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Identification
NamePertuzumab
Accession NumberDB06366
TypeBiotech
GroupsApproved
Description

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. FDA approved June 8, 2012.

Protein structureDb06366
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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Perjetainjection, solution, concentrate30 mg/mLintravenousGenentech, Inc.2012-06-08Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Perjetasolution420 mgintravenousHoffmann La Roche Limited2013-05-08Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Perjeta-herceptinHoffmann La Roche Limited
SaltsNot Available
Categories
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.
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
Injection, solution, concentrateintravenous30 mg/mL
Solutionintravenous420 mg
Solution; kit; powder for solutionintravenous
PricesNot Available
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada23765962009-10-062020-06-23
Canada25798612012-12-182025-10-19
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Protein sequence Link
  2. FDA label
External Links
ATC CodesL01XC13
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (362 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
BelimumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Belimumab.
Food InteractionsNot Available

Targets

1. Receptor tyrosine-protein kinase erbB-2

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: antibody

Components

Name UniProt ID Details
Receptor tyrosine-protein kinase erbB-2 P04626 Details

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

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Drug created on March 19, 2008 10:27 / Updated on January 14, 2016 21:12