Peringatan Keamanan

No data are available regarding overdosage with mobocertinib. Symptoms of overdosage are likely to be consistent with mobocertinib's adverse effects and may therefore include significant gastrointestinal symptoms, pain, fatigue, and rash.L38319

Mobocertinib

DB16390

small molecule approved investigational

Deskripsi

Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used specifically in the treatment of non-small cell lung cancer (NSCLC) caused by exon 20 insertion mutations in the EGFR gene,L38368 which are typically associated with a poorer prognosis (as compared to "classical" EGFR mutants causing NSCLC) and are associated with resistance to standard targeted EGFR inhibitors.A238828 Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on EGFR exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.L38319

Mobocertinib, under the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated approval by the FDA in September 2021 for the treatment of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.L38368

Struktur Molekul 2D

Berat 585.709
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) At steady-state, the mean elimination half-life of mobocertinib and its two active metabolites, AP32960 and AP32914, was 18 hours, 24 hours, and 18 hours, respectively.[L38319]
Volume Distribusi The mean apparent volume of distribution of mobocertinib was approximately 3,509 L at steady-state.[L38319]
Klirens (Clearance) At steady-state, the mean apparent oral clearance of mobocertinib and its two active metabolites, AP32960 and AP32914, was 138 L/hr, 149 L/hr, and 159 L/hr, respectively.[L38319]

Absorpsi

The mean absolute bioavailability of mobocertinib is 37% and the median Tmax is approximately 4 hours.L38319 Following a single oral dose of 160mg of mobocertinib to fasted patients, the mean Cmax and AUC0-inf were 45.8 ng/mL and 862 ng•h/mL, respectively.A238743

Metabolisme

Mobocertinib is metabolized primarily by CYP3A enzymes to two active metabolites, AP32960 and AP32914, which are equipotent to mobocertinib and account for 36% and 4% of its combined molar AUC, respectively.L38319

Rute Eliminasi

Following oral administration of mobocertinib, approximately 76% of the administered dose was recovered in the feces (6% as unchanged parent drug) with only 4% recovered in the urine (1% as unchanged parent drug).L38319 The metabolite AP32960 comprised 12% and 1% of the recovered dose found in the feces and urine, respectively, while the metabolite AP32914 was below the detection limit in both.

Interaksi Makanan

2 Data
  • 1. Avoid St. John's Wort. St. John's Wort is a potent CYP3A inducer and may decrease the efficacy of mobocertinib.
  • 2. Take with or without food. Co-administration with food does not significantly affect the disposition of mobocertinib.

Interaksi Obat

760 Data
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Mobocertinib.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Mobocertinib.
Octreotide The risk or severity of QTc prolongation can be increased when Octreotide is combined with Mobocertinib.
Oxytocin The risk or severity of QTc prolongation can be increased when Oxytocin is combined with Mobocertinib.
Esmolol The risk or severity of QTc prolongation can be increased when Esmolol is combined with Mobocertinib.
Bortezomib The risk or severity of QTc prolongation can be increased when Bortezomib is combined with Mobocertinib.
Betaxolol The risk or severity of QTc prolongation can be increased when Betaxolol is combined with Mobocertinib.
Fluconazole The risk or severity of QTc prolongation can be increased when Fluconazole is combined with Mobocertinib.
Erythromycin The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Mobocertinib.
Dofetilide The risk or severity of QTc prolongation can be increased when Dofetilide is combined with Mobocertinib.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Mobocertinib.
Citalopram The risk or severity of QTc prolongation can be increased when Citalopram is combined with Mobocertinib.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Mobocertinib.
Nelfinavir The risk or severity of QTc prolongation can be increased when Nelfinavir is combined with Mobocertinib.
Pregabalin The risk or severity of QTc prolongation can be increased when Pregabalin is combined with Mobocertinib.
Ranolazine The risk or severity of QTc prolongation can be increased when Ranolazine is combined with Mobocertinib.
Benzatropine The risk or severity of QTc prolongation can be increased when Benzatropine is combined with Mobocertinib.
Ziprasidone The risk or severity of QTc prolongation can be increased when Ziprasidone is combined with Mobocertinib.
Anagrelide The risk or severity of QTc prolongation can be increased when Anagrelide is combined with Mobocertinib.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Mobocertinib.
Isradipine The risk or severity of QTc prolongation can be increased when Isradipine is combined with Mobocertinib.
Disopyramide The risk or severity of QTc prolongation can be increased when Disopyramide is combined with Mobocertinib.
Clemastine The risk or severity of QTc prolongation can be increased when Clemastine is combined with Mobocertinib.
Atomoxetine The risk or severity of QTc prolongation can be increased when Atomoxetine is combined with Mobocertinib.
Ibutilide The risk or severity of QTc prolongation can be increased when Ibutilide is combined with Mobocertinib.
Valproic acid The risk or severity of QTc prolongation can be increased when Valproic acid is combined with Mobocertinib.
Amitriptyline The risk or severity of QTc prolongation can be increased when Amitriptyline is combined with Mobocertinib.
Methadone The risk or severity of QTc prolongation can be increased when Methadone is combined with Mobocertinib.
Olanzapine The risk or severity of QTc prolongation can be increased when Olanzapine is combined with Mobocertinib.
Cetirizine The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Mobocertinib.
Terfenadine The risk or severity of QTc prolongation can be increased when Terfenadine is combined with Mobocertinib.
Diltiazem The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Mobocertinib.
Protriptyline The risk or severity of QTc prolongation can be increased when Protriptyline is combined with Mobocertinib.
Alfuzosin The risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Mobocertinib.
Trimethadione The risk or severity of QTc prolongation can be increased when Trimethadione is combined with Mobocertinib.
Buclizine The risk or severity of QTc prolongation can be increased when Buclizine is combined with Mobocertinib.
Mefloquine The risk or severity of QTc prolongation can be increased when Mefloquine is combined with Mobocertinib.
Clozapine The risk or severity of QTc prolongation can be increased when Clozapine is combined with Mobocertinib.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Grepafloxacin is combined with Mobocertinib.
Doxylamine The risk or severity of QTc prolongation can be increased when Doxylamine is combined with Mobocertinib.
Mirtazapine The risk or severity of QTc prolongation can be increased when Mirtazapine is combined with Mobocertinib.
Timolol The risk or severity of QTc prolongation can be increased when Timolol is combined with Mobocertinib.
Treprostinil The risk or severity of QTc prolongation can be increased when Treprostinil is combined with Mobocertinib.
Digoxin The risk or severity of QTc prolongation can be increased when Digoxin is combined with Mobocertinib.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Mobocertinib.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Mobocertinib.
Sorafenib The risk or severity of QTc prolongation can be increased when Sorafenib is combined with Mobocertinib.
Dexbrompheniramine The risk or severity of QTc prolongation can be increased when Dexbrompheniramine is combined with Mobocertinib.
Promazine The risk or severity of QTc prolongation can be increased when Promazine is combined with Mobocertinib.
Hyoscyamine The risk or severity of QTc prolongation can be increased when Hyoscyamine is combined with Mobocertinib.
Triprolidine The risk or severity of QTc prolongation can be increased when Triprolidine is combined with Mobocertinib.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Mobocertinib.
Cyproheptadine The risk or severity of QTc prolongation can be increased when Cyproheptadine is combined with Mobocertinib.
Droperidol The risk or severity of QTc prolongation can be increased when Droperidol is combined with Mobocertinib.
Imipramine The risk or severity of QTc prolongation can be increased when Imipramine is combined with Mobocertinib.
Enoxacin The risk or severity of QTc prolongation can be increased when Enoxacin is combined with Mobocertinib.
Quinine The risk or severity of QTc prolongation can be increased when Quinine is combined with Mobocertinib.
Fluoxetine The risk or severity of QTc prolongation can be increased when Fluoxetine is combined with Mobocertinib.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Chlorpromazine is combined with Mobocertinib.
Pefloxacin The risk or severity of QTc prolongation can be increased when Pefloxacin is combined with Mobocertinib.
Sotalol The risk or severity of QTc prolongation can be increased when Sotalol is combined with Mobocertinib.
Haloperidol The risk or severity of QTc prolongation can be increased when Haloperidol is combined with Mobocertinib.
Ritonavir The risk or severity of QTc prolongation can be increased when Ritonavir is combined with Mobocertinib.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Mobocertinib.
Foscarnet The risk or severity of QTc prolongation can be increased when Foscarnet is combined with Mobocertinib.
Erlotinib The risk or severity of QTc prolongation can be increased when Erlotinib is combined with Mobocertinib.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Mobocertinib.
Toremifene The risk or severity of QTc prolongation can be increased when Toremifene is combined with Mobocertinib.
Nortriptyline The risk or severity of QTc prolongation can be increased when Nortriptyline is combined with Mobocertinib.
Amoxapine The risk or severity of QTc prolongation can be increased when Amoxapine is combined with Mobocertinib.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Mobocertinib.
Lamotrigine The risk or severity of QTc prolongation can be increased when Lamotrigine is combined with Mobocertinib.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Mobocertinib.
Hydroxyzine The risk or severity of QTc prolongation can be increased when Mobocertinib is combined with Hydroxyzine.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Mobocertinib.
Propranolol The risk or severity of QTc prolongation can be increased when Propranolol is combined with Mobocertinib.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Mobocertinib.
Voriconazole The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Mobocertinib.
Ethosuximide The risk or severity of QTc prolongation can be increased when Ethosuximide is combined with Mobocertinib.
Cisapride The risk or severity of QTc prolongation can be increased when Cisapride is combined with Mobocertinib.
Chloroquine The risk or severity of QTc prolongation can be increased when Chloroquine is combined with Mobocertinib.
Amodiaquine The risk or severity of QTc prolongation can be increased when Amodiaquine is combined with Mobocertinib.
Imatinib The risk or severity of QTc prolongation can be increased when Imatinib is combined with Mobocertinib.
Nicardipine The risk or severity of QTc prolongation can be increased when Nicardipine is combined with Mobocertinib.
Efavirenz The risk or severity of QTc prolongation can be increased when Efavirenz is combined with Mobocertinib.
Astemizole The risk or severity of QTc prolongation can be increased when Astemizole is combined with Mobocertinib.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Mobocertinib.
Trazodone The risk or severity of QTc prolongation can be increased when Trazodone is combined with Mobocertinib.
Galantamine The risk or severity of QTc prolongation can be increased when Galantamine is combined with Mobocertinib.
Tamoxifen The risk or severity of QTc prolongation can be increased when Tamoxifen is combined with Mobocertinib.
Thioridazine The risk or severity of QTc prolongation can be increased when Thioridazine is combined with Mobocertinib.
Moricizine The risk or severity of QTc prolongation can be increased when Moricizine is combined with Mobocertinib.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Trovafloxacin is combined with Mobocertinib.
Moexipril The risk or severity of QTc prolongation can be increased when Moexipril is combined with Mobocertinib.
Tizanidine The risk or severity of QTc prolongation can be increased when Tizanidine is combined with Mobocertinib.
Ibandronate The risk or severity of QTc prolongation can be increased when Ibandronate is combined with Mobocertinib.
Apomorphine The risk or severity of QTc prolongation can be increased when Apomorphine is combined with Mobocertinib.
Azatadine The risk or severity of QTc prolongation can be increased when Azatadine is combined with Mobocertinib.
Trimipramine The risk or severity of QTc prolongation can be increased when Trimipramine is combined with Mobocertinib.
Risperidone The risk or severity of QTc prolongation can be increased when Risperidone is combined with Mobocertinib.

Target Protein

Epidermal growth factor receptor EGFR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34145979
    Zhang S, Jin S, Griffin C, Feng Z, Lin J, Venkatakrishnan K, Gupta N: Effects of Itraconazole and Rifampin on the Pharmacokinetics of Mobocertinib (TAK-788), an Oral Epidermal Growth Factor Receptor Inhibitor, in Healthy Volunteers. Clin Pharmacol Drug Dev. 2021 Sep;10(9):1044-1053. doi: 10.1002/cpdd.967. Epub 2021 Jun 19.
  • PMID: 34118178
    Zhang S, Jin S, Griffin C, Feng Z, Lin J, Baratta M, Brake R, Venkatakrishnan K, Gupta N: Single-Dose Pharmacokinetics and Tolerability of the Oral Epidermal Growth Factor Receptor Inhibitor Mobocertinib (TAK-788) in Healthy Volunteers: Low-Fat Meal Effect and Relative Bioavailability of 2 Capsule Products. Clin Pharmacol Drug Dev. 2021 Sep;10(9):1028-1043. doi: 10.1002/cpdd.951. Epub 2021 Jun 12.
  • PMID: 33728415
    Vasconcelos PENS, Kobayashi IS, Kobayashi SS, Costa DB: Preclinical characterization of mobocertinib highlights the putative therapeutic window of this novel EGFR inhibitor to EGFR exon 20 insertion mutations. JTO Clin Res Rep. 2021 Mar;2(3). doi: 10.1016/j.jtocrr.2020.100105. Epub 2020 Oct 6.
  • PMID: 33632773
    Gonzalvez F, Vincent S, Baker TE, Gould AE, Li S, Wardwell SD, Nadworny S, Ning Y, Zhang S, Huang WS, Hu Y, Li F, Greenfield MT, Zech SG, Das B, Narasimhan NI, Clackson T, Dalgarno D, Shakespeare WC, Fitzgerald M, Chouitar J, Griffin RJ, Liu S, Wong KK, Zhu X, Rivera VM: Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer. Cancer Discov. 2021 Jul;11(7):1672-1687. doi: 10.1158/2159-8290.CD-20-1683. Epub 2021 Feb 25.
  • PMID: 22263017
    Bethune G, Bethune D, Ridgway N, Xu Z: Epidermal growth factor receptor (EGFR) in lung cancer: an overview and update. J Thorac Dis. 2010 Mar;2(1):48-51.
  • PMID: 30854234
    Vyse S, Huang PH: Targeting EGFR exon 20 insertion mutations in non-small cell lung cancer. Signal Transduct Target Ther. 2019 Mar 8;4:5. doi: 10.1038/s41392-019-0038-9. eCollection 2019.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Exkivity
    Capsule • 40 mg/1 • Oral • US • Approved
International Brands
  • Exkivity — Takeda Pharmaceutical Company Limited

Sekuens Gen/Protein (FASTA)

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