Peringatan Keamanan

The FDA label includes a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.

Trastuzumab emtansine

DB05773

biotech approved investigational

Deskripsi

Trastuzumab emtansine, formerly called Trastuzumab-DM1 (T-DM1) is a first-in-class HER2 antibody drug conjugate (ADC) comprised of Genentech's trastuzumab antibody linked to ImmunoGen's cell-killing agent, DM1. T-DM1 combines two strategies-- anti-HER2 activity and targeted intracellular delivery of the potent anti-microtubule agent, DM1 (a maytansine derivative)--to produce cell cycle arrest and apoptosis. Trastuzumab emtansine is marketed under the brand name Kadcyla and is indicated for use in HER2-positive, metastatic breast cancer patients who have already used taxane and/or trastuzumab for metastatic disease or had their cancer recur within 6 months of adjuvant treatment. The FDA label has two precautions. First that trastuzumab emtansine and trastuzumab cannot be interchanged. Second that there is a black box warning of serious side effects such as hepatotoxicity, embryo-fetal toxicity, and cardiac toxicity.

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) Trastuzumab emtansine has a long half life of about 4 days.
Volume Distribusi The volume of distribution of trastuzumab emtansine is about 3.13 L.
Klirens (Clearance) After IV infusion, trastuzumab emtansine has a clearance of 0.68 L/day.

Absorpsi

The absorption/ bioavailability should be close to 100% since trastuzumab emtansine is administered IV.

Metabolisme

Trastuzumab emtansine undergoes lysosomal degradation to MCC-DM1, Lys-MCC-DM1, and DM1. All of these products are detected at low levels in the plasma. DM1 undergoes further degradation by CYP3A4 and CYP3A5, but DM1 does not induce or inhibit any of the CYP450 enzymes.

Rute Eliminasi

The route of elimination has not yet been fully elucidated.

Interaksi Makanan

1 Data
  • 1. Avoid grapefruit products. Trastuzumab emtansine undergoes metabolism through CYP3A4 therefore coadministration with grapefruit, a CYP3A4 inhibitor, may increase serum levels of trastuzumab emtansine.

Interaksi Obat

1368 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Trastuzumab emtansine.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Trastuzumab emtansine.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Trastuzumab emtansine.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Trastuzumab emtansine.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Trastuzumab emtansine.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Trastuzumab emtansine.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Trastuzumab emtansine.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Trastuzumab emtansine.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Trastuzumab emtansine.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Trastuzumab emtansine.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Trastuzumab emtansine.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Trastuzumab emtansine.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Trastuzumab emtansine.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Trastuzumab emtansine.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Trastuzumab emtansine.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Trastuzumab emtansine.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Trastuzumab emtansine.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Trastuzumab emtansine.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Trastuzumab emtansine.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Trastuzumab emtansine.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Trastuzumab emtansine.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Trastuzumab emtansine.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Trastuzumab emtansine.
Cladribine Trastuzumab emtansine may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Trastuzumab emtansine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Trastuzumab emtansine.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Trastuzumab emtansine.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Trastuzumab emtansine.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Trastuzumab emtansine.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Trastuzumab emtansine.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Trastuzumab emtansine.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Trastuzumab emtansine.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Trastuzumab emtansine.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Trastuzumab emtansine.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Trastuzumab emtansine.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Trastuzumab emtansine.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Trastuzumab emtansine.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Trastuzumab emtansine.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Trastuzumab emtansine.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Trastuzumab emtansine.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Trastuzumab emtansine.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Trastuzumab emtansine.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Trastuzumab emtansine.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Trastuzumab emtansine.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Trastuzumab emtansine.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Trastuzumab emtansine.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Trastuzumab emtansine.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Trastuzumab emtansine.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Trastuzumab emtansine.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Trastuzumab emtansine.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Trastuzumab emtansine.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Trastuzumab emtansine.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Trastuzumab emtansine.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Trastuzumab emtansine.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Trastuzumab emtansine.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Trastuzumab emtansine.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Trastuzumab emtansine.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Trastuzumab emtansine.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Trastuzumab emtansine.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Trastuzumab emtansine.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Trastuzumab emtansine.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Trastuzumab emtansine.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Trastuzumab emtansine.
Thalidomide The metabolism of Trastuzumab emtansine can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Trastuzumab emtansine.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Trastuzumab emtansine.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Trastuzumab emtansine.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Trastuzumab emtansine.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Trastuzumab emtansine.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Trastuzumab emtansine.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Trastuzumab emtansine.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Trastuzumab emtansine.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Trastuzumab emtansine.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Trastuzumab emtansine.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Trastuzumab emtansine.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Trastuzumab emtansine.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Trastuzumab emtansine.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Trastuzumab emtansine.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Trastuzumab emtansine.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Trastuzumab emtansine.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Trastuzumab emtansine.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Trastuzumab emtansine.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Trastuzumab emtansine.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Trastuzumab emtansine.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Trastuzumab emtansine.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Trastuzumab emtansine.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Trastuzumab emtansine.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Trastuzumab emtansine.
Mepolizumab The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belimumab.
Teriflunomide The risk or severity of liver damage can be increased when Trastuzumab emtansine is combined with Teriflunomide.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Vedolizumab.

Target Protein

Receptor tyrosine-protein kinase erbB-2 ERBB2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19010901
    Lewis Phillips GD, Li G, Dugger DL, Crocker LM, Parsons KL, Mai E, Blattler WA, Lambert JM, Chari RV, Lutz RJ, Wong WL, Jacobson FS, Koeppen H, Schwall RH, Kenkare-Mitra SR, Spencer SD, Sliwkowski MX: Targeting HER2-positive breast cancer with trastuzumab-DM1, an antibody-cytotoxic drug conjugate. Cancer Res. 2008 Nov 15;68(22):9280-90. doi: 10.1158/0008-5472.CAN-08-1776.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Kadcyla
    Powder, for solution • 160 mg / vial • Intravenous • Canada • Approved
  • Kadcyla
    Powder, for solution • 100 mg / vial • Intravenous • Canada • Approved
  • Kadcyla
    Injection, powder, lyophilized, for solution • 20 mg/1mL • Intravenous • US • Approved
  • Kadcyla
    Injection, powder, lyophilized, for solution • 20 mg/1mL • Intravenous • US • Approved
  • Kadcyla
    Injection, powder, for solution • 100 mg • Intravenous • EU • Approved
  • Kadcyla
    Injection, powder, for solution • 160 mg • Intravenous • EU • Approved

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