Receptor Positive / Metastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentMalignant Neoplasm of Female Breast1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)3
2Active Not RecruitingTreatmentNeoadjuvant Operable Breast Cancer1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingTreatmentOvarian Epithelial Carcinoma1
2Active Not RecruitingTreatmentProstate Cancer1
2Active Not RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)2
2CompletedTreatmentCancer, Breast2
2CompletedTreatmentLiposarcoma / Sarcomas1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentMultiple Myeloma (MM)1
2CompletedTreatmentNeoplasms / Neoplasms, Breast1
2CompletedTreatmentPancreatic Neuroendocrine Cancer1
2CompletedTreatmentUntreated Operable Early Breast Cancer1
2Not Yet RecruitingTreatmentCancer of the Ovary1
2Not Yet RecruitingTreatmentCancer, Breast / HR+/HER2-negative Breast Cancer / Metastasis1
2Not Yet RecruitingTreatmentKRAS Gene Mutation / Metastatic Colorectal Carcinoma / NRAS Gene Mutation / Stage III Colorectal Cancer AJCC v8 / Stage IIIA Colorectal Neuroendocrine Tumor AJCC v8 / Stage IIIB Colorectal Cancer AJCC v8 / Stage IIIC Colorectal Cancer AJCC v8 / Stage IV Colorectal Cancer AJCC v8 / Stage IVA Colorectal Cancer AJCC v8 / Stage IVB Colorectal Cancer AJCC v8 / Stage IVC Colorectal Cancer AJCC v8 / Unresectable Carcinoma1
2Not Yet RecruitingTreatmentMelanoma1
2Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Not Yet RecruitingTreatmentThymic Cancer1
2RecruitingScreeningAdvanced Malignant Solid Neoplasm / Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma / Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma / Childhood Langerhans Cell Histiocytosis / Histiocytic Sarcoma (HS) / Juvenile Xanthogranuloma / Langerhans Cell Histiocytosis (LCH) / Malignant Gliomas / Malignant Lymphomas / Recurrent Central Nervous System Neoplasm / Recurrent Childhood Ependymoma / Recurrent Childhood Malignant Germ Cell Tumor / Recurrent Childhood Medulloblastoma / Recurrent Childhood Non-Hodgkin Lymphoma / Recurrent Childhood Rhabdomyosarcoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma / Recurrent Gliomas / Recurrent Hepatoblastoma / Recurrent Langerhans Cell Histiocytosis / Recurrent Malignant Solid Neoplasm / Recurrent Neuroblastoma / Recurrent Osteosarcoma / Recurrent Peripheral Primitive Neuroectodermal Tumor / Recurrent Rhabdoid Tumor / Refractory Central Nervous System Neoplasm / Refractory Childhood Malignant Germ Cell Tumor / Refractory Ewing Sarcoma / Refractory Glioma / Refractory Hepatoblastoma / Refractory Langerhans cell histiocytosis / Refractory Malignant Solid Neoplasm / Refractory Medulloblastoma / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Refractory Osteosarcoma / Refractory Peripheral Primitive Neuroectodermal Tumor / Refractory Rhabdoid Tumor / Refractory Rhabdomyosarcoma / Rhabdoid Tumors / Stage III Childhood Non-Hodgkin Lymphoma / Stage III Osteosarcoma / Stage III Osteosarcoma AJCC v7 / Stage III Soft Tissue Sarcoma / Stage III Soft Tissue Sarcoma AJCC v7 / Stage IV Childhood Non-Hodgkin Lymphoma / Stage IV Osteosarcoma / Stage IV Osteosarcoma AJCC v7 / Stage IV Soft Tissue Sarcoma / Stage IV Soft Tissue Sarcoma AJCC v7 / Stage IVA Osteosarcoma / Stage IVA Osteosarcoma AJCC v7 / Stage IVB Osteosarcoma / Stage IVB Osteosarcoma AJCC v7 / Wilms' tumor1
2RecruitingTreatmentAdenocarcinoma of the Colon / Adenocarcinoma of the Rectum / Adult Central Nervous System Germ Cell Tumor / Adult Solid Tumor / Adult Teratoma / Benign Teratoma / Estrogen Receptor-negative Breast Cancer / Estrogen Receptor-Positive Breast Cancer / Familial Testicular Germ Cell Tumor / HER2-Negative Breast Cancer / Her2-Positive Breast Cancer / Male Breast Cancer / Metastatic Colon Cancer / Ovarian Immature Teratoma / Ovarian Mature Teratoma / Ovarian Monodermal and Highly Specialized Teratoma / Progesterone Receptor-negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Recurrent Breast Cancer / Recurrent Colon Cancer / Recurrent Extragonadal Germ Cell Tumor / Recurrent Extragonadal Non-seminomatous Germ Cell Tumor / Recurrent Extragonadal Seminoma / Recurrent Malignant Testicular Germ Cell Tumor / Recurrent Melanoma / Recurrent Ovarian Germ Cell Tumor / Recurrent Rectal Cancer / Stage III Extragonadal Non-seminomatous Germ Cell Tumor / Stage III Extragonadal Seminoma / Stage III Malignant Testicular Germ Cell Tumor / Stage III Ovarian Germ Cell Tumor / Stage IV Breast Cancer / Stage IV Extragonadal Non-Seminomatous Germ Cell Tumor / Stage IV Extragonadal Seminoma / Stage IV Melanoma / Stage IV Ovarian Germ Cell Tumor / Stage IV Rectal Cancer / Testicular Immature Teratoma / Testicular Mature Teratoma1
2RecruitingTreatmentAdenocarcinomas / Lung Cancer Non-Small Cell Cancer (NSCLC) / Squamous Cell Carcinoma (SCC)1
2RecruitingTreatmentAdvanced Breast Cancer / Cancer, Breast / Hormone Receptor Positive Tumor / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentAdvanced Malignant Solid Neoplasm / RB1 Positive / Recurrent Childhood Ependymoma / Recurrent Ewing Sarcoma / Recurrent Gliomas / Recurrent Hepatoblastoma / Recurrent Kidney Wilms Tumor / Recurrent Langerhans Cell Histiocytosis / Recurrent Malignant Germ Cell Tumor / Recurrent Malignant Gliomas / Recurrent Medulloblastoma / Recurrent Neuroblastoma / Recurrent Non-Hodgkin Lymphoma / Recurrent Osteosarcoma / Recurrent Peripheral Primitive Neuroectodermal Tumor / Recurrent Rhabdoid Tumor / Recurrent Rhabdomyosarcoma / Recurrent Soft Tissue Sarcoma / Refractory Ependymoma / Refractory Ewing Sarcoma / Refractory Glioma / Refractory Hepatoblastoma / Refractory Langerhans cell histiocytosis / Refractory Malignant Germ Cell Tumor / Refractory Malignant Glioma / Refractory Medulloblastoma / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Refractory Osteosarcoma / Refractory Peripheral Primitive Neuroectodermal Tumor / Refractory Rhabdoid Tumor / Refractory Rhabdomyosarcoma / Refractory Soft Tissue Sarcoma1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)2
2RecruitingTreatmentAnatomic Stage IV Breast Cancer AJCC v8 / Estrogen Receptor Positive / HER2/Neu Negative / Metastatic Breast Carcinoma / Metastatic Malignant Neoplasm in the Bone / Progesterone Receptor Positive / Prognostic Stage IV Breast Cancer AJCC v81
2RecruitingTreatmentBreast Cancer Metastatic1
2RecruitingTreatmentBreast Cancer Stage II / Breast Cancer Stage III1
2RecruitingTreatmentBreast Cancer Stage / Cancer, Breast / HER2 Positive Breast Carcinoma / Her2-Positive Breast Cancer / Metastatic Breast Cancer (MBC) / Recurrent Breast Cancer1
2RecruitingTreatmentCancer of the Breast / Cancer, Breast / Carcinoma, Breast1
2RecruitingTreatmentCancer of the Breast / Cancer, Breast / Carcinoma, Breast / Malignant Tumor of Breast1
2RecruitingTreatmentCancer of the Colon / Colon Neoplasms / Malignant Neoplasm of Colon / Neoplasms, Colonic1
2RecruitingTreatmentCancer, Advanced / Sarcomas1
2RecruitingTreatmentCancer, Breast4
2RecruitingTreatmentCancer, Breast / Estrogen Receptor Positive Tumor / Her2-Positive Breast Cancer1
2RecruitingTreatmentCarcinoma, Squamous Cell of Head and Neck1
2RecruitingTreatmentChordomas1
2RecruitingTreatmentDCIS1
2RecruitingTreatmentEarly-Stage Breast Carcinoma / Estrogen Receptor Positive Tumor1
2RecruitingTreatmentEarly-Stage Breast Carcinoma / Hormone Receptor Positive Tumor1
2RecruitingTreatmentEndometrial Cancers1
2RecruitingTreatmentEstrogen Receptor Positive Breast Cancer / Hormone Receptor Positive Malignant Neoplasm of Breast / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast / Metastatic Breast Cancer (MBC) / Progesterone Receptor Positive Tumor1
2RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Negative / One to five years postmenopausal / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
2RecruitingTreatmentEstrogen Receptor and/or Progesterone Receptor Positive / HER2/Neu Negative / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / HER2/Neu Negative / Stage IV Breast Cancer AJCC v6 and v71
2RecruitingTreatmentFemale Breast Carcinoma1
2RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
2RecruitingTreatmentLymphoma, B Cell / Mantle Cell Lymphoma (MCL)1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)5
2RecruitingTreatmentMetastatic Malignant Neoplasm to Brain1
2RecruitingTreatmentNeoplasms, Breast1
2RecruitingTreatmentOligoastrocytoma / Oligodendrogliomas1
2RecruitingTreatmentProstate Cancer1
2RecruitingTreatmentRare Tumor / Refractory Tumors1
2TerminatedTreatmentAnaplastic Astrocytoma (AA) / Glioblastomas / Gliosarcoma1
2TerminatedTreatmentMetastatic Urothelial Carcinoma (UC)1
2WithdrawnTreatmentCancer, Advanced1
2WithdrawnTreatmentEstrogen Receptor Positive / HER2/Neu Negative / Progesterone Receptor Positive / Stage IV Breast Cancer AJCC v6 and v71
2, 3Active Not RecruitingTreatmentCCND1 Gene Amplification / CCND2 Gene Amplification / CCND3 Gene Amplification / CDK4 Gene Amplification / Recurrent Squamous Cell Lung Carcinoma / Stage IV Squamous Cell Lung Carcinoma / Stage IV Squamous Cell Lung Carcinoma AJCC v71
2, 3Active Not RecruitingTreatmentHormone Receptor Positive HER-2 Negative Breast Cancer / HR+ HER2 Negative Breast Cancer1
2, 3RecruitingTreatmentRecurrent Squamous Cell Lung Carcinoma / Stage IV Squamous Cell Lung Carcinoma / Stage IV Squamous Cell Lung Carcinoma AJCC v71
3Active Not RecruitingTreatmentCancer, Breast / CPS-EG Score / Her2-normal / Hormonreceptor Positive / Postneoadjuvant Treatment With CDK 4/6 Inhibitor1
3Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)3
3Active Not RecruitingTreatmentNeoplasms, Breast3
3CompletedTreatmentAdvanced Breast Cancer (Female) / Advanced Breast Cancer Female1
3Not Yet RecruitingHealth Services ResearchSoft Tissue Sarcoma (STS)1
3Not Yet RecruitingTreatmentHormone Receptor Positive Malignant Neoplasm of Breast / Malignant Neoplasm of Female Breast1
3Not Yet RecruitingTreatmentRecurrent Breast Cancer1
3RecruitingTreatmentBreast Neoplasm Female1
3RecruitingTreatmentCancer, Breast1
3RecruitingTreatmentEstrogen Receptor Positive Breast Cancer / HER-2 Positive Breast Cancer1
4Active Not RecruitingTreatmentCancer, Breast1
4RecruitingTreatmentNeoplasms, Breast1
Not AvailableCompletedNot AvailableAdvanced Breast Cancer / Estrogen Receptor-Positive Breast Cancer / Human Epidermal Growth Factor 2 Negative Carcinoma of Breast / Metastatic Breast Cancer (MBC)1
Not AvailableNo Longer AvailableNot AvailableAdvanced Breast Cancer (Female)1
Not AvailableNot Yet RecruitingNot AvailableHR+/HER2- Locally Advanced, Metastatic Breast Cancer1
Not AvailableNot Yet RecruitingTreatmentBreast Cancer Metastatic / General Surgery / Radiotherapy1
Not AvailableNot Yet RecruitingTreatmentBreast Diseases / Cancer, Breast / Neoplasms, Breast1
Not AvailableRecruitingNot AvailableMalignant Neoplasm of Breast1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral100 mg/1
CapsuleOral100 mg
CapsuleOral125 mg
CapsuleOral125 mg/1
CapsuleOral75 mg
CapsuleOral75 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7456168No2008-11-252023-01-16Us
US6936612No2005-08-302023-01-22Us
US7208489No2007-04-242023-01-16Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

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/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

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
N-arylpiperazine / Pyridinylpiperazine / Pyridopyrimidine / Pyrido[2,3-d]pyrimidine / Tertiary aliphatic/aromatic amine / Aryl ketone / Aryl alkyl ketone / Dialkylarylamine / Aminopyrimidine / Aminopyridine
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)

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
  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. [PubMed:15542782]
  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. [PubMed:28203301]
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. [PubMed:15542782]
  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. [PubMed:28203301]

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. [PubMed:28203301]
2. Sulfotransferase 2A1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. [PubMed:28203301]

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. [PubMed:28203301]
  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. [PubMed:28203301]
  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 on May 14, 2015 14:03 / Updated on June 24, 2019 13:09