Peringatan Keamanan

LD50 information and overdose information for tucatinib are not readily available in the literature. In the case of an overdose with this drug, increased adverse effects, such as diarrhea, nausea, abdominal pain, vomiting fatigue, hepatotoxicity, vomiting, decreased appetite, anemia, headache, and rash are expected.A193590,L12945

Tucatinib

DB11652

small molecule approved investigational

Deskripsi

Tucatinib is a kinase inhibitor drug used with trastuzumab and capecitabine in the treatment of unresectable or metastatic HER-2 positive breast cancer. It was developed by Seattle Genetics and approved by the FDA on April 17, 2020.L12951 Tucatinib is a promising new treatment for patients with metastatic breast cancer who have not responded adequately to other chemotherapy regimens.L12945

Struktur Molekul 2D

Berat 480.532
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) A pharmacokinetic study revealed a half-life of approximately 5.38 hours.[A193593] Prescribing information mentions a geometric mean half-life of about 8.21 hours.[L12945]
Volume Distribusi The volume of distribution of tucatinib is about 1670 L.[L12945] This drug penetrates the blood-brain barrier.[A193605]
Klirens (Clearance) The apparent clearance is 148 L/h.[L12945]

Absorpsi

The Tmax for tucatinib ranges from 1 to 4 hours.L12945 One pharmacokinetic study revealed a Cmax of 1120 ng/mL after a dose of 350 mg twice daily with a Tmax ranging from 1 to 3 hours. The AUCtau was reported to be about 7120 hours×ng/mL.A193554

Metabolisme

Tucatinib is metabolized by CYP2C8 with some contributions from CYP3A.L12945

Rute Eliminasi

In a study of radiolabled tucatinib, about 86% of the total dose was excreted in the feces and 4.1% was found in the urine. About 16% of the tucatinib dose recovered in the feces was identified as unchanged tucatinib.L12945

Interaksi Makanan

1 Data
  • 1. Take with or without food. There is no meaningful clinical effect of food on this drug.

Interaksi Obat

1041 Data
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Tucatinib.
Mifepristone The serum concentration of Tucatinib can be increased when it is combined with Mifepristone.
Troglitazone The metabolism of Tucatinib can be decreased when combined with Troglitazone.
Nabilone The metabolism of Tucatinib can be decreased when combined with Nabilone.
Irbesartan The metabolism of Tucatinib can be decreased when combined with Irbesartan.
Tipiracil The excretion of Tipiracil can be decreased when combined with Tucatinib.
Vemurafenib The serum concentration of Tucatinib can be increased when it is combined with Vemurafenib.
Caffeine Caffeine may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Genistein The metabolism of Tucatinib can be decreased when combined with Genistein.
Topiroxostat The metabolism of Tucatinib can be decreased when combined with Topiroxostat.
Daidzin Daidzin may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Naringenin Naringenin may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Elacridar Elacridar may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Eltrombopag The metabolism of Tucatinib can be decreased when combined with Eltrombopag.
Teriflunomide The metabolism of Tucatinib can be decreased when combined with Teriflunomide.
Alectinib Alectinib may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Letermovir The metabolism of Tucatinib can be decreased when combined with Letermovir.
Clofazimine Clofazimine may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Tucatinib which could result in a higher serum level.
Fluconazole The serum concentration of Tucatinib can be increased when it is combined with Fluconazole.
Loxapine The serum concentration of Tucatinib can be increased when it is combined with Loxapine.
Biricodar The serum concentration of Tucatinib can be increased when it is combined with Biricodar.
Zosuquidar The serum concentration of Tucatinib can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Tucatinib can be increased when it is combined with Tariquidar.
Brefeldin A The serum concentration of Tucatinib can be increased when it is combined with Brefeldin A.
Carfilzomib The serum concentration of Carfilzomib can be increased when it is combined with Tucatinib.
Sarecycline The serum concentration of Tucatinib can be increased when it is combined with Sarecycline.
Favipiravir The serum concentration of Tucatinib can be increased when it is combined with Favipiravir.
Laniquidar The serum concentration of Tucatinib can be increased when it is combined with Laniquidar.
ONT-093 The serum concentration of Tucatinib can be increased when it is combined with ONT-093.
Reserpine The serum concentration of Tucatinib can be increased when it is combined with Reserpine.
Arsenic trioxide The serum concentration of Tucatinib can be increased when it is combined with Arsenic trioxide.
Umbralisib The serum concentration of Tucatinib can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Tucatinib can be increased when it is combined with Diosmin.
Sapropterin The serum concentration of Tucatinib can be increased when it is combined with Sapropterin.
Levoketoconazole The metabolism of Tucatinib can be decreased when combined with Levoketoconazole.
Varenicline The excretion of Varenicline can be decreased when combined with Tucatinib.
Prazosin The serum concentration of Prazosin can be increased when it is combined with Tucatinib.
Ranitidine The serum concentration of Ranitidine can be increased when it is combined with Tucatinib.
Solriamfetol The serum concentration of Solriamfetol can be increased when it is combined with Tucatinib.
Choline salicylate The serum concentration of Choline salicylate can be increased when it is combined with Tucatinib.
Choline The serum concentration of Choline can be increased when it is combined with Tucatinib.
Norepinephrine The serum concentration of Norepinephrine can be increased when it is combined with Tucatinib.
Pramipexole The serum concentration of Pramipexole can be increased when it is combined with Tucatinib.
Cimetidine The metabolism of Tucatinib can be decreased when combined with Cimetidine.
Epinephrine The serum concentration of Epinephrine can be increased when it is combined with Tucatinib.
Lamivudine The serum concentration of Lamivudine can be increased when it is combined with Tucatinib.
Amantadine The serum concentration of Amantadine can be increased when it is combined with Tucatinib.
Dopamine The serum concentration of Dopamine can be increased when it is combined with Tucatinib.
Memantine The serum concentration of Memantine can be increased when it is combined with Tucatinib.
Histamine The serum concentration of Histamine can be increased when it is combined with Tucatinib.
Nafamostat The serum concentration of Nafamostat can be increased when it is combined with Tucatinib.
Cholesterol Cholesterol may increase the excretion rate of Tucatinib which could result in a lower serum level and potentially a reduction in efficacy.
Pyrimethamine The metabolism of Tucatinib can be decreased when combined with Pyrimethamine.
Ketoprofen The metabolism of Tucatinib can be decreased when combined with Ketoprofen.
Ticlopidine The metabolism of Tucatinib can be decreased when combined with Ticlopidine.
Candesartan The metabolism of Tucatinib can be decreased when combined with Candesartan.
Raloxifene The metabolism of Tucatinib can be decreased when combined with Raloxifene.
Nilutamide The metabolism of Tucatinib can be decreased when combined with Nilutamide.
Metronidazole The metabolism of Tucatinib can be decreased when combined with Metronidazole.
Deferasirox The metabolism of Tucatinib can be decreased when combined with Deferasirox.
Licofelone The metabolism of Tucatinib can be decreased when combined with Licofelone.
Sulfaphenazole The metabolism of Tucatinib can be decreased when combined with Sulfaphenazole.
Miconazole The metabolism of Tucatinib can be decreased when combined with Miconazole.
Probenecid The metabolism of Tucatinib can be increased when combined with Probenecid.
Torasemide The metabolism of Tucatinib can be decreased when combined with Torasemide.
Ketorolac The metabolism of Tucatinib can be decreased when combined with Ketorolac.
Mephenytoin The metabolism of Tucatinib can be decreased when combined with Mephenytoin.
Amodiaquine The metabolism of Tucatinib can be decreased when combined with Amodiaquine.
Naproxen The metabolism of Tucatinib can be decreased when combined with Naproxen.
Tazarotene The metabolism of Tucatinib can be decreased when combined with Tazarotene.
Propofol The metabolism of Tucatinib can be decreased when combined with Propofol.
Anastrozole The metabolism of Tucatinib can be decreased when combined with Anastrozole.
Beraprost The metabolism of Tucatinib can be decreased when combined with Beraprost.
Muraglitazar The metabolism of Tucatinib can be decreased when combined with Muraglitazar.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Tucatinib is combined with Benzyl alcohol.
Capravirine The metabolism of Tucatinib can be decreased when combined with Capravirine.
Olodaterol The metabolism of Tucatinib can be decreased when combined with Olodaterol.
Dexibuprofen The metabolism of Tucatinib can be decreased when combined with Dexibuprofen.
Ozanimod The metabolism of Ozanimod can be decreased when combined with Tucatinib.
Apomorphine The metabolism of Tucatinib can be decreased when combined with Apomorphine.
Tolbutamide The metabolism of Tucatinib can be decreased when combined with Tolbutamide.
Piroxicam The metabolism of Tucatinib can be decreased when combined with Piroxicam.
Fluorouracil The metabolism of Fluorouracil can be decreased when combined with Tucatinib.
Tegafur The metabolism of Tegafur can be decreased when combined with Tucatinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Tucatinib.
Ciprofloxacin The excretion of Ciprofloxacin can be decreased when combined with Tucatinib.
Acyclovir The excretion of Acyclovir can be decreased when combined with Tucatinib.
Emtricitabine The excretion of Emtricitabine can be decreased when combined with Tucatinib.
Ganciclovir The excretion of Ganciclovir can be decreased when combined with Tucatinib.
Levofloxacin The excretion of Levofloxacin can be decreased when combined with Tucatinib.
Flecainide The excretion of Flecainide can be decreased when combined with Tucatinib.
Nadolol The excretion of Nadolol can be decreased when combined with Tucatinib.

Target Protein

Receptor tyrosine-protein kinase erbB-2 ERBB2
Receptor tyrosine-protein kinase erbB-3 ERBB3

Referensi & Sumber

Synthesis reference: Philip Kocienski. Synthesis of Tucatinib.Synthesis of Natural Products and Potential Drugs 2019. Georg Thieme Verlag Stuttgart DOI 10.1055/s-0039-1690496
Artikel (PubMed)
  • PMID: 32241871
    Kulukian A, Lee P, Taylor J, Rosler R, de Vries P, Watson D, Forero-Torres A, Peterson S: Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models. Mol Cancer Ther. 2020 Apr;19(4):976-987. doi: 10.1158/1535-7163.MCT-19-0873.
  • PMID: 29955792
    Borges VF, Ferrario C, Aucoin N, Falkson C, Khan Q, Krop I, Welch S, Conlin A, Chaves J, Bedard PL, Chamberlain M, Gray T, Vo A, Hamilton E: Tucatinib Combined With Ado-Trastuzumab Emtansine in Advanced ERBB2/HER2-Positive Metastatic Breast Cancer: A Phase 1b Clinical Trial. JAMA Oncol. 2018 Sep 1;4(9):1214-1220. doi: 10.1001/jamaoncol.2018.1812.
  • PMID: 29804905
    Murthy R, Borges VF, Conlin A, Chaves J, Chamberlain M, Gray T, Vo A, Hamilton E: Tucatinib with capecitabine and trastuzumab in advanced HER2-positive metastatic breast cancer with and without brain metastases: a non-randomised, open-label, phase 1b study. Lancet Oncol. 2018 Jul;19(7):880-888. doi: 10.1016/S1470-2045(18)30256-0. Epub 2018 May 24.
  • PMID: 28053022
    Moulder SL, Borges VF, Baetz T, Mcspadden T, Fernetich G, Murthy RK, Chavira R, Guthrie K, Barrett E, Chia SK: Phase I Study of ONT-380, a HER2 Inhibitor, in Patients with HER2(+)-Advanced Solid Tumors, with an Expansion Cohort in HER2(+) Metastatic Breast Cancer (MBC). Clin Cancer Res. 2017 Jul 15;23(14):3529-3536. doi: 10.1158/1078-0432.CCR-16-1496. Epub 2017 Jan 4.
  • PMID: 29772459
    Duchnowska R, Loibl S, Jassem J: Tyrosine kinase inhibitors for brain metastases in HER2-positive breast cancer. Cancer Treat Rev. 2018 Jun;67:71-77. doi: 10.1016/j.ctrv.2018.05.004. Epub 2018 May 9.
  • PMID: 15912202
    Paul MK, Mukhopadhyay AK: Tyrosine kinase - Role and significance in Cancer. Int J Med Sci. 2004;1(2):101-115. doi: 10.7150/ijms.1.101. Epub 2004 Jun 1.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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