Peringatan Keamanan

Data regarding overdose of tafasitamab are unavailable. Symptoms of overdosage are likely to be consistent with its adverse effect profile, and may therefore involve significant infusion-related reactions and/or myelosuppression.L15292

Tafasitamab

DB15044

biotech approved investigational

Deskripsi

Tafasitamab is a humanized, CD19-directed cytolytic monoclonal antibody intended for the treatment of B-cell malignancies.L15302 It is produced using recombinant DNA technology in Chinese hamster ovary cells, and contains an IgG1/2 hybrid Fc-domain which has been modified with 2 amino acid substitutions to enhance its cytotoxicity relative to non-engineered anti-CD19 antibodies.L15292,A191829

The CD19 surface protein is highly expressed on the surface of B-cells, where it appears to play a role in enhancing B-cell receptor signaling.L15302 Its relative ubiquity across different stages of B-cell development, including pre-B and mature B-lymphocytes,L15292 as well as its presence in several B-cell malignancies (e.g. chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), diffuse large B-cell lymphoma (DLBCL))L15302 has made it a desirable target in the treatment these B-cell malignancies. Tafasatimab is designed to bind to and block the activity of the CD19 surface antigen, which ultimately results in the lysis of B-cells (both healthy and malignant).L15292

Having previously received Breakthrough Therapy, Fast Track, and Orphan designations from the FDA,A191829 tafasatimab-cxix (Monjuvi®) received an accelerated approval on July 31st, 2020, for the treatment of relapsed or refractory DLBCL in adult patients who cannot receive autologous stem cell transplants.L15307 It must be used in combination with lenalidomide, as this combination results in greater efficacy as compared to either agent alone.L15292

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of tafasitamab is approximately 17 days.[L15292]
Volume Distribusi The total volume of distribution of tafasitamab following intravenous injection is approximately 9.3 L.[L15292]
Klirens (Clearance) The clearance of tafasitamab is approximately 0.41 L/day.[L15292]

Absorpsi

Following intravenous administration of tafasitamab 12 mg/kg on Days 1, 8, 15, and 22 in cycle(s) 1-3 (with an additional dose on Day 4 of cycle 1), mean trough concentrations were 179 (± 53) ?g/mL. From cycle 4 onwards, which involve the administration of tafasitamab 12 mg/kg on Days 1 and 15, mean trough concentrations were 153 (± 68) ?g/mL.L15292 The overall maximum tafasitamab serum concentrations reached were 483 (± 109) ?g/mL.L15292

Metabolisme

The biotransformation of tafasitamab has not been elucidated. Most monoclonal antibodies undergo intracellular catabolism via lysosomal degradation to smaller amino acids and peptides.A19126,A216712

Rute Eliminasi

Monoclonal antibodies are typically eliminated via uptake into cells and subsequent catabolism via lysosomal degradation. Due to their large size, they are only eliminated renally under pathologic conditions.A216712

Interaksi Obat

411 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Tafasitamab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Tafasitamab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Tafasitamab.
Estrone Estrone may increase the thrombogenic activities of Tafasitamab.
Estradiol Estradiol may increase the thrombogenic activities of Tafasitamab.
Dienestrol Dienestrol may increase the thrombogenic activities of Tafasitamab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Tafasitamab.
Mestranol Mestranol may increase the thrombogenic activities of Tafasitamab.
Estriol Estriol may increase the thrombogenic activities of Tafasitamab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Tafasitamab.
Quinestrol Quinestrol may increase the thrombogenic activities of Tafasitamab.
Hexestrol Hexestrol may increase the thrombogenic activities of Tafasitamab.
Tibolone Tibolone may increase the thrombogenic activities of Tafasitamab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Tafasitamab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Tafasitamab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Tafasitamab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Tafasitamab.
Zeranol Zeranol may increase the thrombogenic activities of Tafasitamab.
Equol Equol may increase the thrombogenic activities of Tafasitamab.
Promestriene Promestriene may increase the thrombogenic activities of Tafasitamab.
Methallenestril Methallenestril may increase the thrombogenic activities of Tafasitamab.
Epimestrol Epimestrol may increase the thrombogenic activities of Tafasitamab.
Moxestrol Moxestrol may increase the thrombogenic activities of Tafasitamab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Tafasitamab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Tafasitamab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Tafasitamab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Tafasitamab.
Biochanin A Biochanin A may increase the thrombogenic activities of Tafasitamab.
Formononetin Formononetin may increase the thrombogenic activities of Tafasitamab.
Estetrol Estetrol may increase the thrombogenic activities of Tafasitamab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Tafasitamab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Tafasitamab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Tafasitamab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Tafasitamab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Tafasitamab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Tafasitamab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Tafasitamab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Tafasitamab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Tafasitamab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Tafasitamab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Tafasitamab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Tafasitamab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Tafasitamab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Tafasitamab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Tafasitamab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Tafasitamab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Tafasitamab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Tafasitamab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Tafasitamab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Tafasitamab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Tafasitamab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Tafasitamab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Tafasitamab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Tafasitamab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Tafasitamab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Tafasitamab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Tafasitamab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Tafasitamab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Tafasitamab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Tafasitamab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Tafasitamab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Tafasitamab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Tafasitamab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Tafasitamab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Tafasitamab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Tafasitamab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Tafasitamab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Tafasitamab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Tafasitamab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Tafasitamab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Tafasitamab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Tafasitamab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Tafasitamab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Tafasitamab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Tafasitamab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Tafasitamab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Tafasitamab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Tafasitamab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Tafasitamab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Tafasitamab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Tafasitamab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Tafasitamab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Tafasitamab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Tafasitamab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Tafasitamab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Tafasitamab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Tafasitamab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Tafasitamab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Tafasitamab.
Stamulumab The risk or severity of adverse effects can be increased when MYO-029 is combined with Tafasitamab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Tafasitamab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Tafasitamab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Tafasitamab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Tafasitamab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Tafasitamab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Tafasitamab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Tafasitamab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Tafasitamab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Tafasitamab.
Lumiliximab The risk or severity of adverse effects can be increased when Lumiliximab is combined with Tafasitamab.

Target Protein

B-lymphocyte antigen CD19 CD19

Referensi & Sumber

Synthesis reference: ??? ???, ????? ???, ?? ???, ??? ?????, ?? ???. Anti-CD19 antibody preparation. South Korean Patent KR20190021373A. Published March 5, 2019.
Artikel (PubMed)
  • PMID: 31847708
    Kaplon H, Muralidharan M, Schneider Z, Reichert JM: Antibodies to watch in 2020. MAbs. 2020 Jan-Dec;12(1):1703531. doi: 10.1080/19420862.2019.1703531.
  • PMID: 28653357
    Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29.
  • PMID: 20608753
    Keizer RJ, Huitema AD, Schellens JH, Beijnen JH: Clinical pharmacokinetics of therapeutic monoclonal antibodies. Clin Pharmacokinet. 2010 Aug;49(8):493-507. doi: 10.2165/11531280-000000000-00000.
  • PMID: 32052309
    Temrikar ZH, Suryawanshi S, Meibohm B: Pharmacokinetics and Clinical Pharmacology of Monoclonal Antibodies in Pediatric Patients. Paediatr Drugs. 2020 Apr;22(2):199-216. doi: 10.1007/s40272-020-00382-7.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Minjuvi
    Injection, powder, for solution • 200 mg • Intravenous • EU • Approved
  • Minjuvi
    Powder, for solution • 200 mg / vial • Intravenous • Canada • Approved
  • Monjuvi
    Injection, powder, lyophilized, for solution • 200 mg/5mL • Intravenous • US • Approved
  • Monjuvi
    Injection, powder, lyophilized, for solution • 200 mg/5mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

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