Peringatan Keamanan

Toxicity information regarding epcoritamab is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as cytokine release syndrome and immune effector cell-associated neurotoxicity syndrome.L46516 Symptomatic and supportive measures are recommended. The carcinogenicity or genotoxicity of epcoritamab has not been evaluated. No dedicated fertility studies have been conducted with epcoritamab.L46516

Epcoritamab

DB16672

biotech approved investigational

Deskripsi

Epcoritamab is an IgG1-bispecific antibody that simultaneously binds to CD3 on T-cells and CD20 on B-cells.A259736,A258488,A259761,L46516 Epcoritamab promotes the activation and expansion of T-cells and, by being able to bind to both CD20 and CD3, it leads to the T-cell–mediated killing of CD20+ malignant B cells.A259761,L46516 Diffuse large B-cell lymphoma (DLBCL) is an aggressive type of cancer commonly treated with several cycles of rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone. Although this regimen is effective in up to 60% of patients, patients with relapsed or refractory DLBCL have poor outcomes.A259736,A258488 The use of epcoritamab in this group of patients has high response rates, durable complete responses and manageable adverse events with few discontinuations.A259736

The use of epcoritamab may lead to cytokine release syndrome and immune effector cell-associated neurotoxicity syndrome.L46516 It is administered subcutaneously and is currently being evaluated as a monotherapy and in combination for the treatment of a variety of hematologic malignancies. In May 2023, epcoritamab was approved by the FDA under accelerated approval for the treatment of relapsed or refractory DLBCL. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).L46516,L46556 In September 2023, epcoritamab was also approved in the EU for the same indication.L49464

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) A full dose of epcoritamab (48 mg) has a half-life of approximately 22 days at the end of the third treatment cycle.[L46516]
Volume Distribusi Epcoritamab has an apparent total volume of distribution of 25.6 L.[L46516]
Klirens (Clearance) A full dose of epcoritamab (48 mg) has an apparent total clearance of approximately 0.53 L/day at the end of the third treatment cycle.[L46516]

Absorpsi

Over a full dosage range from 1.5 to 60 mg (0.03125 to 1.25 times the recommended dose), the AUC of epcoritamab increases in a more than dose-proportional manner. A Cmax of 11.1 mcg/mL was achieved after the eleventh dose of 48 mg (first dose of cycle 4). After the first full dose, the Tmax of epcoritamab was 4 days, and at the end of the weekly dosing regimen (end of Cycle 3), the Tmax was 2.3 days.L46516

Metabolisme

As a monoclonal antibody, epcoritamab is expected to be metabolized into small peptides by catabolic pathways throughout the body.L46516

Rute Eliminasi

Since epcoritamab is an immunoglobulin G (IgG) antibody, it is expected to be mainly eliminated via intracellular catabolism.

Interaksi Obat

971 Data
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Epcoritamab.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Epcoritamab.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Epcoritamab.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Epcoritamab.
Lidocaine The serum concentration of Lidocaine can be increased when it is combined with Epcoritamab.
Ropivacaine The serum concentration of Ropivacaine can be increased when it is combined with Epcoritamab.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Epcoritamab.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Proparacaine.
Meloxicam The serum concentration of Meloxicam can be increased when it is combined with Epcoritamab.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Oxybuprocaine.
Cocaine The serum concentration of Cocaine can be increased when it is combined with Epcoritamab.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Mepivacaine.
Levobupivacaine The serum concentration of Levobupivacaine can be increased when it is combined with Epcoritamab.
Diphenhydramine The serum concentration of Diphenhydramine can be increased when it is combined with Epcoritamab.
Benzocaine The serum concentration of Benzocaine can be increased when it is combined with Epcoritamab.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Tetrodotoxin.
Ambroxol The serum concentration of Ambroxol can be increased when it is combined with Epcoritamab.
Benzyl alcohol The serum concentration of Benzyl alcohol can be increased when it is combined with Epcoritamab.
Capsaicin The serum concentration of Capsaicin can be increased when it is combined with Epcoritamab.
Etidocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Epcoritamab is combined with Quinisocaine.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Epcoritamab.
Calcitriol The serum concentration of Calcitriol can be increased when it is combined with Epcoritamab.
Vitamin E The serum concentration of Vitamin E can be increased when it is combined with Epcoritamab.
Cholecalciferol The serum concentration of Cholecalciferol can be increased when it is combined with Epcoritamab.
Fluvoxamine The serum concentration of Fluvoxamine can be increased when it is combined with Epcoritamab.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Epcoritamab.
Cevimeline The serum concentration of Cevimeline can be increased when it is combined with Epcoritamab.
Bortezomib The serum concentration of Bortezomib can be increased when it is combined with Epcoritamab.
Phentermine The serum concentration of Phentermine can be increased when it is combined with Epcoritamab.
Tramadol The serum concentration of Tramadol can be increased when it is combined with Epcoritamab.
Erythromycin The serum concentration of Erythromycin can be increased when it is combined with Epcoritamab.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Epcoritamab.
Dofetilide The serum concentration of Dofetilide can be increased when it is combined with Epcoritamab.
Azithromycin The serum concentration of Azithromycin can be increased when it is combined with Epcoritamab.
Pantoprazole The serum concentration of Pantoprazole can be increased when it is combined with Epcoritamab.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Epcoritamab.
Eletriptan The serum concentration of Eletriptan can be increased when it is combined with Epcoritamab.
Nelfinavir The serum concentration of Nelfinavir can be increased when it is combined with Epcoritamab.
Indinavir The serum concentration of Indinavir can be increased when it is combined with Epcoritamab.
Lovastatin The serum concentration of Lovastatin can be increased when it is combined with Epcoritamab.
Reboxetine The serum concentration of Reboxetine can be increased when it is combined with Epcoritamab.
Nevirapine The serum concentration of Nevirapine can be increased when it is combined with Epcoritamab.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Epcoritamab.
Ziprasidone The serum concentration of Ziprasidone can be increased when it is combined with Epcoritamab.
Methysergide The serum concentration of Methysergide can be increased when it is combined with Epcoritamab.
Cabergoline The serum concentration of Cabergoline can be increased when it is combined with Epcoritamab.
Dapsone The serum concentration of Dapsone can be increased when it is combined with Epcoritamab.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Epcoritamab.
Medrysone The serum concentration of Medrysone can be increased when it is combined with Epcoritamab.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be increased when it is combined with Epcoritamab.
Isradipine The serum concentration of Isradipine can be increased when it is combined with Epcoritamab.
Theophylline The serum concentration of Theophylline can be increased when it is combined with Epcoritamab.
Disopyramide The serum concentration of Disopyramide can be increased when it is combined with Epcoritamab.
Venlafaxine The serum concentration of Venlafaxine can be increased when it is combined with Epcoritamab.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Epcoritamab.
Etonogestrel The serum concentration of Etonogestrel can be increased when it is combined with Epcoritamab.
Morphine The serum concentration of Morphine can be increased when it is combined with Epcoritamab.
Desogestrel The serum concentration of Desogestrel can be increased when it is combined with Epcoritamab.
Bexarotene The serum concentration of Bexarotene can be increased when it is combined with Epcoritamab.
Vindesine The serum concentration of Vindesine can be increased when it is combined with Epcoritamab.
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Epcoritamab.
Gefitinib The serum concentration of Gefitinib can be increased when it is combined with Epcoritamab.
Codeine The serum concentration of Codeine can be increased when it is combined with Epcoritamab.
Dihydroergotamine The serum concentration of Dihydroergotamine can be increased when it is combined with Epcoritamab.
Amitriptyline The serum concentration of Amitriptyline can be increased when it is combined with Epcoritamab.
Fluorometholone The serum concentration of Fluorometholone can be increased when it is combined with Epcoritamab.
Methadone The serum concentration of Methadone can be increased when it is combined with Epcoritamab.
Terfenadine The serum concentration of Terfenadine can be increased when it is combined with Epcoritamab.
Diltiazem The serum concentration of Diltiazem can be increased when it is combined with Epcoritamab.
Alfuzosin The serum concentration of Alfuzosin can be increased when it is combined with Epcoritamab.
Trimethadione The serum concentration of Trimethadione can be increased when it is combined with Epcoritamab.
Clobazam The serum concentration of Clobazam can be increased when it is combined with Epcoritamab.
Megestrol acetate The serum concentration of Megestrol acetate can be increased when it is combined with Epcoritamab.
Methylergometrine The serum concentration of Methylergometrine can be increased when it is combined with Epcoritamab.
Chlorzoxazone The serum concentration of Chlorzoxazone can be increased when it is combined with Epcoritamab.
Mefloquine The serum concentration of Mefloquine can be increased when it is combined with Epcoritamab.
Sulfadiazine The serum concentration of Sulfadiazine can be increased when it is combined with Epcoritamab.
Vinorelbine The serum concentration of Vinorelbine can be increased when it is combined with Epcoritamab.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Epcoritamab.
Grepafloxacin The serum concentration of Grepafloxacin can be increased when it is combined with Epcoritamab.
Levonorgestrel The serum concentration of Levonorgestrel can be increased when it is combined with Epcoritamab.
Mirtazapine The serum concentration of Mirtazapine can be increased when it is combined with Epcoritamab.
Palonosetron The serum concentration of Palonosetron can be increased when it is combined with Epcoritamab.

Target Protein

B-lymphocyte antigen CD20 MS4A1
T-cell surface glycoprotein CD3 epsilon chain CD3E

Referensi & Sumber

Synthesis reference: Van Der Brink, E., et al. (2019). Humanized or chimeric CD3 antibodies (U.S. Patent No. 10,465,006 B2). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/2d/41/2d/932e259d52f1b3/US10465006.pdf
Artikel (PubMed)
  • PMID: 36548927
    Thieblemont C, Phillips T, Ghesquieres H, Cheah CY, Clausen MR, Cunningham D, Do YR, Feldman T, Gasiorowski R, Jurczak W, Kim TM, Lewis DJ, van der Poel M, Poon ML, Cota Stirner M, Kilavuz N, Chiu C, Chen M, Sacchi M, Elliott B, Ahmadi T, Hutchings M, Lugtenburg PJ: Epcoritamab, a Novel, Subcutaneous CD3xCD20 Bispecific T-Cell-Engaging Antibody, in Relapsed or Refractory Large B-Cell Lymphoma: Dose Expansion in a Phase I/II Trial. J Clin Oncol. 2023 Apr 20;41(12):2238-2247. doi: 10.1200/JCO.22.01725. Epub 2022 Dec 22.
  • PMID: 35928819
    Gonzalez Barca E: Role of Bispecific Antibodies in Relapsed/Refractory Diffuse Large B-Cell Lymphoma in the CART Era. Front Immunol. 2022 Jul 19;13:909008. doi: 10.3389/fimmu.2022.909008. eCollection 2022.
  • PMID: 35996883
    Li T, Hiemstra IH, Chiu C, Oliveri RS, Elliott B, DeMarco D, Salcedo T, Egerod FL, Sasser K, Ahmadi T, Gupta M: Semimechanistic Physiologically-Based Pharmacokinetic/Pharmacodynamic Model Informing Epcoritamab Dose Selection for Patients With B-Cell Lymphomas. Clin Pharmacol Ther. 2022 Nov;112(5):1108-1119. doi: 10.1002/cpt.2729. Epub 2022 Sep 27.

Contoh Produk & Brand

Produk: 6 • International brands: 1
Produk
  • Epkinly
    Injection, solution • 48 mg/0.8mL • Subcutaneous • US • Approved
  • Epkinly
    Injection, solution • 4 mg/0.8mL • Subcutaneous • US • Approved
  • Epkinly
    Solution • 5 mg / mL • Subcutaneous • Canada • Approved
  • Epkinly
    Solution • 60 mg / mL • Subcutaneous • Canada • Approved
  • Tepkinly
    Injection, solution, concentrate • 4 mg/0.8ml • Subcutaneous • EU • Approved
  • Tepkinly
    Injection, solution • 48 mg • Subcutaneous • EU • Approved
International Brands
  • Epkinly — Genmab US, Inc.

Sekuens Gen/Protein (FASTA)

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