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
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 IDs R1273
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PerjetaSolution420 mgIntravenousHoffmann La Roche2013-05-08Not applicableCanada
PerjetaInjection, solution, concentrate30 mg/mLIntravenousGenentech, Inc.2012-06-08Not applicableUs
PerjetaInjection, solution, concentrate420 mgIntravenousRoche Registration Limited2013-03-04Not 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
Categories
UNIIK16AIQ8CTM
CAS number380610-27-5
Pharmacology
Indication

Pertuzumab 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.

Structured Indications
PharmacodynamicsNot Available
Mechanism of action

Pertuzumab 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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Receptor tyrosine-protein kinase erbB-2Proteinyes
antibody
HumanP04626 details
Related Articles
Absorption

When 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 life

18 days

Clearance

0.24 L/day

Toxicity

The 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
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Pertuzumab.Approved
BelimumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Belimumab.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Pertuzumab.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Pertuzumab.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Pertuzumab.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Pertuzumab.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Pertuzumab.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Pertuzumab.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Pertuzumab.Approved, Investigational
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Pertuzumab.Investigational
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Pertuzumab.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Pertuzumab.Investigational
OleandrinAnvirzel may decrease the cardiotoxic activities of Pertuzumab.Experimental
OuabainOuabain may decrease the cardiotoxic activities of Pertuzumab.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Pertuzumab.Approved, Vet Approved
RindopepimutThe therapeutic efficacy of CDX-110 can be decreased when used in combination with Pertuzumab.Investigational
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Pertuzumab.Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Pertuzumab.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Pertuzumab protein sequence [Link]
External Links
ATC CodesL01XC13 — Pertuzumab
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (362 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingDiagnosticNeoplasms, Breast1
1Active Not RecruitingTreatmentHER2-positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1CompletedTreatmentCancer, Breast2
1CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
1CompletedTreatmentTumors, Solid2
1RecruitingTreatmentAsymptomatic or Low Symptomatic Brain Metastasis in Breast Cancer / HER2 Positive Untreated Metastatic Breast Cancer1
1RecruitingTreatmentCancer, Breast1
1RecruitingTreatmentHER2 Positive Breast Cancers / HER2-negative Metastatic Breast Cancer / HER2-positive Metastatic Breast Cancer / Locally Advanced or Early Breast Cancer1
1RecruitingTreatmentMetastatic Breast Cancer (MBC) / Recurrent Breast Cancer1
1RecruitingTreatmentStage I Breast Carcinoma1
1RecruitingTreatmentTumors, Solid1
1, 2Active Not RecruitingTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentCancer, Breast / DCIS Breast Cancer1
1, 2CompletedTreatmentAdenocarcinoma of the Colon / Adenocarcinoma of the Rectum / Recurrent Colon Cancer / Recurrent Rectal Cancer / Stage III Colon Cancer / Stage III Rectal Cancer / Stage IV Colon Cancer / Stage IV Rectal Cancer1
1, 2CompletedTreatmentMetastatic Breast Cancer (MBC)2
1, 2CompletedTreatmentOesophageal Carcinoma1
1, 2Not Yet RecruitingTreatmentMalignant Neoplasm of Breast1
1, 2RecruitingTreatmentHER2/Neu Positive / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
1, 2TerminatedTreatmentCancer, Breast1
2Active Not RecruitingNot AvailableNeoplasms, Breast1
2Active Not RecruitingBasic ScienceStage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2Active Not RecruitingTreatmentCancer, Breast3
2Active Not RecruitingTreatmentElderly Metastatic Breast Cancer Population1
2Active Not RecruitingTreatmentHER-2 Positive Breast Cancer1
2Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
2Active Not RecruitingTreatmentMalignant Tumor of the Breast / Neoplasms, Breast1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentMetastatic HER2-Positive Breast Cancer1
2CompletedTreatmentCancer, Breast6
2CompletedTreatmentCancer, Ovarian2
2CompletedTreatmentCancer, Ovarian / Fallopian Tube Cancer / Peritoneal Cancer1
2CompletedTreatmentMalignant Neoplasm of Prostate1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentNeuroendocrine Carcinomas1
2CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)2
2CompletedTreatmentSolid Cancers1
2Not Yet RecruitingTreatmentBreast Cancer Stage II / Breast Cancer Stage III / Cancer, Breast1
2Not Yet RecruitingTreatmentCancer, Breast1
2RecruitingNot AvailableCancer, Breast / Locally Advanced Malignant Neoplasm1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Neoplasm of Prostate / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentBreast Adenocarcinoma / HER2-positive Breast Cancer / Inflammatory Breast Carcinoma / Recurrent Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2RecruitingTreatmentCancer, Breast6
2RecruitingTreatmentCancer, Breast / HER-2 Positive Breast Cancer / Stage II Breast Cancer / Stage III Breast Cancer1
2RecruitingTreatmentCancer, Breast / Neoplasms, Breast / Tumors, Breast1
2RecruitingTreatmentCancers / Neoplasia / Neoplasms / Tumors1
2RecruitingTreatmentCarcinoma, Breast1
2RecruitingTreatmentEndocrine Sensitive HER2+/HR+ Breast Cancer1
2RecruitingTreatmentEpidermal Growth Factor Receptor (EGFR) Protein Overexpression / Malignant Neoplasm of Cardio-esophageal Junction of Stomach / Malignant Neoplasm of Stomach1
2RecruitingTreatmentHER2 Positive Breast Cancers / Inflammatory carcinoma of the breast / Invasive Ductal Breast Carcinoma / Malignant Neoplasm of Female Breast / Mucinous Breast Cancer Stage II / Tubular Breast Cancer Stage II / Tubular Breast Cancer Stage III1
2RecruitingTreatmentHER2-positive Breast Cancer2
2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2RecruitingTreatmentNeoplasms1
2RecruitingTreatmentNeoplasms, Breast1
2TerminatedTreatmentAdrenal Gland Tumors / Carcinoid Tumors / Multiple Endocrine Neoplasia / Neuroblastomas / Neuroendocrine Tumors / Progressive Neuroendocrine Tumors of pancreatic origin1
2TerminatedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentMalignant Neoplasm of Prostate1
2, 3RecruitingTreatmentEarly-Stage Breast Carcinoma / HER-2 Positive Breast Cancer1
2, 3RecruitingTreatmentGastroesophageal Junction Cancer / Malignant Neoplasm of Stomach1
3Active Not RecruitingTreatmentCancer, Breast7
3Active Not RecruitingTreatmentCancer, Breast / HER2 Positive1
3Active Not RecruitingTreatmentCancer, Breast / Neoplasms, Breast1
3Active Not RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Positive / Progesterone Receptor Positive / Stage IB Breast Cancer / Stage II Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
3Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
3Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
3CompletedTreatmentCancer, Ovarian1
3CompletedTreatmentHER2 Positive Breast Cancers / Inflammatory carcinoma of the breast / Invasive Ductal Breast Carcinoma / Malignant Neoplasm of Female Breast / Mucinous Breast Cancer Stage II / Tubular Breast Cancer Stage II / Tubular Breast Cancer Stage III1
3Not Yet RecruitingTreatmentHER2/Neu Positive / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
3RecruitingTreatmentCancer, Breast2
3RecruitingTreatmentEstrogen Receptor Positive Breast Cancer / HER-2 Positive Breast Cancer1
3RecruitingTreatmentHER2-positive Locally Advanced or Metastatic Breast Cancer1
3RecruitingTreatmentMetastatic Breast Cancer (MBC)1
3RecruitingTreatmentTumors, Solid1
3Unknown StatusTreatmentCancer, Breast1
4Active Not RecruitingTreatmentCancer, Breast1
Not AvailableCompletedTreatmentCancer, Breast1
Not AvailableRecruitingNot AvailableCancer, Breast1
Not AvailableRecruitingNot AvailableCancer, Breast / Metastatic Breast Cancer, Neoadjuvant Treatment of Breast Cancer1
Not AvailableRecruitingNot AvailableCancer, Breast / Pregnancy1
Not AvailableRecruitingTreatmentHER2 Positive Breast Carcinoma / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, solution, concentrateIntravenous30 mg/mL
Injection, solution, concentrateIntravenous420 mg
SolutionIntravenous420 mg
Kit; powder, for solution; 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
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

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 ]
Drug created on March 19, 2008 10:27 / Updated on August 17, 2016 12:24