==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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Primary information
ThPP IDTh1121
Therapeutic Peptide/Protein NamePertuzumab
Sequencelight chain DIQMTQSPSSLSASVGDRVTITCKASQDVSIGVAWYQQ view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight148000
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life18 days
DescriptionRecombinant, humanized monoclonal antibody that targets the extracellular dimerization domain (Subdomain II) of the human epidermal growth factor receptor 2 protein (HER2). Two heavy chains and two lights chains are composed of 448 and 214 residues respectively. FDA approved June 8, 2012.
Indication/DiseasePertuzumab is indicated for use in combination with trastuzumab and docetaxel for the treatment of patients with HER2-positive metastatic breast cancer who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease.
PharmacodynamicsN.A.
Mechanism of ActionPertuzumab is a humanized monoclonal antibody designed to bind to the HER2 receptor and inhibit the ability of HER2 to interact with other HER family members (HER1, HER2, HER3, and HER4) on the surface of cancer cells. The HER signaling pathway plays a role in the formation and growth of numerous cancers, and previous clinical trials of pertuzumab in a single agent setting had suggested clinical activity - including stable disease - in heavily pretreated patients with advanced ovarian and breast cancers.
ToxicityThe most common adverse reactions (> 30%) with PERJETA in combination with trastuzumab and docetaxel were diarrhea, alopecia, neutropenia, nausea, fatigue, rash, and peripheral neuropathy.
MetabolismN.A.
AbsorptionWhen an initial dose of 840 mg followed by a maintenance dose of 420 mg every three weeks thereafter is administered, steady-state concentrations were achieved on the first maintenance dose.
Volume of Distribution5.12 L
Clearance0.24 L/day
CategoriesMonoclonal antibodies
Patents NumberCA2376596
Date of Issue07/10/13
Date of Expiry24/06/24
Drug InteractionN.A.
TargetReceptor tyrosine-protein kinase erbB-2
Information of corresponding available drug in the market
Brand NamePerjeta
CompanyGenentech
Brand DiscriptionPertuzumab is a recombinant humanized monoclonal antibody that targets the extracellular dimerization domain (Subdomain II) of the human epidermal growth factor receptor 2 protein (HER2). Pertuzumab is produced by recombinant DNA technology in a mammalian cell (Chinese Hamster Ovary) culture containing the antibiotic, gentamicin. Gentamicin is not detectable in the final product. Pertuzumab has an approximate molecular weight of 148 kDa.
Prescribed forNeoadjuvant Treatment of Breast Cancer, Metastatic Breast Cancer (MBC),
Chemical NameN.A.
FormulationEach single use vial contains 420 mg of pertuzumab at a concentration of 30 mg/mL in 20 mM L-histidine acetate (pH 6.0), 120 mM sucrose and 0.02% polysorbate 20
Physcial AppearnceSterile, clear to slightly opalescent, colorless to pale brown liquid
Route of AdministrationIntravenous infusion
Recommended DosageThe initial dose of PERJETA is 840 mg administered as a 60-minute Intravenous infusion, followed every 3 weeks by a dose of 420 mg administered as an Intravenous infusion over 30 to 60 minutes. When administered with PERJETA, the recommended initial dose of trastuzumab is 8 mg/kg administered as a 90-minute Intravenous infusion, followed every 3 weeks by a dose of 6 mg/kg administered as an Intravenous infusion over 30 to 90 minutes.PERJETA, trastuzumab, and docetaxel should be administered sequentially. PERJETA and trastuzumab can be given in any order. Docetaxel should be administered after PERJETA and trastuzumab. An observation period of 30 to 60 minutes is recommended after each PERJETA infusion and before commencement of any subsequent infusion of trastuzumab.
ContraindicationN.A.
Side EffectsEmbryo-Fetal Toxicity , Left Ventricular Dysfunction , Infusion-Related Reactions, Hypersensitivity Reactions.
Useful Linkhttp://www.rxlist.com/perjeta-drug.htm http://www.gene.com/download/pdf/perjeta_prescribing.pdf
PubMed ID25572781, 25547504, 25542663, 25532690, 25494663
3-D StructureTh1121 Light chainor (Download), Th1121 Heavy chain (View) or (Download)