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Neoplasia (BIOCHEMISTRY OF INTERCELLULAR AND INTRACELLULAR SIGNAL…
Neoplasia
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ANTINEOPLASTIC DRUGS
CLASSIFICATION
B. Targeted drugs
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Monoclonal Antibodies:
Rituximab - It lyses B lymphocytes by binding to the calcium-channel forming CD20 protein and activating complement
Alemtuzumab
Ofatumab
Brentixumab
Trastuzumab - oncogenic protein termed HER2
panitumumab and cetuximab
Bevacizumab -It neutralises VEGF (vascular endothelial growth factor), thereby preventing the angiogenesis that is crucial to tumour survival.
Catumaxomab -attaches to an epithelial adhesion molecule, EpCAM, which is overexpressed in some malignant cells (e.g. malignant ascites in the peritoneal cavity). The antibody binds to this adhesion molecule and also to T lymphocytes and antigen-presenting cells, thus facilitating the action of the immune system in clearing the cancer.
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A. Cytotoxic drugs
1. Alkylating agents
Bis(chlorethyl)amines (nitrogen mustards): -ph(f)os-ph(f)amide
Prototype: cyclophosphamide
Others: mechlorethamine, chlorambucil, melphalan, ifosfamide
Nitrosoureas: -mustine
Prototype: carmustine
Others: lomustine, semustine, bendamustine
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Platinum coordination complexes:-platin
Prototype: cisplatin
Others: carboplatin, oxaliplatin
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Triazine: -carbazine
Dacarbazine (DTIC),
Temozolomide
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GENERAL TOXICITY OF
CYTOTOXIC DRUGS:
Majority of the cytotoxic drugs have more
profound effect on rapidly multiplying cells,
because the most important target of action are
the nucleic acids and their precursors, and rapid nucleic acid synthesis occurs during cell division.
Many cancers (especially large solid tumours)
have a lower growth fraction (lower percentage
of cells are in division) than normal bone marrow,
epithelial linings, reticuloendothelial (RE) system
and gonads. These tissues are particularly affected
in a dose-dependent manner by majority of drugs;
though, there are differences in susceptibility to
individual members.
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10. Individual toxicities:
neuropathy by vincristine, cardiomyopathy
by doxorubicin, cystitis and alopecia
by cyclophosphamide, pulmonary
fibrosis and skin pigmentation- Busulfan