Targeted drugs in oncology: new names, new mechanisms, new paradigm
William Rotea1, Everardo D Saad
1Division of Pharmacy, Department of Medical Oncology, Albert Einstein Hospital, São Paulo, Brazil. rotea@uol.com.br
Abstract:
The molecular mechanisms of action, clinical development, and efficacy and safety of targeted antineoplastic drugs are discussed. Recently introduced mechanism-based systemic therapies for cancer may be more specific, less toxic, and more effective and represent a paradigm shift in treatment. Currently, receptor tyrosine kinases (RTKs), nonreceptor kinases, the angiogenic molecules, the enzymes involved in extracellular matrix degradation, and the enzymes responsible for protein anchorage to the cytoplasmic membrane are among the targets against which specific interventions have been developed. Monoclonal antibodies against the extracellular portion of RTKs and small-molecule inhibitors of their tyrosine kinase activity are strategies in more advanced phases of clinical development. Over the next few years, one can expect to see the results of many studies of such new pharmacologic agents or combinations. It seems likely, at this point, that targeted drugs will be used in association with existing medical, surgical, and radiotherapeutic modalities and will play an important role in the ultimate goal of reducting the burden of cancer. Targeting of molecular abnormalities that are differentially expressed in tumors may represent a more specific and less toxic way of treating cancer.
Insights
Targeted antineoplastic drugs offer a paradigm shift in cancer treatment, showing promise for increased specificity and reduced toxicity. These mechanism-based therapies are expected to complement existing treatments, significantly reducing the cancer burden.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Cancer treatment is evolving with the introduction of mechanism-based systemic therapies.
- Targeted antineoplastic drugs represent a new frontier, aiming for greater specificity and reduced toxicity compared to traditional treatments.
Purpose of the Study:
- To discuss the molecular mechanisms of action, clinical development, efficacy, and safety of targeted antineoplastic drugs.
- To highlight the paradigm shift these therapies represent in cancer treatment.
Main Methods:
- Review of current targeted therapies focusing on specific molecular targets.
- Discussion of clinical development phases for monoclonal antibodies and small-molecule inhibitors.
- Analysis of targets including receptor tyrosine kinases (RTKs), nonreceptor kinases, and enzymes involved in matrix degradation.
Main Results:
- Targeted therapies demonstrate potential for increased specificity, reduced toxicity, and improved efficacy.
- Monoclonal antibodies and small-molecule inhibitors targeting RTKs are in advanced clinical development.
- Combinations of targeted drugs with existing modalities are anticipated.
Conclusions:
- Targeting molecular abnormalities offers a more specific and less toxic approach to cancer treatment.
- Targeted drugs are likely to be integrated with conventional therapies, playing a key role in reducing cancer burden.
- Continued research and clinical trials are crucial for realizing the full potential of targeted antineoplastic drugs.
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