Trastuzumab

Trastuzumab


TRASTUZUMAB/HERCEPTIN

INTRODUCTION:

  • A recombinant humanized unarmed monoclonal antibody against Human Epidermal Growth Receptor-2-protein (HER2)
  • Shows better response in combination with paclitaxel.

MODE OF ACTION:

Trastuzumab mediates Antibody-Dependent Cell-mediated Cytotoxicity (ADCC): 

  • After binding to HER2 on tumour cell surface, trastuzumab induces ADCC against tumour cells that overexpress HER2.
  • Also, once bound to Fc domain of trastuzumab, NK cells release substances that perforate tumour cell membrane and promote cell death.

INDICATIONS:

Approved to be used alone or with other drugs to treat:

  • Adenocarcinoma of stomach or gastro oesophagal junction.
  • Metastasized HER-2 positive conditions, who have not already been treated for metastatic cancer.
  • HER-2 (+ve) Breast cancer.
  • HER2 overexpressed by many adenocarcinomas, particularly breast adenocarcinomas.
  • HER2 protein overexpression, HER2 gene amplificationor both, occur in approximately 15-25% of breast cancers, associated with aggressive behaviour in tumour.

For women with breast cancer with HER2 overexpression:

  • Adjuvant therapy (before/after/in combination) with established chemotherapeutic agents.
  • Eg: Anthracyclines & Taxanes, surgery & radiation treatment.
  • Improves survival benefit.

ADVERSE EFFECT:

  • Diarrhoea.
  • Constipation.
  • Heartburn.
  • Loss of appetite.
  • Back, bone, joint, or muscle pain.
  • Insomnia.
  • Numbness, burning or tingling in arms, hands, feet, or legs.
  • Changes in appearance of nails.
  • Cardiomyopathy.
  • Sore throat, fever, chills, difficulty urinating, pain when urinating, and other signs of infection.
  • Nosebleeds and other unusual bruising or bleeding.
  • Excessive tiredness.
  • Pale skin.

LATEST NEW DRUG:

  • Ado-trastuzumab mertansine – Conjugate of trastuzumab (monoclonal antibody against her-2) & mertansine (microtubule inhibitor). 
  • Approved for HER-2 positive metastatic breast cancer treatment.
Exam Question
 
  • Trastuzumab has a specific activity in a subset of female breast cancers.
  • Trastuzumab shows a better response in combination with paclitaxel.
  • Trastuzumab is used in metastatic breast cancer.
  • Trastuzumab is a monoclonal antibody produced by injecting HER-2 antigen.
  • Trastuzumab causes dilated cardiomyopathy.
Don’t Forget to Solve all the previous Year Question asked on Trastuzumab

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