Pertuzumab

Identification

Name
Pertuzumab
Accession Number
DB06366
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
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 structure
Db06366
Protein chemical formula
Not Available
Protein average weight
148000.0 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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PerjetaSolution420 mgIntravenousHoffmann La Roche2013-05-08Not applicableCanada
PerjetaInjection, solution, concentrate30 mg/1mLIntravenousGenentech, Inc.2012-06-08Not applicableUs
PerjetaInjection, solution, concentrate420 mgIntravenousRoche Registration Gmb H2013-03-04Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Perjeta-herceptinPertuzumab (420 mg) + Trastuzumab (440 mg)Kit; Powder, for solution; SolutionIntravenousHoffmann La Roche2013-05-09Not applicableCanada
Categories
UNII
K16AIQ8CTM
CAS number
380610-27-5

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.

Associated Conditions
Pharmacodynamics
Not 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.

TargetActionsOrganism
AReceptor tyrosine-protein kinase erbB-2
antibody
Human
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 binding
Not Available
Metabolism
Not Available
Route of elimination
Not 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Pertuzumab.
AbituzumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Abituzumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Pertuzumab.
AdecatumumabThe risk or severity of adverse effects can be increased when Adecatumumab is combined with Pertuzumab.
AducanumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Aducanumab.
AfelimomabThe risk or severity of adverse effects can be increased when Afelimomab is combined with Pertuzumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pertuzumab.
AlirocumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Alirocumab.
AmatuximabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Amatuximab.
AMG 108The risk or severity of adverse effects can be increased when AMG 108 is combined with Pertuzumab.
Food Interactions
Not Available

References

General References
  1. Pertuzumab protein sequence [Link]
External Links
KEGG Drug
D05446
PubChem Substance
347910348
ChEMBL
CHEMBL2007641
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pertuzumab
ATC Codes
L01XC13 — Pertuzumab
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (362 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingDiagnosticNeoplasms, Breast1
1Active Not RecruitingTreatmentHER2 Positive Breast Cancers / Her2-negative Metastatic Breast Cancer / HER2-positive Metastatic Breast Cancer / Locally Advanced or Early Breast Cancer1
1CompletedTreatmentCancer, Breast2
1CompletedTreatmentHer2-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
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentStage I Breast Carcinoma1
1CompletedTreatmentTumors, Solid2
1Not Yet RecruitingTreatmentCancer, Breast1
1RecruitingTreatmentCancer, Breast1
1RecruitingTreatmentMetastatic Breast Cancer (MBC) / Recurrent Breast Cancer1
1RecruitingTreatmentNeoplasms, Breast1
1TerminatedTreatmentAsymptomatic or Low Symptomatic Brain Metastasis in Breast Cancer / HER2 Positive Untreated Metastatic Breast Cancer1
1TerminatedTreatmentTumors, Solid1
1, 2Active Not RecruitingTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentCancer, Breast / DCIS Breast Cancer1
1, 2Active Not RecruitingTreatmentHER2/Neu Positive / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
1, 2CompletedTreatmentAdenocarcinoma of the Colon / Adenocarcinoma of the Rectum / Metastatic Colon Cancer / Recurrent Colon Cancer / Recurrent Rectal Cancer / Stage III Colon Cancer / Stage III Rectal Cancer / Stage IV Rectal Cancer1
1, 2CompletedTreatmentMetastatic Breast Cancer (MBC)2
1, 2CompletedTreatmentOesophageal Carcinoma1
1, 2RecruitingTreatmentBreast Diseases / Neoplasms, Breast1
1, 2RecruitingTreatmentMalignant Neoplasm of Breast1
1, 2TerminatedTreatmentCancer, Breast / Her2-Positive Breast Cancer1
1, 2TerminatedTreatmentER-positive Breast Cancer / Her2-Positive Breast Cancer1
2Active Not RecruitingBasic ScienceStage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2Active Not RecruitingOtherCancer, Breast / Locally Advanced Malignant Neoplasm1
2Active Not RecruitingOtherNeoplasms, Breast1
2Active Not RecruitingTreatmentCancer, Breast4
2Active Not RecruitingTreatmentElderly Metastatic Breast Cancer Population1
2Active Not RecruitingTreatmentHer2-Positive Breast Cancer1
2Active Not RecruitingTreatmentMalignant Tumor of the Breast / Neoplasms, Breast1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2Active Not RecruitingTreatmentMetastatic Colorectal Cancers1
2Active Not RecruitingTreatmentMetastatic HER2-Positive Breast Cancer1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2CompletedTreatmentCancer of the Ovary2
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2CompletedTreatmentCancer, Breast7
2CompletedTreatmentEndocrine Sensitive HER2+/HR+ Breast Cancer1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2CompletedTreatmentMalignant Neoplasm of Stomach1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentNeuroendocrine Carcinomas1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentSolid Cancers1
2Not Yet RecruitingTreatmentCancer, Breast / Estrogen Receptor Positive Tumor / Her2-Positive Breast Cancer1
2Not Yet RecruitingTreatmentCancer, Breast / Her2-Positive Breast Cancer1
2Not Yet RecruitingTreatmentHER2-Positive Early Breast Cancer1
2Not Yet RecruitingTreatmentLocally Advanced Breast Cancer (LABC)1
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 Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / 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
2RecruitingTreatmentBiliary Cancer / Bladder Cancers / Neoplasms / Salivary Cancer / Tumors, Solid1
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 of Unknown Primary Site1
2RecruitingTreatmentCancer, Breast4
2RecruitingTreatmentCancer, Breast / HER-2 Positive Breast Cancer / Stage II Breast Cancer / Stage III Breast Cancer1
2RecruitingTreatmentCancer, Breast / Neoplasms Metastasis1
2RecruitingTreatmentCancer, Breast / Neoplasms, Breast / Tumors, Breast1
2RecruitingTreatmentCarcinoma, Breast1
2RecruitingTreatmentCentral Nervous System Metastases / HER2-positive Metastatic Breast Cancer1
2RecruitingTreatmentColon Adenocarcinoma / ERBB2 Gene Amplification / Rectal Adenocarcinoma / Recurrent Colon Carcinoma / Recurrent Rectal Carcinoma / Stage III Colon Cancer AJCC v7 / Stage III Rectal Cancer AJCC v7 / Stage IIIA Colon Cancer AJCC v7 / Stage IIIA Rectal Cancer AJCC v7 / Stage IIIB Colon Cancer AJCC v7 / Stage IIIB Rectal Cancer AJCC v7 / Stage IIIC Colon Cancer AJCC v7 / Stage IIIC Rectal Cancer AJCC v7 / Stage IV Colon Cancer AJCC v7 / Stage IV Rectal Cancer AJCC v7 / Stage IVA Colon Cancer AJCC v7 / Stage IVA Rectal Cancer AJCC v7 / Stage IVB Colon Cancer AJCC v7 / Stage IVB Rectal Cancer AJCC v71
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 Cancer1
2RecruitingTreatmentMalignancies / Neoplasms / Tumors1
2RecruitingTreatmentNeoplasms, Breast1
2SuspendedTreatmentColorectal Cancers1
2TerminatedTreatmentAdrenal Gland Tumors / Carcinoid Tumors / Multiple Endocrine Neoplasia / Neuroblastomas / Neuroendocrine Tumors / Progressive Neuroendocrine Tumors of pancreatic origin1
2TerminatedTreatmentHER-2 Positive Breast Cancer / Her2-Positive Breast Cancer / Metastatic Breast Cancer (MBC)1
2TerminatedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentProstate Cancer1
2WithdrawnTreatmentBreast Cancer Stage II / Breast Cancer Stage III / Cancer, Breast1
2, 3Active Not RecruitingTreatmentGastroesophageal Junction Cancer / Malignant Neoplasm of Stomach1
2, 3RecruitingTreatmentEarly-Stage Breast Carcinoma / HER-2 Positive Breast Cancer1
3Active Not RecruitingTreatmentCancer, Breast5
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 IB Breast Cancer AJCC v7 / Stage II Breast Cancer / Stage IIA Breast Cancer / Stage IIA Breast Cancer AJCC v6 and v7 / Stage IIB Breast Cancer / Stage IIB Breast Cancer AJCC v6 and v7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v71
3Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
3Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
3CompletedTreatmentCancer of the Ovary1
3CompletedTreatmentCancer, Breast3
3CompletedTreatmentCancer, Breast / Neoplasms, Breast1
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 RecruitingOtherBreast Cancer Invasive Nos1
3Not Yet RecruitingTreatmentBreast Adenocarcinoma / HER2/Neu Positive / Recurrent Breast Carcinoma / Stage III Breast Cancer AJCC V7 / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
3Not Yet RecruitingTreatmentCancer, Breast1
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
3RecruitingTreatmentStage I Breast Carcinoma1
3RecruitingTreatmentTumors, Solid1
4CompletedTreatmentCancer, 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

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solution, concentrateIntravenous30 mg/1mL
Injection, solution, concentrateIntravenous420 mg
SolutionIntravenous420 mg
Kit; powder, for solution; solutionIntravenous
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2376596No2009-10-062020-06-23Canada
CA2579861No2012-12-182025-10-19Canada

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not 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, alt...
Gene Name
ERBB2
Uniprot ID
P04626
Uniprot Name
Receptor tyrosine-protein kinase erbB-2
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 December 14, 2018 05:40