Identification

Name
Tazemetostat
Accession Number
DB12887
Description

Tazemetostat is a methyltransferase inhibitor used to treat metastatic or locally advanced epithelioid sarcoma not eligible for complete resection.6 Tazemetostat was first named in literature as EPZ-6438.5

Tazemetaostat was granted FDA approval on 23 January 2020.6

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 572.75
Monoisotopic: 572.336255913
Chemical Formula
C34H44N4O4
Synonyms
  • Tazemetostat
  • Tazémétostat
  • Tazemetostatum
External IDs
  • E 7438
  • EPZ-6438

Pharmacology

Indication

Tazemetostat is indicated to treat adult and pediatric patients 16 years and older with metastatic or locally advanced epithelioid sarcoma that is not eligible for complete resection.6

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Tazemetostat is a methyltransferase inhibitor that prevents hyper-trimethylation of histones and inhibits cancer cell de-differentiation.6 The duration of action is long as it is given twice daily.6 Patients should be counselled regarding the risk of secondary malignancies and embryo-fetal toxicity.6

Mechanism of action

EZH2 is a methyltransferase subunit of the polycomb repressive complex 2 (PRC2) which catalyzes multiple methylations of lysine 27 on histone H3 (H3K27).6 Trimethylation of this lysine inhibits the transcription of genes associated with cell cycle arrest.3,6 PRC2 is antagonized by the switch/sucrose non-fermentable (SWI/SNF) multiprotein complex.3 Abnormal activation of EZH2 or loss of function mutations in SWI/SNF lead to hyper-trimethylation of H3K27.3 Hyper-trimethylation of H3K27 leads to cancer cell de-differentiation,1 a gain of cancer stem cell-like properties.2 De-differentiation can allow for cancer cell proliferation.1,2,3,6

Tazemetostat inhibits EZH2,6 preventing hyper-trimethylation of H3K27 and an uncontrollable cell cycle.3

TargetActionsOrganism
AHistone-lysine N-methyltransferase EZH2
inhibitor
Humans
UHistone-lysine N-methyltransferase EZH1
inhibitor
Humans
Absorption

Tazemetostat 800mg twice daily leads to a Cmax of 829ng/mL, with a Tmax of 1-2 hours , and an AUC of 3340ng*h/mL.4,6 Absorption is not significantly affected by a high fat, high calorie meal.6 Tazemetostat is 33% bioavailable.6

Volume of distribution

Tazemetostat has a volume of distribution of 1230L.6

Protein binding

Tazemetostat is 88% protein bound in plasma.6

Metabolism

Tazemetostat is metabolized by CYP3A4 to an inactive desethyl metabolite and one other inactive metabolite not described.4,6

Hover over products below to view reaction partners

Route of elimination

Tazemetostat is 15% eliminated in urine and 79% eliminated in feces.6

Half-life

Tazemetostat has a terminal elimination half life of 3.1h.4,6

Clearance

Tazemetostat has an apparent total clearance of 274L/h.6

Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Data regarding the presentation and management of tazemetostat overdoses are not readily available.6 The most common adverse reactions associated with tazemetostat are pain, fatigue, nausea, decreased appetite, vomiting, and constipation.6

Affected organisms
  • Humans
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 Tazemetostat can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Tazemetostat can be increased when combined with Abatacept.
AbemaciclibThe excretion of Tazemetostat can be decreased when combined with Abemaciclib.
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Tazemetostat.
AcalabrutinibThe metabolism of Tazemetostat can be decreased when combined with Acalabrutinib.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Tazemetostat.
AcetaminophenThe metabolism of Tazemetostat can be increased when combined with Acetaminophen.
AcetazolamideThe metabolism of Tazemetostat can be decreased when combined with Acetazolamide.
AcyclovirThe excretion of Acyclovir can be decreased when combined with Tazemetostat.
AdalimumabThe metabolism of Tazemetostat can be increased when combined with Adalimumab.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Take with or without food.

Products

Product Ingredients
IngredientUNIICASInChI Key
Tazemetostat hydrobromide6P89T5M0731467052-75-0UQRICAQPWZSJNF-UHFFFAOYSA-N
International/Other Brands
Tazverik
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
TazverikTablet, film coated200 mg/1OralEpizyme, Inc.2020-01-23Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

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

    Learn more
  • Product Code
    Product Code

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

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Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Biphenyls and derivatives
Direct Parent
Biphenyls and derivatives
Alternative Parents
Aminobenzamides / o-Toluamides / Benzamides / Benzoyl derivatives / Benzylamines / Phenylmethylamines / Dialkylarylamines / Aniline and substituted anilines / Aminotoluenes / Pyridinones
show 16 more
Substituents
Amine / Amino acid or derivatives / Aminobenzamide / Aminobenzoic acid or derivatives / Aminotoluene / Aniline or substituted anilines / Aralkylamine / Aromatic heteromonocyclic compound / Azacycle / Benzamide
show 36 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Chemical Identifiers

UNII
Q40W93WPE1
CAS number
1403254-99-8
InChI Key
NSQSAUGJQHDYNO-UHFFFAOYSA-N
InChI
InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)
IUPAC Name
N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methyl-4'-[(morpholin-4-yl)methyl]-[1,1'-biphenyl]-3-carboxamide
SMILES
CCN(C1CCOCC1)C1=C(C)C(=CC(=C1)C1=CC=C(CN2CCOCC2)C=C1)C(=O)NCC1=C(C)C=C(C)NC1=O

References

General References
  1. Fu H, Cheng L, Sa R, Jin Y, Chen L: Combined tazemetostat and MAPKi enhances differentiation of papillary thyroid cancer cells harbouring BRAF(V600E) by synergistically decreasing global trimethylation of H3K27. J Cell Mol Med. 2020 Jan 22. doi: 10.1111/jcmm.15007. [PubMed:31970877]
  2. Friedmann-Morvinski D, Verma IM: Dedifferentiation and reprogramming: origins of cancer stem cells. EMBO Rep. 2014 Mar;15(3):244-53. doi: 10.1002/embr.201338254. Epub 2014 Feb 14. [PubMed:24531722]
  3. Makita S, Tobinai K: Targeting EZH2 with tazemetostat. Lancet Oncol. 2018 May;19(5):586-587. doi: 10.1016/S1470-2045(18)30149-9. Epub 2018 Apr 9. [PubMed:29650364]
  4. Italiano A, Soria JC, Toulmonde M, Michot JM, Lucchesi C, Varga A, Coindre JM, Blakemore SJ, Clawson A, Suttle B, McDonald AA, Woodruff M, Ribich S, Hedrick E, Keilhack H, Thomson B, Owa T, Copeland RA, Ho PTC, Ribrag V: Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study. Lancet Oncol. 2018 May;19(5):649-659. doi: 10.1016/S1470-2045(18)30145-1. Epub 2018 Apr 9. [PubMed:29650362]
  5. Knutson SK, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock RM, Kuntz KW, Yokoi A, Keilhack H: Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21. [PubMed:24563539]
  6. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]
PubChem Compound
66558664
PubChem Substance
347829042
ChemSpider
30208713
BindingDB
172038
RxNav
2274378
ChEMBL
CHEMBL3414621
ZINC
ZINC000100285161
Wikipedia
Tazemetostat

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3RecruitingTreatmentAdvanced Epithelioid Sarcoma / Advanced Soft Tissue Sarcoma1
3RecruitingTreatmentRelapsed/Refractory Follicular Lymphoma1
2Active Not RecruitingTreatmentRelapsed or Refractory B-cell Non-Hodgkin's Lymphoma1
2CompletedTreatmentBAP1 Loss of Function / Mesothelioma1
2RecruitingScreeningAdvanced Malignant Solid Neoplasm / Ann Arbor Stage III Non-Hodgkin Lymphoma / Ann Arbor Stage IV Non-Hodgkin Lymphoma / Ependymoma, Recurrent / Gliomas, Malignant / Histiocytic Sarcoma (HS) / Juvenile Xanthogranuloma / Langerhans Cell Histiocytosis (LCH) / Recurrent Childhood Rhabdomyosarcoma / Recurrent Ewing Sarcoma / Recurrent Gliomas / Recurrent Hepatoblastoma / Recurrent Langerhans Cell Histiocytosis / Recurrent Malignant Germ Cell Tumor / Recurrent Malignant Solid Neoplasm / Recurrent Medulloblastoma / Recurrent Neuroblastoma / Recurrent Non-Hodgkin Lymphoma / Recurrent Osteosarcoma / Recurrent Peripheral Primitive Neuroectodermal Tumor / Recurrent Primary Central Nervous System Neoplasm / Recurrent Rhabdoid Tumor / Recurrent Soft Tissue Sarcoma / Refractory Ewing Sarcoma / Refractory Glioma / Refractory Hepatoblastoma / Refractory Langerhans cell histiocytosis / Refractory Malignant Germ Cell Tumor / Refractory Malignant Solid Neoplasm / Refractory Medulloblastoma / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Refractory Osteosarcoma / Refractory Peripheral Primitive Neuroectodermal Tumor / Refractory Primary Central Nervous System Neoplasm / Refractory Rhabdoid Tumor / Refractory Rhabdomyosarcoma / Rhabdoid Tumors / Stage III Osteosarcoma AJCC v7 / Stage III Soft Tissue Sarcoma AJCC v7 / Stage IV Osteosarcoma AJCC v7 / Stage IV Soft Tissue Sarcoma AJCC v7 / Stage IVA Osteosarcoma AJCC v7 / Stage IVB Osteosarcoma AJCC v7 / Wilms' tumor1
2RecruitingTreatmentAdvanced Solid Tumors / Atypical Teratoid Rhabdoid Tumors (ATRT) / Diffuse Large B-Cell Lymphoma (DLBCL) / Epitheliod Sarcoma / Follicular Lymphoma (FL) / Malignant Rhabdoid Tumors (MRT) / Mesothelioma / Rhabdoid Tumors of the Kidney (RTK) / Synovial Sarcoma1
2RecruitingTreatmentAny Solid Tumor With an EZH2 GOF Mutation / Atypical Teratoid Rhabdoid Tumors (ATRT) / Epithelioid Sarcoma (ES) / INI1-negative Tumors / Malignant Rhabdoid Tumor of Ovary / Malignant Rhabdoid Tumors (MRT) / Poorly Differentiated Chordoma (or Other Chordoma With Sponsor Approval) / Renal Medullary Carcinoma / Rhabdoid Tumors of the Kidney (RTK) / Selected Tumors With Rhabdoid Features / Synovial Sarcoma1
2SuspendedTreatmentAdvanced Malignant Solid Neoplasm / Ann Arbor Stage III Hodgkin Lymphoma / Ann Arbor Stage III Non-Hodgkin Lymphoma / Ann Arbor Stage IV Hodgkin Lymphoma / Ann Arbor Stage IV Non-Hodgkin Lymphoma / Ependymoma, Recurrent / Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Low Grade Glioma (LGG) / Recurrent Ewing Sarcoma / Recurrent Gliomas / Recurrent Hepatoblastoma / Recurrent Hodgkin Lymphoma / Recurrent Langerhans Cell Histiocytosis / Recurrent Malignant Germ Cell Tumor / Recurrent Malignant Gliomas / Recurrent Malignant Solid Neoplasm / Recurrent Medulloblastoma / Recurrent Neuroblastoma / Recurrent Non-Hodgkin Lymphoma / Recurrent Osteosarcoma / Recurrent Peripheral Primitive Neuroectodermal Tumor / Recurrent Primary Central Nervous System Neoplasm / Recurrent Rhabdoid Tumor / Recurrent Rhabdomyosarcoma / Recurrent Soft Tissue Sarcoma / Refractory Hodgkin Lymphoma / Refractory Langerhans cell histiocytosis / Refractory Malignant Germ Cell Tumor / Refractory Malignant Glioma / Refractory Malignant Solid Neoplasm / Refractory Medulloblastoma / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Refractory Osteosarcoma / Refractory Peripheral Primitive Neuroectodermal Tumor / Refractory Rhabdoid Tumor / Refractory Soft Tissue Sarcoma / Rhabdoid Tumors / Stage III Soft Tissue Sarcoma AJCC v7 / Stage IV Soft Tissue Sarcoma AJCC v7 / Wilms' tumor1
2SuspendedTreatmentFIGO Grade 1 Endometrial Endometrioid Adenocarcinoma / FIGO Grade 2 Endometrial Endometrioid Adenocarcinoma / Recurrent Endometrial Endometrioid Adenocarcinoma / Recurrent Ovarian Carcinoma / Recurrent Ovarian Clear Cell Adenocarcinoma / Recurrent Ovarian Endometrioid Adenocarcinoma / Recurrent Uterine Corpus Cancer1
1Active Not RecruitingTreatmentAdvanced Solid Tumors / Diffuse Large B-Cell Lymphoma (DLBCL) / Mantle Cell Lymphoma (MCL) / Marginal Zone Lymphoma (MZL) / Primary Mediastinal Lymphoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral200 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9090562No2015-07-282032-04-13US flag
US8410088No2013-04-022032-04-13US flag
US9394283No2016-07-192033-04-11US flag
US9872862No2018-01-232033-04-11US flag
US9522152No2016-12-202032-04-13US flag
US10369155No2019-08-062035-10-16US flag
US10420775No2019-09-242032-04-13US flag
US9855275No2018-01-022032-04-13US flag
US9549931No2017-01-242032-04-13US flag
US9688665No2017-06-272034-08-22US flag
US10245269No2019-04-022033-04-11US flag
US10155002No2018-12-182032-04-13US flag
US9889138No2018-02-132035-10-16US flag
US8765732No2012-04-132032-04-13US flag
US9334527No2011-09-122031-09-12US flag
US9333217No2011-09-122031-09-12US flag
US8691507No2011-09-122031-09-12US flag
US9175331No2011-09-122031-09-12US flag
US8895245No2011-09-122031-09-12US flag
US9949999No2011-09-122031-09-12US flag
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
logP2.82ChemSpider
Predicted Properties
PropertyValueSource
Water Solubility0.00932 mg/mLALOGPS
logP4.44ALOGPS
logP3.45ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)11.64ChemAxon
pKa (Strongest Basic)7.19ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area83.14 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity171.5 m3·mol-1ChemAxon
Polarizability66.04 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' (H3K9me) and 'Lys-27' (H3K27me) of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Displays a preference for substrates with less methylation, loses activity when progressively more methyl groups are incorporated into H3K27, H3K27me0 > H3K27me1 > H3K27me2 (PubMed:22323599). Compared to EZH1-containing complexes, it is more abundant in embryonic stem cells and plays a major role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation. The PRC2/EED-EZH2 complex may also serve as a recruiting platform for DNA methyltransferases, thereby linking two epigenetic repression systems. Genes repressed by the PRC2/EED-EZH2 complex include HOXC8, HOXA9, MYT1, CDKN2A and retinoic acid target genes. EZH2 can also methylate non-histone proteins such as the transcription factor GATA4 and the nuclear receptor RORA. Regulates the circadian clock via histone methylation at the promoter of the circadian genes. Essential for the CRY1/2-mediated repression of the transcriptional activation of PER1/2 by the CLOCK-ARNTL/BMAL1 heterodimer; involved in the di and trimethylation of 'Lys-27' of histone H3 on PER1/2 promoters which is necessary for the CRY1/2 proteins to inhibit transcription.
Specific Function
Chromatin binding
Gene Name
EZH2
Uniprot ID
Q15910
Uniprot Name
Histone-lysine N-methyltransferase EZH2
Molecular Weight
85362.435 Da
References
  1. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH1 complex, which methylates 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Required for embryonic stem cell derivation and self-renewal, suggesting that it is involved in safeguarding embryonic stem cell identity. Compared to EZH2-containing complexes, it is less abundant in embryonic stem cells, has weak methyltransferase activity and plays a less critical role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation.
Specific Function
Chromatin binding
Gene Name
EZH1
Uniprot ID
Q92800
Uniprot Name
Histone-lysine N-methyltransferase EZH1
Molecular Weight
85270.37 Da
References
  1. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]

Enzymes

Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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...

Components:
References
  1. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Italiano A, Soria JC, Toulmonde M, Michot JM, Lucchesi C, Varga A, Coindre JM, Blakemore SJ, Clawson A, Suttle B, McDonald AA, Woodruff M, Ribich S, Hedrick E, Keilhack H, Thomson B, Owa T, Copeland RA, Ho PTC, Ribrag V: Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study. Lancet Oncol. 2018 May;19(5):649-659. doi: 10.1016/S1470-2045(18)30145-1. Epub 2018 Apr 9. [PubMed:29650362]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Zhang P, de Gooijer MC, Buil LC, Beijnen JH, Li G, van Tellingen O: ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors. Int J Cancer. 2015 Oct 15;137(8):2007-18. doi: 10.1002/ijc.29566. Epub 2015 Apr 24. [PubMed:25868794]
  2. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. FDA Approved Drug Products: Tazverik Tazemetostat Oral Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Zhang P, de Gooijer MC, Buil LC, Beijnen JH, Li G, van Tellingen O: ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors. Int J Cancer. 2015 Oct 15;137(8):2007-18. doi: 10.1002/ijc.29566. Epub 2015 Apr 24. [PubMed:25868794]

Drug created on October 20, 2016 19:01 / Updated on June 12, 2020 10:53

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