If small molecules immunotherapy comes, can the prime be far behind?
Jingyu Zhang1, Yu Zhang1, Bingxue Qu1
1Hangzhou Institute of Innovative Medicine, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, PR China.
European Journal of Medicinal Chemistry
|March 27, 2021
Summary
Small molecule inhibitors offer an alternative to antibody-based anti-cancer immunotherapies, overcoming limitations like poor bioavailability. This review explores their mechanisms and potential in combination with immune checkpoint inhibitors for improved cancer treatment.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- Anti-cancer immunotherapy, including immune checkpoint blockade (ICB), has revolutionized cancer treatment.
- Current immune checkpoint inhibitors (ICIs) are monoclonal antibodies (mAbs) with limitations such as poor oral bioavailability and tissue penetration.
- The tumor micro-environment (TME) presents challenges for effective cancer immunotherapy.
Purpose of the Study:
- To review the mechanisms and therapeutic potential of small molecule inhibitors targeting cancer.
- To discuss the advantages of small molecule inhibitors over monoclonal antibodies in cancer immunotherapy.
- To summarize the current status of small molecule inhibitors in combination therapies for cancer.
Main Methods:
- Literature review of anti-cancer immunotherapy, focusing on immune checkpoint inhibitors.
- Analysis of the limitations of monoclonal antibody-based ICIs.
- Exploration of small molecule inhibitors as alternatives and their role in combination therapies.
Main Results:
- Small molecule inhibitors offer potential solutions to the limitations of mAbs, including improved bioavailability and permeability.
- Combination therapies involving ICIs and small molecule agents are under investigation to enhance treatment efficacy.
- Various molecular targets are being explored for small molecule inhibitor development in cancer treatment.
Conclusions:
- Small molecule inhibitors represent a promising advancement in anti-cancer immunotherapy, addressing key limitations of current antibody-based treatments.
- Further research and clinical trials are essential to fully realize the therapeutic potential of small molecule inhibitors, particularly in combination strategies.
- Targeting the TME with novel small molecule agents could lead to improved patient outcomes and reduced tumor recurrence.
Related Concept Videos
Tumor Immunotherapy
820
Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
820
Antigens Involved in Adaptive Immunity
896
An antigen is any substance the immune system identifies as foreign and potentially harmful to the body, prompting an immune response. Antigens have two functional properties: immunogenicity and reactivity. Immunogenicity is the ability of an antigen to stimulate a specific immune response. At the same time, reactivity describes the antigen's ability to react with the cells and antibodies produced in response to it.
Complete Antigens
Complete antigens possess both immunogenicity and...
Complete Antigens
Complete antigens possess both immunogenicity and...
896
Targeted Cancer Therapies
8.1K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
8.1K
Microorganisms in Medicine and Therapeutics
627
Microorganisms play a fundamental role in vaccine development, gene therapy, and therapeutic production. Their biological properties are harnessed to advance medicine and public health. Beyond immunization, microorganisms contribute to gut health, antibiotic synthesis, and genetic disease treatment.Live Attenuated and Inactivated VaccinesLive attenuated vaccines, such as the measles, mumps, and rubella (MMR) vaccine, utilize weakened forms of pathogens to closely resemble natural infections.
627
Vaccinations
49.1K
Overview
49.1K
Combination Therapies and Personalized Medicine
5.6K
Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
5.6K


