Monoclonal antibodies Flashcards
How does monoclonal antibodies work in general ?
They target specific antigens that are over expressed on the tumour cell surface and create MAC complexes which cause complement mediated cell lysis or the monoclonal anti-bodies trigger immune mediated destruction. All monoclonal antibodies are administered IV.
what is the speciality of human cell derived monoclonal antibodies which ends with ‘ umab’ ?
They are less likely to cause HSR.
What is the speciality of chimeric antibodies ends with ‘ Ximab’ ?
They have both human and non-human components. They are more likely to be recognized as foreign leading to HSR.
what is the speciality of humanised monoclonal antibodies ends in ‘Zumab’ ?
These are drugs derived from non human species and are less likely to cause HSR as compared to chimeric antibodies.
What is the MOA of Cetuximab ?
It inhibits the activation of K-RAS pathway by binding to the tyrosine kinase receptor EGFR resulting in inhibition of cell proliferation, migration , and angiogenesis.
What are the indications for Cetuximab ?
They are indicated for the Tx of metastatic colorectal cancer as well as Head and neck cancers.
What are the side effects of chimeric antibody Cetuximab?
- infusion HSR
- GI and hepatic toxicity.
- Acniform skin rashes with pruritus.
What is the MOA and indication of Trastuzumab ( Herceptin) ?
It is a HER2 receptor antagonist which act by inhibiting HER2 mediated tumorogenesis by inhibiting the signaling through PI3K AKt mTOR pathway, and MAPK pathway. It is mainly used to treat HER2 positive breast cancer. It is also used to treat gastric, ovarian, and lung cancers caused by HER2 mutation.
What is the main side effect of Trastuzumab ?
Inhibition of HER2 receptors on the normal cardiomyocytes leads to cardiotoxic heart failure. Other side effects are GI disturbances, fever, chills, and headaches.
What is the MOA and indication of Bevacizumab?
It inhibits VEGF and prevent angiogenesis of the solid tumours leading to the apoptosis of the tumour cells. It is used to treat colorectal cancer, renal cell carcinoma, breast cancer and non-small cell lung cancer.
What are the side effects of Bevacizumab ?
- Impaired angiogenesis of normal tissue.
- Impaired wound healing.
- Epistaxis and hemoptysis.
- GI and intracerebral haemorrhage.
What is the MOA and indication of Rituximab ?
It binds to the CD20 receptor of the B cell and drives cmplement mediated MAC formation which causes pores on the cell leading to cell lysis. In addition, it also enhance apoptosis signaling and anti-body dependent cell mediated cytotoxicity.
It is indicated for the Tx of non-hodgkins B cell lymphoma, CLL, Ideopathic thormbocytopaenic purpura and RA.
What are the side effects of Rituximab ?
- HSR and immune supression.
- Activation of latent viral infections.
- JC virus activation leading to progressive multifocal leukoencephalopathy.
What is the MOA and indication of Alemtuzumab ?
It acts by binding to CD52 receptors of all lymphocytes and destroy them through complement mediated lysis, apoptosis, and phagocytosis by NK cells. It is indicated to treat CLL and MS.
What is the MOA and indication of Imatinibe ?
It inhibits the signaling mediated by the BCR-ABL gene formed by the 9 , 22 chromosomal translocation. It is indicated to treat the Philadelphia chromosome positive CML.
