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Identification
- Summary
Pertuzumab is an antineoplastic agent used in the treatment of HER2-positive metastatic breast cancer in combination with other antineoplastic agents.
- Brand Names
- Perjeta, Perjeta-Herceptin, Phesgo
- Generic Name
- Pertuzumab
- DrugBank Accession Number
- DB06366
- Background
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. It was first approved by the FDA in 2012 for use with docetaxel and another HER2-targeted monoclonal antibody, trastuzumab, in the treatment of metastatic HER2-positive breast cancer. Its indicated conditions have since expanded to include use as both a neoadjuvant therapy and an adjuvant therapy in the treatment of HER2-positive breast cancers at high risk of recurrence.5,8
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- 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
- Pertuzumab
- rhuMAb-2C4
- External IDs
- R1273
- RG-1273
Pharmacology
- Indication
Pertuzumab is indicated for intravenous administration 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.6 It is also indicated in combination with trastuzumab and other chemotherapies for the neoadjuvant treatment of HER2-positive locally advanced, inflammatory, or early-stage breast cancer as part of a complete treatment regimen6 and as adjuvant treatment in patients with HER2-positive early-stage breast cancer at high risk of recurrence.6
Pertuzumab is also indicated for subcutaneous injection - in combination with trastuzumab and hyaluronidase - in the treatment of HER2-positive breast cancers in adults.4
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Early breast cancer Combination Product in combination with: Hyaluronidase (human recombinant) (DB06205), Trastuzumab (DB00072) •••••••••••• •••• •••• •• •••••••••• ••••••••• Used in combination to treat Early breast cancer Combination Product in combination with: Trastuzumab (DB00072), Hyaluronidase (human recombinant) (DB06205) •••••••••••• ••••••••• Used in combination to treat Early breast cancer Regimen in combination with: Trastuzumab (DB00072) •••••••••••• •••• •••• •• •••••••••• ••••••••• Used in combination to treat Early breast cancer Regimen in combination with: Trastuzumab (DB00072) •••••••••••• ••••••••• Used in combination to treat Inflammatory breast cancer (ibc) Combination Product in combination with: Trastuzumab (DB00072), Hyaluronidase (human recombinant) (DB06205) •••••••••••• ••••••••• - Contraindications & Blackbox Warnings
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Pertuzumab exerts its antineoplastic effects by binding to and inhibiting the activity of HER2, an oncogene that has been implicated in the formation of numerous cancers.6 As with other therapeutic monoclonal antibodies, pertuzumab has a relatively long duration of action necessitating dosing every 3 weeks.6 Drugs that block HER2 activity, including pertuzumab, have been implicated in the development of cardiotoxicity (specifically left ventricular dysfunction) - a baseline assessment of left ventricular ejection fraction (LVEF) should be conducted prior to beginning therapy with pertuzumab and at regular intervals throughout therapy to ensure LVEF remains within normal limits. Consider indefinite suspension of therapy if LVEF declines and does not improve.6
- Mechanism of action
Human epidermal growth factor receptor-2 (HER2) is a tyrosine kinase receptor that plays an integral role in cell proliferation, differentiation, and survival. HER2 becomes active following dimerization with another HER2 receptor, another member of the HER protein family (e.g. HER3), or with a ligand - this dimer then phosphorylates and activates numerous intracellular signaling proteins, initiating signal transduction via pathways that include the Ras/mitogen-activated protein kinase pathway, the phosphatidylinositol 3' kinase (PI3K)/Akt pathway, and then Janus kinases/signal transducer and activator transcription pathway.2 HER2 is also a known oncogene - it is overexpressed or gene-amplified (i.e. HER2-positive) in approximately 20% of breast cancers and these cancers carry a generally poorer prognosis than HER2-negative breast cancers.2
Pertuzumab targets the extracellular dimerization domain (subdomain II) of HER2, thereby inhibiting ligand-initiated intracellular signaling via the MAP kinase and PI3K pathways. Inhibition of these pathways results in inhibition of cell growth and the initiation of apoptosis, respectively.5 Pertuzumab also appears to mediate antibody-dependent cell-mediated cytotoxicity.5
Target Actions Organism AReceptor tyrosine-protein kinase erbB-2 binderantibodyHumans - Absorption
Intravenously administered pertuzumab, given as a loading dose of 840mg followed by a maintenance dose of 420mg every 3 weeks, reaches steady-state concentration following the first maintenance dose.6 In its subcutaneous formulation, in combination with [hylauronidase], the absolute bioavailability of pertuzumab is approximately 0.7 and the median Tmax is 4 days.7 This subcutaneous formulation leverages the benefits of co-administration with hyaluronidase - this enzyme breaks down hylauronic acid, thereby decreasing the viscosity of the extracellular matrix (ECM) and allowing for greater bioavailability with subcutaneous administration.7
- Volume of distribution
The average steady-state volume of distribution following intravenous administration is 3.53 - 7.5 L.6
- Protein binding
Not Available
- Metabolism
The metabolism of pertuzumab has not been studied directly. Monoclonal antibodies are typically subject to catabolism to smaller peptides and proteins prior to elimination.6
- Route of elimination
Not Available
- Half-life
The median half-life of pertuzumab was determined to be 18 days based on a population pharmacokinetic analysis.5
- Clearance
The median clearance of pertuzumab was determined to be 0.24 L/day based on a population pharmacokinetic analysis.5
- Adverse Effects
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There are no data regarding overdose of pertuzumab. Single doses higher than 25 mg/kg have not been tested.6 Symptoms of overdose are likely to be consistent with pertuzumab's adverse effect profile, and may therefore involve significant diarrhea, alopecia, neutropenia, nausea, fatigue, rash, and/or peripheral neuropathy.5 Pertuzumab has been associated with the development of left ventricular dysfunction (i.e. cardiotoxicity) that may be exacerbated in instances of overdose.5
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Pertuzumab. Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Pertuzumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Pertuzumab. Aducanumab The risk or severity of adverse effects can be increased when Pertuzumab is combined with Aducanumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Pertuzumab. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Omnitarg / Perjeta
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Perjeta Solution 420 mg / 14 mL Intravenous Hoffmann La Roche 2013-05-08 Not applicable Canada 
Perjeta Injection, solution, concentrate 30 mg/1mL Intravenous Genentech, Inc. 2012-06-08 Not applicable US 
Perjeta Injection, solution, concentrate 420 mg Intravenous Roche Registration Gmb H 2016-09-08 Not applicable EU 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Perjeta-herceptin Pertuzumab (420 mg / 14 mL) + Trastuzumab (440 mg / vial) Kit; Powder, for solution; Solution Intravenous Hoffmann La Roche 2013-05-09 Not applicable Canada Phesgo Pertuzumab (600 mg/10mL) + Hyaluronidase (human recombinant) (20000 U/10mL) + Trastuzumab (600 mg/10mL) Injection, solution Subcutaneous Genentech, Inc. 2020-06-29 Not applicable US Phesgo Pertuzumab (80 mg / mL) + Trastuzumab (40 mg / mL) Solution Subcutaneous Hoffmann La Roche 2021-04-08 Not applicable Canada Phesgo Pertuzumab (600 mg) + Trastuzumab (600 mg) Injection, solution Subcutaneous Roche Registration Gmb H 2021-01-28 Not applicable EU Phesgo Pertuzumab (1200 mg/15mL) + Hyaluronidase (human recombinant) (30000 U/15mL) + Trastuzumab (600 mg/15mL) Injection, solution Subcutaneous Genentech, Inc. 2020-06-29 Not applicable US
Categories
- ATC Codes
- L01FY01 — Pertuzumab and trastuzumab
- L01FY — Combinations of monoclonal antibodies and antibody drug conjugates
- L01F — MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
- L01 — ANTINEOPLASTIC AGENTS
- L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Breast Neoplasms
- Cancer immunotherapy
- Cardiotoxic antineoplastic agents
- Globulins
- HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors
- HER2 Receptor Antagonists
- HER2/Neu/cerbB2 Antagonists
- Immunoglobulins
- Immunoproteins
- Immunotherapy
- Monoclonal antibodies and antibody drug conjugates
- Proteins
- Receptor, ErbB-2, antagonists & inhibitors
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- 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
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- K16AIQ8CTM
- CAS number
- 380610-27-5
References
- Synthesis Reference
Adams CW, Allison DE, Flagella K, Presta L, Clarke J, Dybdal N, McKeever K, Sliwkowski MX: Humanization of a recombinant monoclonal antibody to produce a therapeutic HER dimerization inhibitor, pertuzumab. Cancer Immunol Immunother. 2006 Jun;55(6):717-27. doi: 10.1007/s00262-005-0058-x. Epub 2005 Sep 3.
- General References
- Adams CW, Allison DE, Flagella K, Presta L, Clarke J, Dybdal N, McKeever K, Sliwkowski MX: Humanization of a recombinant monoclonal antibody to produce a therapeutic HER dimerization inhibitor, pertuzumab. Cancer Immunol Immunother. 2006 Jun;55(6):717-27. doi: 10.1007/s00262-005-0058-x. Epub 2005 Sep 3. [Article]
- Malenfant SJ, Eckmann KR, Barnett CM: Pertuzumab: a new targeted therapy for HER2-positive metastatic breast cancer. Pharmacotherapy. 2014 Jan;34(1):60-71. doi: 10.1002/phar.1338. Epub 2013 Aug 5. [Article]
- Pertuzumab protein sequence [Link]
- FDA News Release: FDA Approves Breast Cancer Treatment That Can Be Administered At Home By Health Care Professional [Link]
- FDA Approved Drug Products: Perjeta (pertuzumab) for intravenous injection [Link]
- Health Canada Product Monograph: Perjeta (pertuzumab) for intravenous injection [Link]
- FDA Approved Drug Products: Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) for subcutaneous injection [Link]
- FDA Drug Approvals: FDA grants regular approval to pertuzumab for adjuvant treatment of HER2-positive breast cancer [Link]
- External Links
- KEGG Drug
- D05446
- PubChem Substance
- 347910348
- 1298944
- ChEMBL
- CHEMBL2007641
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Pertuzumab
- FDA label
- Download (362 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Breast Cancer 1 somestatus stop reason just information to hide Not Available Active Not Recruiting Treatment Breast Cancer 1 somestatus stop reason just information to hide Not Available Approved for Marketing Not Available Coronavirus Disease 2019 (COVID‑19) / HER2/Neu-positive Breast Cancer 1 somestatus stop reason just information to hide Not Available Completed Not Available Breast Cancer 2 somestatus stop reason just information to hide Not Available Completed Not Available Breast Cancer / Pregnancy 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 30 MG/ML Injection, solution, concentrate Intravenous 30 mg/1mL Injection, solution, concentrate Intravenous 420 MG Injection, solution, concentrate Intravenous 420 mg/14ml Injection, solution, concentrate Intravenous; Parenteral 420 MG Solution Intravenous 420 mg / 14 mL Solution Intravenous 420.000 mg Injection, solution, concentrate Parenteral 420 mcg/14mL Injection, solution, concentrate Intravenous Solution Intravenous 30 mg/ml Kit; powder, for solution; solution Intravenous Solution, concentrate Intravenous 420 mg Solution, concentrate Intravenous 42000000 mg Injection, solution Subcutaneous Solution Subcutaneous Injection, solution Subcutaneous 1200 mg Injection, solution Subcutaneous 600 mg Solution Subcutaneous 6000000 mg Solution Intravenous 420 mg/14ml - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2376596 No 2009-10-06 2020-06-23 Canada CA2579861 No 2012-12-18 2025-10-19 Canada
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- BinderAntibody
- General 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-RHOA-DIAPH1 signaling pathway elicits the phosphorylation and thus the inhibition of GSK3B at cell membrane. This prevents the phosphorylation of APC and CLASP2, allowing its association with the cell membrane. In turn, membrane-bound APC allows the localization of MACF1 to the cell membrane, which is required for microtubule capture and stabilization
- Specific Function
- ATP binding
- Gene Name
- ERBB2
- Uniprot ID
- P04626
- Uniprot Name
- Receptor tyrosine-protein kinase erbB-2
- Molecular Weight
- 137909.27 Da
References
Drug created at March 19, 2008 16:27 / Updated at June 03, 2022 07:24