Drug/Small Molecule:
Pertuzumab

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB gathers information regarding PGx on FDA drug labels from the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels", and from FDA-approved FDA and EMA-approved (European Medicines Agency) EMA labels brought to our attention. Excerpts from the label and downloadable highlighted label PDFs are manually curated by PharmGKB.

Please note that some drugs may have been removed from or added to the FDA's "Table of Pharmacogenomic Biomarkers in Drug Labels" without our knowledge. We periodically check the table for additions to this table and update PharmGKB accordingly.

There is currently no such list for European drug labels - we are working with the EMA to establish a list of European Public Assessment Reports (EPAR)s that contain PGx information. We are constructing this list by initially searching for drugs for which we have PGx-containing FDA drug labels - of these 44 EMA EPARs were identified and are being curated for pgx information.

We welcome any information regarding drug labels containing PGx information approved by the FDA, EMA or other Medicine Agencies around the world - please contact feedback.



last updated 10/25/2013

FDA Label for Pertuzumab and ERBB2

This label is on the FDA Biomarker List
Genetic testing required

Summary

Pertuzumab is a targeted antibody drug designed to bind to ERBB2. Detection of HER2 protein overexpression is necessary for selection of patients appropriate for PERJETA therapy because these are the only patients studied and for whom benefit has been shown.

Annotation

Pertuzumab is a targeted antibody drug designed to bind to ERBB2.

Excerpt from the Pertuzumab (Perjeta) label:

PERJETA is a HER2/neu receptor antagonist indicated 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 .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).

Detection of HER2 protein overexpression is necessary for selection of patients appropriate for PERJETA therapy because these are the only patients studied and for whom benefit has been shown. Patients with breast cancer were required to have evidence of HER2 overexpression defined as 3+ IHC or FISH amplification ratio in the clinical studies. Only limited data were available for patients whose breast cancer was positive by FISH, but did not demonstrate protein overexpression by IHC. Assessment of HER2 status should be performed by laboratories using FDA-approved tests with demonstrated proficiency in the specific technology being utilized.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the Pertuzumab (Perjeta) drug label.

*Disclaimer: The contents of this page have not been endorsed by the FDA and are the sole responsibility of PharmGKB.

Full label available at DailyMed

Genes and/or phenotypes found in this label

  • Breast Neoplasms
    • Indications & usage section
    • source: FDA Label
  • Cardiomyopathies
    • Boxed warning section
    • source: FDA Label
  • Hypersensitivity
    • Adverse reactions section, Warnings and precautions section
    • source: FDA Label
  • Ventricular Dysfunction, Left
    • Adverse reactions section, Warnings and precautions section
    • source: FDA Label
  • ERBB2
    • Clinical pharmacology section, Warnings and precautions section, efficacy
    • source: FDA Label

last updated 06/13/2014

European Medicines Agency (EMA) Label for Pertuzumab and ERBB2

Genetic testing required

Summary

The EMA European Public Assessment Report (EPAR) for pertuzumab (Perjeta) states that testing by a specialized laboratory must be performed to establish HER2 (ERBB2)-positive tumor status due to the action of the drug.

Annotation

Pertuzumab (Perjeta) is a monoclonal antibody that targets HER2 (ERBB2) to block signalling pathways to induce cell growth arrest and apoptosis. In combination with trastuzumab it was shown to augment antitumour activity.

Excerpts from the pertuzumab (Perjeta) EPAR:

Perjeta is indicated for use in combination with trastuzumab and docetaxel in adult patients with HER2-positive metastatic or locally recurrent unresectable breast cancer, who have not received previous anti-HER2 therapy or chemotherapy for their metastatic disease.


Patients treated with Perjeta must have HER2-positive tumour status, defined as a score of 3+ by immunohistochemistry (IHC) and/or a ratio of more than or equal to 2.0 by in situ hybridisation (ISH) assessed by a validated test. To ensure accurate and reproducible results, the testing must be performed in a specialised laboratory, which can ensure validation of the testing procedures. For full instructions on assay performance and interpretation please refer to the package leaflets of validated HER2 testing assays.

For the complete drug label text with sections containing pharmacogenetic information highlighted, see the pertuzumab (Perjeta) EMA drug label.

*Disclaimer: The contents of this page have not been endorsed by the EMA and are the sole responsibility of PharmGKB.

Genes and/or phenotypes found in this label

  • Breast Neoplasms
    • Indications & usage section, Information for patients section, Pediatric use section, Pharmacodynamics section, Use in specific populations section, efficacy
    • source: European Medicines Agency (EMA) Label
  • ERBB2
    • Indications & usage section, Information for patients section, Pharmacodynamics section, Warnings and precautions section, efficacy
    • source: European Medicines Agency (EMA) Label

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Immunoglobulin G1, anti-(human v (receptor)) (human-mouse monoclonal 2C4 heavy chain), disulfide with human-mouse monoclonal 2C4 kappa-chain, dimer
  • LS-185920
  • Omnitarg
Trade Names
Brand Mixture Names

PharmGKB Accession Id:
PA165290933

Description

Pertuzumab is a monoclonal antibody that targets an epitope located at subdomain II of HER2, distinct from the epitope recognized by trastuzumab [Article:22475266].

Source: PharmGKB

Indication

Pertuzumab is targeted for HER2 positive (ERBB2) breast cancer [Article:22475266].

Source: PharmGKB

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available DL No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ERBB2
No related drugs are available.

Curated Information ?

Publications related to Pertuzumab: 8

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug Interaction Potential of Trastuzumab Emtansine Combined With Pertuzumab in Patients With HER2-Positive Metastatic Breast Cancer. Current drug metabolism. 2012. Lu Dan, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CLEOPATRA: a phase III evaluation of pertuzumab and trastuzumab for HER2-positive metastatic breast cancer. Clinical breast cancer. 2010. Baselga José, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Open-label, phase II, multicenter, randomized study of the efficacy and safety of two dose levels of Pertuzumab, a human epidermal growth factor receptor 2 dimerization inhibitor, in patients with human epidermal growth factor receptor 2-negative metastatic breast cancer. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Gianni Luca, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
In vitro activity of pertuzumab in combination with trastuzumab in uterine serous papillary adenocarcinoma. British journal of cancer. 2010. El-Sahwi K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Evolving novel anti-HER2 strategies. The lancet oncology. 2009. Jones Kellie L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Efficacy and safety of single-agent pertuzumab, a human epidermal receptor dimerization inhibitor, in patients with non small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2007. Herbst Roy S, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Efficacy and safety of single-agent pertuzumab (rhuMAb 2C4), a human epidermal growth factor receptor dimerization inhibitor, in castration-resistant prostate cancer after progression from taxane-based therapy. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2007. Agus David B, et al. PubMed

LinkOuts

PubChem Substance:
47207115

Clinical Trials

These are trials that mention Pertuzumab and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.