Peringatan Keamanan

There is no information available regarding acute toxicity and overdose of futibatinib.

Futibatinib

DB15149

small molecule approved investigational

Deskripsi

Futibatinib is an inhibitor of Fibroblast Growth Factor receptor (FGFR), which comprises a group of receptor tyrosine kinases that play a key role in cell proliferation, differentiation, migration, and survival. FGFR was investigated in oncology as a therapeutic target, as FGFR genomic aberrations and dysregulated FGFR signalling pathways are observed in some cancers such as cholangiocarcinoma and urothelial malignancies.A253193,A253198

As a novel inhibitor of FGFR, futibatinib was first approved by the FDA in September 2022 to treat different types of intrahepatic cholangiocarcinoma.L43347 On July 4, 2023, the European Commission granted Conditional Marketing Authorization for futibatinib for the treatment of cholangiocarcinoma.L47800

Struktur Molekul 2D

Berat 418.457
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean (CV%) elimination half-life (t<sub>1/2</sub>) of futibatinib is 2.9 hours (27%).[L43347]
Volume Distribusi The geometric mean (CV%) apparent volume of distribution (Vc/F) is 66 L (18%).[L43347]
Klirens (Clearance) The geometric mean (CV%) apparent clearance (CL/F) is 20 L/h (23%).[L43347]

Absorpsi

Tmax ranges from 1.2 to 22.8 hours, with a median value of two hours. In healthy subjects, a high-fat and high-calorie meal (900 to 1000 calories with approximately 50% of total caloric content from fat) decreased futibatinib AUC by 11% and Cmax by 42%.L43347

Metabolisme

In vitro, futibatinib is primarily metabolized by CYP3A and to a lesser extent by CYP2C9 and CYP2D6. Unchanged futibatinib is the major drug-related moiety in plasma (accounting for 59% of radioactivity) in healthy subjects.L43347

Rute Eliminasi

Following a single oral dose of 20 mg radiolabeled futibatinib, approximately 91% of the total recovered radioactivity was observed in feces and 9% in urine, with negligible unchanged futibatinib in urine or feces.L43347

Interaksi Makanan

2 Data
  • 1. Take at the same time every day.
  • 2. Take with or without food. A high-fat and high-calorie meal decreases drug exposure, but not to a clinically significant extent.

Interaksi Obat

347 Data
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Futibatinib.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Futibatinib.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Futibatinib.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Futibatinib.
Ranolazine The serum concentration of Futibatinib can be increased when it is combined with Ranolazine.
Lumacaftor The metabolism of Futibatinib can be increased when combined with Lumacaftor.
Phenytoin The metabolism of Futibatinib can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Futibatinib can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Futibatinib can be increased when combined with Carbamazepine.
Mitotane The metabolism of Futibatinib can be increased when combined with Mitotane.
Primidone The metabolism of Futibatinib can be increased when combined with Primidone.
Rifampin The metabolism of Futibatinib can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Futibatinib can be increased when combined with Phenobarbital.
Rifapentine The metabolism of Futibatinib can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Futibatinib can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Futibatinib can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Futibatinib can be increased when combined with St. John's Wort.
Midostaurin The metabolism of Futibatinib can be decreased when combined with Midostaurin.
Enzalutamide The metabolism of Futibatinib can be increased when combined with Enzalutamide.
Apalutamide The metabolism of Futibatinib can be increased when combined with Apalutamide.
Cyclosporine The serum concentration of Futibatinib can be increased when it is combined with Cyclosporine.
Fluvoxamine The metabolism of Futibatinib can be decreased when combined with Fluvoxamine.
Fluconazole The serum concentration of Futibatinib can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Futibatinib can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Futibatinib can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Futibatinib can be decreased when combined with Isradipine.
Diltiazem The metabolism of Futibatinib can be decreased when combined with Diltiazem.
Clozapine The metabolism of Futibatinib can be decreased when combined with Clozapine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Futibatinib.
Ciprofloxacin The metabolism of Futibatinib can be decreased when combined with Ciprofloxacin.
Voriconazole The metabolism of Futibatinib can be decreased when combined with Voriconazole.
Nicardipine The metabolism of Futibatinib can be decreased when combined with Nicardipine.
Verapamil The serum concentration of Futibatinib can be increased when it is combined with Verapamil.
Aprepitant The metabolism of Futibatinib can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Futibatinib can be decreased when combined with Isoniazid.
Primaquine The metabolism of Futibatinib can be decreased when combined with Primaquine.
Miconazole The metabolism of Futibatinib can be decreased when combined with Miconazole.
Danazol The metabolism of Futibatinib can be decreased when combined with Danazol.
Fusidic acid The metabolism of Futibatinib can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Futibatinib can be decreased when combined with Zimelidine.
Dronedarone The serum concentration of Futibatinib can be increased when it is combined with Dronedarone.
Milnacipran The metabolism of Futibatinib can be decreased when combined with Milnacipran.
Simeprevir The serum concentration of Futibatinib can be increased when it is combined with Simeprevir.
Isavuconazonium The serum concentration of Futibatinib can be increased when it is combined with Isavuconazonium.
Desvenlafaxine The metabolism of Futibatinib can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Futibatinib can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Futibatinib can be decreased when combined with Seproxetine.
Crizotinib The serum concentration of Futibatinib can be increased when it is combined with Crizotinib.
Linagliptin The serum concentration of Futibatinib can be increased when it is combined with Linagliptin.
Indalpine The metabolism of Futibatinib can be decreased when combined with Indalpine.
Netupitant The serum concentration of Futibatinib can be increased when it is combined with Netupitant.
Barnidipine The metabolism of Futibatinib can be decreased when combined with Barnidipine.
Benidipine The metabolism of Futibatinib can be decreased when combined with Benidipine.
Venetoclax The serum concentration of Futibatinib can be increased when it is combined with Venetoclax.
Isavuconazole The serum concentration of Futibatinib can be increased when it is combined with Isavuconazole.
Fosnetupitant The metabolism of Futibatinib can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Futibatinib can be decreased when combined with Berotralstat.
Nelfinavir The metabolism of Futibatinib can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Futibatinib can be decreased when combined with Indinavir.
Terfenadine The metabolism of Futibatinib can be decreased when combined with Terfenadine.
Ritonavir The metabolism of Futibatinib can be decreased when combined with Ritonavir.
Efavirenz The metabolism of Futibatinib can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Futibatinib can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Futibatinib can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Futibatinib can be decreased when combined with Delavirdine.
Methimazole The metabolism of Futibatinib can be decreased when combined with Methimazole.
Conivaptan The metabolism of Futibatinib can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Futibatinib can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Futibatinib can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Futibatinib can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Futibatinib can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Futibatinib can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Futibatinib can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Futibatinib can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Futibatinib can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Futibatinib can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Futibatinib can be decreased when combined with Posaconazole.
Darunavir The metabolism of Futibatinib can be decreased when combined with Darunavir.
Lopinavir The metabolism of Futibatinib can be decreased when combined with Lopinavir.
Ditiocarb The metabolism of Futibatinib can be decreased when combined with Ditiocarb.
Nilotinib The metabolism of Futibatinib can be decreased when combined with Nilotinib.
Telaprevir The metabolism of Futibatinib can be decreased when combined with Telaprevir.
Levoketoconazole The metabolism of Futibatinib can be decreased when combined with Levoketoconazole.
Lonafarnib The metabolism of Futibatinib can be decreased when combined with Lonafarnib.
Boceprevir The metabolism of Futibatinib can be decreased when combined with Boceprevir.
Cobicistat The serum concentration of Futibatinib can be increased when it is combined with Cobicistat.
Elvitegravir The metabolism of Futibatinib can be decreased when combined with Elvitegravir.
Stiripentol The metabolism of Futibatinib can be decreased when combined with Stiripentol.
Curcumin The metabolism of Futibatinib can be decreased when combined with Curcumin.
Ribociclib The metabolism of Futibatinib can be decreased when combined with Ribociclib.
Danoprevir The metabolism of Futibatinib can be decreased when combined with Danoprevir.
Troleandomycin The metabolism of Futibatinib can be decreased when combined with Troleandomycin.
Vemurafenib The serum concentration of Futibatinib can be increased when it is combined with Vemurafenib.
Pitolisant The serum concentration of Futibatinib can be decreased when it is combined with Pitolisant.
Sildenafil The serum concentration of Futibatinib can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Futibatinib can be increased when it is combined with Reserpine.
Mefloquine The serum concentration of Futibatinib can be increased when it is combined with Mefloquine.
Sapropterin The serum concentration of Futibatinib can be increased when it is combined with Sapropterin.
Sorafenib The serum concentration of Futibatinib can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Futibatinib can be increased when it is combined with Loxapine.

Target Protein

Fibroblast growth factor receptor 1 FGFR1
Fibroblast growth factor receptor 2 FGFR2
Fibroblast growth factor receptor 3 FGFR3
Fibroblast growth factor receptor 4 FGFR4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34199304
    Kommalapati A, Tella SH, Borad M, Javle M, Mahipal A: FGFR Inhibitors in Oncology: Insight on the Management of Toxicities in Clinical Practice. Cancers (Basel). 2021 Jun 13;13(12). pii: cancers13122968. doi: 10.3390/cancers13122968.
  • PMID: 32973082
    Sootome H, Fujita H, Ito K, Ochiiwa H, Fujioka Y, Ito K, Miura A, Sagara T, Ito S, Ohsawa H, Otsuki S, Funabashi K, Yashiro M, Matsuo K, Yonekura K, Hirai H: Futibatinib Is a Novel Irreversible FGFR 1-4 Inhibitor That Shows Selective Antitumor Activity against FGFR-Deregulated Tumors. Cancer Res. 2020 Nov 15;80(22):4986-4997. doi: 10.1158/0008-5472.CAN-19-2568. Epub 2020 Sep 24.
  • PMID: 33054456
    Rizzo A, Ricci AD, Brandi G: Futibatinib, an investigational agent for the treatment of intrahepatic cholangiocarcinoma: evidence to date and future perspectives. Expert Opin Investig Drugs. 2021 Apr;30(4):317-324. doi: 10.1080/13543784.2021.1837774. Epub 2020 Oct 25.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Lytgobi
    Tablet, film coated • 4 mg • Oral • EU • Approved
  • Lytgobi
    Tablet, film coated • 4 mg • Oral • EU • Approved
  • Lytgobi
    Tablet, film coated • 4 mg • Oral • EU • Approved
  • Lytgobi
    Tablet • 4 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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