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Related Concept Videos

Tumor Immunotherapy01:27

Tumor Immunotherapy

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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.
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Targeted Cancer Therapies02:57

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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...
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Combination Therapies and Personalized Medicine02:50

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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.
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Drugs Used in Lower Respiratory Disorders: Overview01:17

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Lower respiratory tract disorders present challenges that often require skilled and nuanced approaches for effective management. Common ailments, such as asthma and chronic obstructive pulmonary disease (COPD), have prompted the development of intricate treatment strategies involving bronchodilators and anti-inflammatory drugs, each tailored to ease breathing and revitalize the lungs.
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Crohn's disease is an inflammatory bowel disorder marked by chronic inflammation of the GI tract. Various treatment strategies for Crohn's disease are employed, such as immunomodulatory agents, glucocorticoids, and biologics or anti-TNF therapy. Azathioprine (Imuran), a commonly used immunomodulatory drug for Crohn's disease, is converted in the body to mercaptopurine, which inhibits purine biosynthesis and cell proliferation. Both are utilized in severe cases of Inflammatory Bowel...
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Targets for Drug Action: Overview01:26

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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Related Experiment Video

Updated: Aug 26, 2025

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
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Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology

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Small-Molecule Drugs in Immunotherapy.

Xuanrun Hao1, Zhongliang Chen2,3, Haining Li1

  • 1School of Pharmacy, Chengdu Medical College, Chengdu 610500, China.

Mini Reviews in Medicinal Chemistry
|October 6, 2022
PubMed
Summary

Small molecule immunotherapies harness the immune system to fight cancer with fewer side effects than chemotherapy. This review covers advances in small molecule immune-oncology drugs, including PD-1/PD-L1 inhibitors and STING activators.

Keywords:
Cancer immunotherapyIDO inhibitorPd-1/Pd-L1 inhibitorRORγt agonistsSTING agonistsTGF- β inhibitors.inhibitors

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Area of Science:

  • Oncology
  • Immunology
  • Pharmacology

Background:

  • Immunotherapy is a growing cancer treatment modality, offering advantages over chemotherapy such as fewer side effects.
  • Small molecule immune-oncological drugs present favorable pharmacokinetic profiles, including bioavailability and tissue penetration.

Purpose of the Study:

  • To review current advancements in small molecule approaches within tumor immunology.
  • To highlight small molecules in clinical trials and preclinical studies targeting key immune pathways.

Main Methods:

  • Literature review of small molecule immune-oncology drugs.
  • Categorization of molecules based on their targets (e.g., PD-1/PD-L1, IDO, STING, RORγt, TGF-β).
  • Analysis of clinical and preclinical data for selected agents.

Main Results:

  • PD-1/PD-L1 inhibitors are a primary focus, with oral agents like CA-170 showing promise.
  • IDO inhibitors, particularly dual IDO and PD-1 inhibitors, demonstrate synergistic potential.
  • Activators of STING, agonists of RORγt, and inhibitors of TGF-β are also discussed for their roles in modulating anti-tumor immunity.

Conclusions:

  • Small molecule immunotherapies offer a promising avenue for cancer treatment.
  • Combination therapies involving immunotherapy agents are likely to enhance treatment efficacy.
  • Targeting multiple immune pathways with small molecules may overcome limitations of current treatments.