Peringatan Keamanan

Data regarding the presentation and management of tazemetostat overdoses are not readily available.L11476 The most common adverse reactions associated with tazemetostat are pain, fatigue, nausea, decreased appetite, vomiting, and constipation.L11476

Tazemetostat

DB12887

small molecule approved investigational

Deskripsi

Tazemetostat is a methyltransferase inhibitor used to treat metastatic or locally advanced epithelioid sarcoma not eligible for complete resection.L11476 Tazemetostat was first named in literature as EPZ-6438.A190363

Tazemetaostat was granted FDA approval on 23 January 2020.L11476

Struktur Molekul 2D

Berat 572.75
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Tazemetostat has a terminal elimination half life of 3.1h.[A190360,L11476]
Volume Distribusi Tazemetostat has a volume of distribution of 1230L.[L11476]
Klirens (Clearance) Tazemetostat has an apparent total clearance of 274L/h.[L11476]

Absorpsi

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.A190360,L11476 Absorption is not significantly affected by a high fat, high calorie meal.L11476 Tazemetostat is 33% bioavailable.L11476

Metabolisme

Tazemetostat is metabolized by CYP3A4 to an inactive desethyl metabolite and one other inactive metabolite not described.A190360,L11476

Rute Eliminasi

Tazemetostat is 15% eliminated in urine and 79% eliminated in feces.L11476

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

644 Data
Ranolazine The serum concentration of Tazemetostat can be increased when it is combined with Ranolazine.
Fosphenytoin The metabolism of Tazemetostat can be increased when combined with Fosphenytoin.
Phenytoin The metabolism of Tazemetostat can be increased when combined with Phenytoin.
Lumacaftor The serum concentration of Tazemetostat can be decreased when it is combined with Lumacaftor.
Bexarotene The metabolism of Tazemetostat can be increased when combined with Bexarotene.
Bosentan The metabolism of Tazemetostat can be increased when combined with Bosentan.
Nafcillin The metabolism of Tazemetostat can be increased when combined with Nafcillin.
Modafinil The metabolism of Tazemetostat can be increased when combined with Modafinil.
Etravirine The metabolism of Tazemetostat can be increased when combined with Etravirine.
Avasimibe The metabolism of Tazemetostat can be increased when combined with Avasimibe.
Echinacea The metabolism of Tazemetostat can be increased when combined with Echinacea.
Dexamethasone acetate The metabolism of Tazemetostat can be increased when combined with Dexamethasone acetate.
Vemurafenib The serum concentration of Tazemetostat can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Tazemetostat can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Tazemetostat can be decreased when it is combined with Pitolisant.
Isavuconazole The serum concentration of Tazemetostat can be increased when it is combined with Isavuconazole.
Isavuconazonium The serum concentration of Tazemetostat can be increased when it is combined with Isavuconazonium.
Pravastatin Pravastatin may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Caffeine Caffeine may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Diethylstilbestrol Diethylstilbestrol may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Gefitinib Gefitinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Beclomethasone dipropionate Beclomethasone dipropionate may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Estradiol Estradiol may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Buprenorphine Buprenorphine may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Genistein Genistein may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Topiroxostat Topiroxostat may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Fusidic acid The metabolism of Tazemetostat can be decreased when combined with Fusidic acid.
Naringenin Naringenin may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Elacridar Elacridar may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Eltrombopag Eltrombopag may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Simeprevir The metabolism of Tazemetostat can be decreased when combined with Simeprevir.
Safinamide Safinamide may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Afatinib Afatinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Daclatasvir Daclatasvir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Dasabuvir Dasabuvir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Rolapitant Rolapitant may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Paritaprevir Paritaprevir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Velpatasvir Velpatasvir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Istradefylline Istradefylline may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Glasdegib Glasdegib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Fostamatinib Fostamatinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Voxilaprevir Voxilaprevir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Letermovir The metabolism of Tazemetostat can be decreased when combined with Letermovir.
Gilteritinib Gilteritinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Rucaparib Rucaparib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Fedratinib The serum concentration of Tazemetostat can be increased when it is combined with Fedratinib.
Pibrentasvir Pibrentasvir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Glecaprevir Glecaprevir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Estradiol acetate Estradiol acetate may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Estradiol benzoate Estradiol benzoate may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Estradiol cypionate Estradiol cypionate may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Estradiol dienanthate Estradiol dienanthate may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Estradiol valerate Estradiol valerate may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Medical Cannabis The metabolism of Tazemetostat can be decreased when combined with Medical Cannabis.
Nabiximols Nabiximols may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Rilpivirine Rilpivirine may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Ripretinib Ripretinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Fostemsavir Fostemsavir may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Tazemetostat.
Tivozanib Tivozanib may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Belumosudil Belumosudil may decrease the excretion rate of Tazemetostat which could result in a higher serum level.
Fluconazole The metabolism of Tazemetostat can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Tazemetostat can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Tazemetostat can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Tazemetostat can be increased when it is combined with Reserpine.
Loxapine The serum concentration of Tazemetostat can be increased when it is combined with Loxapine.
Quinine The serum concentration of Tazemetostat can be increased when it is combined with Quinine.
Toremifene The serum concentration of Tazemetostat can be increased when it is combined with Toremifene.
Verapamil The metabolism of Tazemetostat can be decreased when combined with Verapamil.
Mifepristone The serum concentration of Tazemetostat can be increased when it is combined with Mifepristone.
Zonisamide The serum concentration of Tazemetostat can be increased when it is combined with Zonisamide.
Carvedilol The serum concentration of Tazemetostat can be increased when it is combined with Carvedilol.
Propafenone The serum concentration of Tazemetostat can be increased when it is combined with Propafenone.
Lapatinib The serum concentration of Tazemetostat can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Tazemetostat can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Tazemetostat can be increased when it is combined with Mibefradil.
Biricodar The serum concentration of Tazemetostat can be increased when it is combined with Biricodar.
Flibanserin The serum concentration of Tazemetostat can be increased when it is combined with Flibanserin.
Zosuquidar The serum concentration of Tazemetostat can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Tazemetostat can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Tazemetostat can be increased when it is combined with Brefeldin A.
Ivacaftor The serum concentration of Tazemetostat can be increased when it is combined with Ivacaftor.
Linagliptin The metabolism of Tazemetostat can be decreased when combined with Linagliptin.
Mirabegron The serum concentration of Tazemetostat can be increased when it is combined with Mirabegron.

Target Protein

Histone-lysine N-methyltransferase EZH2 EZH2
Histone-lysine N-methyltransferase EZH1 EZH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31970877
    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.
  • PMID: 24531722
    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.
  • PMID: 29650364
    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.
  • PMID: 29650362
    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.
  • PMID: 24563539
    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.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Tazverik
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
International Brands
  • Tazverik

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul