How does pertuzumab work?

How does pertuzumab work?

Pertuzumab works by locking onto HER2 on the cancer cells. It stops them from growing and kills them. Pertuzumab only works if your cancer is HER2 positive.

What is trastuzumab mechanism of action?

Mechanism of Action of Trastuzumab Trastuzumab consists of two antigen-specific sites that bind to the juxtamembrane portion of the extracellular domain of the HER2 receptor and that prevent the activation of its intracellular tyrosine kinase. The remainder of the antibody is human IgG with a conserved Fc portion.

Is pertuzumab an EGFR inhibitor?

Pertuzumab is a recombinant, humanized, monoclonal antibody that binds to the extracellular dimerization domain II of HER2 (located on the opposite side of the domain IV where trastuzumab binds). Pertuzumab inhibits heterodimerization of HER2 with EGFR, HER3, HER4 (Nahta et al.

What drug class is pertuzumab?

This medication is classified as an “antineoplastic agent and a monoclonal antibody”.

How effective is pertuzumab?

Pertuzumab has been shown to be safe and effective in metastatic and early HER2-positive breast cancer. Pertuzumab has been demonstrated to be effective for progressive growth against trastuzumab single-agent treatment for metastatic HER2-positive breast cancer.

Is pertuzumab a monoclonal antibody?

Pertuzumab is a humanized monoclonal antibody targeting HER2 that is different from trastuzumab in that it binds to a different domain of HER2; hence, combining the two drugs leads to a more comprehensive blockade of the receptor.

How is trastuzumab metabolized?

Trastuzumab is metabolized to peptides and amino acids. The elimination is a complex of processes in humans but is specifically mediated by epithelial cells. Trastuzumab binds to HER-2 and is metabolized intracellularly. The consequence of intracellular binding explains a dose-dependent (nonlinear) elimination.

Is trastuzumab chemotherapy or immunotherapy?

These are active specific immunotherapy with Theratope and passive immunotherapy targeting the HER-2 receptor with trastuzumab (Herceptin). Trastuzumab has a proven efficacy as monotherapy as well as in combination with chemotherapeutic agents in HER-2-overexpressing metastatic breast cancer.

What are the side effects of pertuzumab?

Common side effects of pertuzumab and trastuzumab

• Risk of infection. This treatment can reduce the number of white blood cells in your blood.
• Bruising and bleeding.
• Anaemia (low number of red blood cells)
• Effects on the heart.
• Diarrhoea.
• Feeling sick.
• Loss of appetite.
• Sore mouth.

What is the mechanism of action for the chemotherapeutic drug cetuximab?

By binding to EGFR on cancer cell, cetuximab blocks EGF from binding to this receptor (activation). This stops the cell from continuing the pathway that promotes cell division and growth, effectively stopping the cancer by stopping the cancerous cells from growing and multiplying.

How is pertuzumab made?

Pertuzumab is a man-made antibody developed using molecular cloning and recombinant DNA technology. Pertuzumab is thought to block the HER2 receptors when there is overexpression, thereby blocking growth of the cancer.

Is pertuzumab and trastuzumab chemotherapy?

Trastuzumab and pertuzumab are types of targeted cancer drugs. You might have them on their own or with other chemotherapy drugs. It is a treatment for breast cancer.

Summary The humanized monoclonal antibody pertuzumab prevents the dimerization of HER2 with other HER receptors, in particular the pairing of the most potent signaling heterodimer HER2/HER3, thus providing a potent strategy for dual HER2 inhibition. It binds to the extracellular domain of HER2 at a different epitope than trastuzumab.

What is the mechanism of action of humanized monoclonal antibody pertuzumab?

Pertuzumab is a humanized monoclonal antibody that binds to the dimerization domain of HER2. Blocking the pairing of the most potent signaling HER dimer, HER2-HER3, affects key signaling pathways [13, 17, 20, 21].

How does pertuzumab work with the HER3 dimer?

The most potent dimer for activating signalling pathways is HER2/HER3. The epitope for pertuzumab is the domain of HER2 where it binds to HER3, and pertuzumab prevents the HER2/HER3 dimer from forming, which blocks signalling by the dimer.

Does pertuzumab interact with doxorubicin?

It is unknown if pertuzumab interacts with doxorubicin. It is the first-in-class of a kind of drug called a ” HER dimerization inhibitor” — it inhibits the dimerization of HER2 with other HER receptors, which prevents them from signalling in ways that promote cell growth and proliferation.