Peringatan Keamanan

There are no data regarding overdose of pertuzumab. Single doses higher than 25 mg/kg have not been tested.L14747 Symptoms of overdose are likely to be consistent with pertuzumab's adverse effect profile, and may therefore involve significant diarrhea, alopecia, neutropenia, nausea, fatigue, rash, and/or peripheral neuropathy.L14642 Pertuzumab has been associated with the development of left ventricular dysfunction (i.e. cardiotoxicity) that may be exacerbated in instances of overdose.L14642

Pertuzumab

DB06366

biotech approved

Deskripsi

Pertuzumab is a recombinant humanized monoclonal antibody that targets the extracellular dimerization domain (subdomain II) of the human epidermal growth factor receptor 2 protein (HER2). It consists of two heavy chains and two lights chains that have 448 and 214 residues respectively. It was first approved by the FDA in 2012 for use with docetaxel and another HER2-targeted monoclonal antibody, trastuzumab, in the treatment of metastatic HER2-positive breast cancer. Its indicated conditions have since expanded to include use as both a neoadjuvant therapy and an adjuvant therapy in the treatment of HER2-positive breast cancers at high risk of recurrence.L14642,L14772

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median half-life of pertuzumab was determined to be 18 days based on a population pharmacokinetic analysis.[L14642]
Volume Distribusi The average steady-state volume of distribution following intravenous administration is 3.53 - 7.5 L.[L14747]
Klirens (Clearance) The median clearance of pertuzumab was determined to be 0.24 L/day based on a population pharmacokinetic analysis.[L14642]

Absorpsi

Intravenously administered pertuzumab, given as a loading dose of 840mg followed by a maintenance dose of 420mg every 3 weeks, reaches steady-state concentration following the first maintenance dose.L14747 In its subcutaneous formulation, in combination with hylauronidase, the absolute bioavailability of pertuzumab is approximately 0.7 and the median Tmax is 4 days.L14531 This subcutaneous formulation leverages the benefits of co-administration with hyaluronidase - this enzyme breaks down hylauronic acid, thereby decreasing the viscosity of the extracellular matrix (ECM) and allowing for greater bioavailability with subcutaneous administration.L14531

Metabolisme

The metabolism of pertuzumab has not been studied directly. Monoclonal antibodies are typically subject to catabolism to smaller peptides and proteins prior to elimination.L14747

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

463 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Pertuzumab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Pertuzumab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Pertuzumab.
Estrone Estrone may increase the thrombogenic activities of Pertuzumab.
Estradiol Estradiol may increase the thrombogenic activities of Pertuzumab.
Dienestrol Dienestrol may increase the thrombogenic activities of Pertuzumab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Pertuzumab.
Mestranol Mestranol may increase the thrombogenic activities of Pertuzumab.
Estriol Estriol may increase the thrombogenic activities of Pertuzumab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Pertuzumab.
Quinestrol Quinestrol may increase the thrombogenic activities of Pertuzumab.
Hexestrol Hexestrol may increase the thrombogenic activities of Pertuzumab.
Tibolone Tibolone may increase the thrombogenic activities of Pertuzumab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Pertuzumab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Pertuzumab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Pertuzumab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Pertuzumab.
Zeranol Zeranol may increase the thrombogenic activities of Pertuzumab.
Equol Equol may increase the thrombogenic activities of Pertuzumab.
Promestriene Promestriene may increase the thrombogenic activities of Pertuzumab.
Methallenestril Methallenestril may increase the thrombogenic activities of Pertuzumab.
Epimestrol Epimestrol may increase the thrombogenic activities of Pertuzumab.
Moxestrol Moxestrol may increase the thrombogenic activities of Pertuzumab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Pertuzumab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Pertuzumab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Pertuzumab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Pertuzumab.
Biochanin A Biochanin A may increase the thrombogenic activities of Pertuzumab.
Formononetin Formononetin may increase the thrombogenic activities of Pertuzumab.
Estetrol Estetrol may increase the thrombogenic activities of Pertuzumab.
Digoxin Digoxin may decrease the cardiotoxic activities of Pertuzumab.
Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Pertuzumab.
Deslanoside Deslanoside may decrease the cardiotoxic activities of Pertuzumab.
Ouabain Ouabain may decrease the cardiotoxic activities of Pertuzumab.
Digitoxin Digitoxin may decrease the cardiotoxic activities of Pertuzumab.
Oleandrin Oleandrin may decrease the cardiotoxic activities of Pertuzumab.
Cymarin Cymarin may decrease the cardiotoxic activities of Pertuzumab.
Proscillaridin Proscillaridin may decrease the cardiotoxic activities of Pertuzumab.
Metildigoxin Metildigoxin may decrease the cardiotoxic activities of Pertuzumab.
Lanatoside C Lanatoside C may decrease the cardiotoxic activities of Pertuzumab.
Gitoformate Gitoformate may decrease the cardiotoxic activities of Pertuzumab.
Acetyldigoxin Acetyldigoxin may decrease the cardiotoxic activities of Pertuzumab.
Peruvoside Peruvoside may decrease the cardiotoxic activities of Pertuzumab.
Bevacizumab The risk or severity of cardiotoxicity can be increased when Bevacizumab is combined with Pertuzumab.
Peginterferon alfa-2a The risk or severity of cardiotoxicity can be increased when Peginterferon alfa-2a is combined with Pertuzumab.
Bortezomib The risk or severity of cardiotoxicity can be increased when Bortezomib is combined with Pertuzumab.
Cladribine The risk or severity of cardiotoxicity can be increased when Cladribine is combined with Pertuzumab.
Carmustine The risk or severity of cardiotoxicity can be increased when Carmustine is combined with Pertuzumab.
Amsacrine The risk or severity of cardiotoxicity can be increased when Amsacrine is combined with Pertuzumab.
Bleomycin The risk or severity of cardiotoxicity can be increased when Bleomycin is combined with Pertuzumab.
Mitomycin The risk or severity of cardiotoxicity can be increased when Mitomycin is combined with Pertuzumab.
Vindesine The risk or severity of cardiotoxicity can be increased when Vindesine is combined with Pertuzumab.
Vinorelbine The risk or severity of cardiotoxicity can be increased when Vinorelbine is combined with Pertuzumab.
Teniposide The risk or severity of cardiotoxicity can be increased when Teniposide is combined with Pertuzumab.
Epirubicin The risk or severity of cardiotoxicity can be increased when Epirubicin is combined with Pertuzumab.
Cisplatin The risk or severity of cardiotoxicity can be increased when Cisplatin is combined with Pertuzumab.
Cyclophosphamide The risk or severity of cardiotoxicity can be increased when Cyclophosphamide is combined with Pertuzumab.
Vincristine The risk or severity of cardiotoxicity can be increased when Vincristine is combined with Pertuzumab.
Fluorouracil The risk or severity of cardiotoxicity can be increased when Fluorouracil is combined with Pertuzumab.
Pentostatin The risk or severity of cardiotoxicity can be increased when Pentostatin is combined with Pertuzumab.
Methotrexate The risk or severity of cardiotoxicity can be increased when Methotrexate is combined with Pertuzumab.
Vinblastine The risk or severity of cardiotoxicity can be increased when Vinblastine is combined with Pertuzumab.
Imatinib The risk or severity of cardiotoxicity can be increased when Imatinib is combined with Pertuzumab.
Tamoxifen The risk or severity of cardiotoxicity can be increased when Tamoxifen is combined with Pertuzumab.
Daunorubicin The risk or severity of cardiotoxicity can be increased when Daunorubicin is combined with Pertuzumab.
Tretinoin The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Pertuzumab.
Etoposide The risk or severity of cardiotoxicity can be increased when Etoposide is combined with Pertuzumab.
Mechlorethamine The risk or severity of cardiotoxicity can be increased when Mechlorethamine is combined with Pertuzumab.
Doxorubicin The risk or severity of cardiotoxicity can be increased when Doxorubicin is combined with Pertuzumab.
Busulfan The risk or severity of cardiotoxicity can be increased when Busulfan is combined with Pertuzumab.
Thalidomide The risk or severity of cardiotoxicity can be increased when Thalidomide is combined with Pertuzumab.
Fludarabine The risk or severity of cardiotoxicity can be increased when Fludarabine is combined with Pertuzumab.
Capecitabine The risk or severity of cardiotoxicity can be increased when Capecitabine is combined with Pertuzumab.
Arsenic trioxide The risk or severity of cardiotoxicity can be increased when Arsenic trioxide is combined with Pertuzumab.
Idarubicin The risk or severity of cardiotoxicity can be increased when Idarubicin is combined with Pertuzumab.
Ifosfamide The risk or severity of cardiotoxicity can be increased when Ifosfamide is combined with Pertuzumab.
Mitoxantrone The risk or severity of cardiotoxicity can be increased when Mitoxantrone is combined with Pertuzumab.
Anastrozole The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Pertuzumab.
Paclitaxel The risk or severity of cardiotoxicity can be increased when Paclitaxel is combined with Pertuzumab.
Docetaxel The risk or severity of cardiotoxicity can be increased when Docetaxel is combined with Pertuzumab.
Aldoxorubicin The risk or severity of cardiotoxicity can be increased when Aldoxorubicin is combined with Pertuzumab.
Paclitaxel trevatide The risk or severity of cardiotoxicity can be increased when Paclitaxel trevatide is combined with Pertuzumab.
Cabazitaxel The risk or severity of cardiotoxicity can be increased when Pertuzumab is combined with Cabazitaxel.
Paclitaxel poliglumex The risk or severity of cardiotoxicity can be increased when Pertuzumab is combined with Paclitaxel poliglumex.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Pertuzumab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Pertuzumab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Pertuzumab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Pertuzumab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Pertuzumab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Pertuzumab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Pertuzumab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Pertuzumab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Pertuzumab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Pertuzumab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Pertuzumab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Pertuzumab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Pertuzumab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Pertuzumab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pertuzumab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Pertuzumab.

Target Protein

Receptor tyrosine-protein kinase erbB-2 ERBB2

Referensi & Sumber

Synthesis reference: Adams CW, Allison DE, Flagella K, Presta L, Clarke J, Dybdal N, McKeever K, Sliwkowski MX: Humanization of a recombinant monoclonal antibody to produce a therapeutic HER dimerization inhibitor, pertuzumab. Cancer Immunol Immunother. 2006 Jun;55(6):717-27. doi: 10.1007/s00262-005-0058-x. Epub 2005 Sep 3.
Artikel (PubMed)
  • PMID: 16151804
    Adams CW, Allison DE, Flagella K, Presta L, Clarke J, Dybdal N, McKeever K, Sliwkowski MX: Humanization of a recombinant monoclonal antibody to produce a therapeutic HER dimerization inhibitor, pertuzumab. Cancer Immunol Immunother. 2006 Jun;55(6):717-27. doi: 10.1007/s00262-005-0058-x. Epub 2005 Sep 3.
  • PMID: 23918291
    Malenfant SJ, Eckmann KR, Barnett CM: Pertuzumab: a new targeted therapy for HER2-positive metastatic breast cancer. Pharmacotherapy. 2014 Jan;34(1):60-71. doi: 10.1002/phar.1338. Epub 2013 Aug 5.

Contoh Produk & Brand

Produk: 10 • International brands: 2
Produk
  • Perjeta
    Solution • 420 mg / 14 mL • Intravenous • Canada • Approved
  • Perjeta
    Injection, solution, concentrate • 420 mg • Intravenous • EU • Approved
  • Perjeta
    Injection, solution, concentrate • 30 mg/1mL • Intravenous • US • Approved
  • Perjeta-herceptin
    Kit; Powder, for solution; Solution • - • Intravenous • Canada • Approved
  • Phesgo
    Solution • - • Subcutaneous • Canada • Approved
  • Phesgo
    Solution • - • Subcutaneous • Canada • Approved
  • Phesgo
    Injection, solution • - • Subcutaneous • EU • Approved
  • Phesgo
    Injection, solution • - • Subcutaneous • EU • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Omnitarg
  • Perjeta

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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