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Identification
NamePertuzumab
Accession NumberDB06366
TypeBiotech
GroupsApproved
DescriptionPertuzumab 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. FDA approved June 8, 2012.
Protein structureDb06366
Related Articles
Protein chemical formulaNot Available
Protein average weight148000.0 Da
Sequences
>Amino acid sequence for pertuzumab light chain 
DIQMTQSPSSLSASVGDRVTITCKASQDVSIGVAWYQQKPGKAPKLLIYSASYRYTGVPS
RFSGSGSGTDFTLTISSLQPEDFATYYCQQYYIYPYTFGQGTKVEIKRTVAAPSVFIFPP
SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT
LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
>Amino acid sequence for pertuzumab heavy chain 
EVQLVESGGGLVQPGGSLRLSCAASGFTFTDYTMDWVRQAPGKGLEWVADVNPNSGGSIY
NQRFKGRFTLSVDRSKNTLYLQMNSLRAEDTAVYYCARNLGPSFYFDYWGQGTLVTVSSA
STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP
SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS
TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM
TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ
QGNVFSCSVMHEALHNHYTQKSLSLSPG
Download FASTA Format
Synonyms
2C4 Antibody
MOAB 2C4
Monoclonal Antibody 2C4
Omnitarg
rhuMAb-2C4
External Identifiers
  • R1273
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Perjetasolution420 mgintravenousHoffmann La Roche Limited2013-05-08Not applicableCanada
Perjetainjection, solution, concentrate30 mg/mLintravenousGenentech, Inc.2012-06-08Not applicableUs
PerjetaConcentrate for solution for infusion420 mgIntravenous useRoche Registration Limited  2013-03-04Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Perjeta-herceptinHoffmann La Roche Limited
SaltsNot Available
Categories
UNIIK16AIQ8CTM
CAS number380610-27-5
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationPertuzumab 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.
PharmacodynamicsNot Available
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.
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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 distribution

5.12 L

Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life18 days
Clearance

0.24 L/day

ToxicityThe most common adverse reactions (> 30%) with PERJETA in combination with trastuzumab and docetaxel were diarrhea, alopecia, neutropenia, nausea, fatigue, rash, and peripheral neuropathy.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Concentrate for solution for infusionIntravenous use420 mg
Injection, solution, concentrateintravenous30 mg/mL
Solutionintravenous420 mg
Solution; kit; powder for solutionintravenous
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2376596 No2009-10-062020-06-23Canada
CA2579861 No2012-12-182025-10-19Canada
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Pertuzumab protein sequence [Link]
External Links
ATC CodesL01XC13
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (362 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Pertuzumab.
BelimumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Belimumab.
BevacizumabBevacizumab may increase the cardiotoxic activities of Pertuzumab.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Pertuzumab.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Pertuzumab.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Pertuzumab.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Pertuzumab.
DigoxinDigoxin may decrease the cardiotoxic activities of Pertuzumab.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Pertuzumab.
OuabainOuabain may decrease the cardiotoxic activities of Pertuzumab.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Pertuzumab.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Pertuzumab.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antibody
General Function:
Transmembrane signaling receptor activity
Specific Function:
Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-...
Gene Name:
ERBB2
Uniprot ID:
P04626
Molecular Weight:
137909.27 Da
References
  1. Franklin MC, Carey KD, Vajdos FF, Leahy DJ, de Vos AM, Sliwkowski MX: Insights into ErbB signaling from the structure of the ErbB2-pertuzumab complex. Cancer Cell. 2004 Apr;5(4):317-28. [PubMed:15093539 ]
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Drug created on March 19, 2008 10:27 / Updated on August 17, 2016 12:24