PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
trastuzumab

Overview

Generic Names: Anti HER2; Ig gamma-1 chain C region
Trade Names: Herceptin (Genentech)
PharmGKB Accession Id: PA451743

Description

A recombinant IgG1 kappa, humanized monoclonal antibody that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein. Produced in CHO cell culture. (source: Drug Bank)

Indication

For treatment of HER2-positive metatsatic breast cancer (source: Drug Bank)

ATC Therapeutic Category

  • L01XC:Monoclonal antibodies

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Trastuzumab binds to the HER2 (or c-erbB2) proto-oncogene, an EGF receptor-like protein found on 20-30% of breast cancer cells. The binding leads to antibody mediated (complement mediated) killing of the HER2 positive cells. (source: Drug Bank)

Pharmacology

Used in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 25%-30% of primary breast cancers.Trastuzumab has been shown, in both in vitro assays and in animals, to inhibit the proliferation of human tumorcells that overexpress HER2. It is a mediator of antibody dependent cellular cytotoxicity, in that the binding of the antibody to HER2 overexpressing cells leads to preferential cell death. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Most likely removed by opsonization via the reticuloendothelial system. (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs1136201 at chr17:35133114 in ERBB2
    This variant is associated with cardiotoxicity in breast cancer patients treated with trastuzumab. The presence of Val allele may be a risk factor for cardiac toxicity. The Val form is also more sensitive to trastuzamab in vitro.
    Variant Name:
    ERBB2:Ile655Val
    Related Drugs:
    trastuzumab
    Related Diseases:
    Breast Neoplasms, Drug Toxicity
    Evidence:
    PMID:17693647
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available No genotype data Literature annotations available Not annotated
CDKN1A
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CDKN1B
  •   
  • PD
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
EGFR
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ERBB2
  • CO
  • PD
  •   
  • FA
  • GN
Publications, Variants
Phenotype data available No genotype data Literature annotations available Not annotated
ERBB3
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ERBB4
  • CO
  •   
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ESR1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
FCGR3A
  •   
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IGF1R
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
PTEN
  • CO
  • PD
  •   
  •   
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
VEGFA
  •   
  •   
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
FCGR1A Uncurated Annotation (source: Drug Bank)
FCGR3A Uncurated Annotation (source: Drug Bank)
FCGR3B Uncurated Annotation (source: Drug Bank)
FCGR2A Uncurated Annotation (source: Drug Bank)
FCGR2B Uncurated Annotation (source: Drug Bank)
FCGR2C Uncurated Annotation (source: Drug Bank)
C1QA Uncurated Annotation (source: Drug Bank)
C1QB Uncurated Annotation (source: Drug Bank)
C1QC Uncurated Annotation (source: Drug Bank)
C1R Uncurated Annotation (source: Drug Bank)
C1S Uncurated Annotation (source: Drug Bank)
EGFR Uncurated Annotation (source: Drug Bank)
ERBB2 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
lapatinib
  • CO
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
maytansine
  • CO
  •   
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
tamoxifen
  •   
  •   
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Breast Neoplasms
  • CO
  • PD
  •   
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Carcinoma, Non-Small-Cell Lung
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Cardiomyopathies
  • CO
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Cystadenocarcinoma, Papillary
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Cystadenocarcinoma, Serous
  • CO
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Drug Resistance
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Drug Toxicity
  • CO
  •   
  •   
  •   
  •   
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Endometrial Neoplasms
  • CO
  •   
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Neoplasms
  • CO
  •   
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Ovarian Neoplasms
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Uterine Neoplasms
  • CO
  •   
  •   
  • FA
  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00072
PubChem Substance ID:
736684

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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