Oncological Drugs

Subtopic:

Immunological agents

Immunological agents are a wide category of medications that alter the immune system’s activity, either by strengthening or reducing its performance.

They are akin to tools that assist your immune system in functioning more effectively or in a different manner. For instance, vaccines aid your body in combating specific illnesses (strengthening) or autoimmune drugs manage autoimmune conditions, where the immune system targets the body’s own tissues (reducing).

Types of Immunological Agents:
  1. Immunostimulants: These are medications that boost the immune system’s function, often employed when the immune system is weakened or not performing optimally.

  2. Immunosuppressants: These medications lessen or suppress the immune system’s activity, crucial for preventing transplant rejection and managing autoimmune diseases.

Examples include:

IMMUNE STIMULANTS

Interferons

interferon alfa-2b

interferon alfacon-1

interferon alfa-n3

interferon beta-1a

interferon beta-1b

interferon gamma-1b

peginterferon alfa-2a

peginterferon alfa-2b

Interleukins

aldesleukin

oprelvekin

IMMUNE SUPPRESSANTS

T- and B-Cell Suppressors

abatacept

alefacept

azathioprine

Interleukin-Receptor Antagonist

anakinra

Monoclonal Antibodies

adalimumab

alemtuzumab

basiliximab

bevacizumab

certolizumab

 

Immunostimulants

1. Interferons

Interferons: These are naturally occurring proteins produced by cells when exposed to viral infections or other triggers. Their mechanism involves disrupting viral duplication inside cells, activating immune cells such as NK cells and macrophages, and enhancing antigen presentation to lymphocytes.

DrugIndicationsTherapeutic ActionAdverse Effects
Interferon alfa-2bUsed for chronic Hepatitis C, Kaposi’s sarcoma, and malignant melanoma.Works by blocking virus multiplication, boosting the immune response, and enhancing macrophage function.May cause flu-like symptoms, bone marrow suppression, and suicidal thoughts.
Interferon alfacon-1Used for Hepatitis C.Functions to inhibit viral duplication and enhance the immune system.Can lead to headache, dizziness, bone marrow suppression, and increased sensitivity to light.
Interferon alfa-n3Used for genital warts and basal cell carcinoma.Acts by blocking viral duplication and tumor growth.May result in fatigue, loss of appetite, nausea, and vomiting.
Interferon beta-1aUsed for Multiple Sclerosis (MS).Decreases the frequency of MS clinical flare-ups and slows down disability progression in MS.Can cause reactions at the injection site, flu-like symptoms, and liver problems.
Interferon beta-1bUsed for Multiple Sclerosis (MS).Similar to Interferon beta-1a; it modulates the immune system to lessen inflammation.May cause fatigue, depression, flu-like symptoms, and liver damage.
Interferon gamma-1bUsed for Chronic Granulomatous Disease and severe Osteopetrosis.Boosts macrophage respiratory burst, leading to enhanced antimicrobial activity.Can lead to fever, rash, diarrhea, and muscle pain.
Peginterferon alfa-2aUsed for chronic Hepatitis C and B.Enhances the immune response to combat hepatitis viruses.May cause low neutrophil count, low platelet count, abnormal liver enzymes, and flu-like symptoms.
Peginterferon alfa-2bUsed for chronic Hepatitis C.Provides longer-lasting effects due to its pegylated form, enabling less frequent administration.Similar to Peginterferon alfa-2a, including blood-related toxicity and depression.

 

General Therapeutic Actions of Interferons:
  • Prevent viral replication inside host cells.

  • Stimulate cells to produce antiviral proteins, enhancing the cytotoxicity of T-cells and NK cells.

  • Inhibit tumor growth by augmenting the body’s immune response.

Pharmacokinetics of Interferons:

  • Well absorbed via subcutaneous or intramuscular injection, reaching peak plasma levels within 3-8 hours.

  • Metabolized in the liver and kidneys.

  • Primarily excreted through the kidneys.

Contraindications for Interferon Use:

  • Known allergies to interferons or any of their components.

  • Pregnancy and lactation (due to potential teratogenic effects).

  • Pre-existing cardiac conditions, especially arrhythmias and hypertension.

  • Myelosuppression.

2. Interleukins

Interleukins: Interleukins are a type of cytokine crucial for immune responses. They function by promoting the growth and multiplication of lymphocytes and other immune cells.

Cytokines: Broadly, cytokines are small proteins that facilitate communication between cells.

Imagine your immune system as a big army. Interleukins are like the signals that tell different parts of the army what to do.

Key Actions of Interleukins:

  • Activate immune cells: Direct specific cells to initiate defense against invaders.

  • Control inflammation: Help regulate the intensity of inflammatory responses to infections or injuries.

  • Promote cell growth: Assist immune cells in multiplying and strengthening.

DrugIndicationsTherapeutic ActionAdverse Effects
AldesleukinUsed for metastatic renal cell carcinoma and metastatic melanoma.Promotes the multiplication of T-cells and NK cells and enhances cell-mediated immunity against cancer.May cause capillary leak syndrome, low blood pressure, and anemia.
OprelvekinUsed to prevent severe thrombocytopenia in patients undergoing chemotherapy.Increases platelet production by stimulating megakaryocytes.Can cause fluid retention, swelling, shortness of breath, and irregular heartbeats.

 

General Therapeutic Actions of Interleukins: Interleukins enhance immune cell activity, improving the body’s ability to combat tumors and increase platelet production.

Pharmacokinetics of Interleukins:

  • Absorbed via subcutaneous injection, with peak levels occurring within hours.

  • Metabolized in the kidneys.

  • Excreted in urine.

Contraindications for Interleukin Use:

  • Allergies to interleukins or E. coli-produced products.

  • Pregnancy and lactation due to potential teratogenic effects.

  • Patients with pre-existing renal, liver, or cardiovascular impairments.

Immunosuppressants

Immunosuppressants are key medications in preventing organ rejection after transplantation and in managing autoimmune disorders. They function by suppressing the activity of the immune system. They act to reduce the immune system’s intensity, preventing excessive reactions. These drugs are vital in conditions where the body’s immune system mistakenly targets its own tissues. Cyclosporine is a frequently prescribed example of an immunosuppressant.

1. T- and B-cell Suppressors

T- and B-cell Suppressors: These agents work by decreasing the activity of T and B lymphocytes. This action diminishes the immune system’s capacity to attack transplanted organs or the body’s own tissues in autoimmune conditions.

DrugIndicationsTherapeutic ActionAdverse Effects
AbataceptRheumatoid arthritis, juvenile idiopathic arthritisBlocks T-cell activation by interacting with CD80 and CD86 on antigen-presenting cells.Headache, infections, hypertension, nausea
AlefaceptPlaque psoriasisSuppresses T-cell activation and lowers the count of T-cells.Lymphopenia, hepatotoxicity, infections
AzathioprinePrevention of kidney transplant rejection, rheumatoid arthritisReduces purine synthesis, leading to decreased T and B cell proliferation.Bone marrow suppression, hepatotoxicity, nausea

 

Therapeutic Action: These medications function by inhibiting the multiplication and activity of T and B lymphocytes, which is crucial for preventing transplant rejection and managing autoimmune diseases.

Pharmacokinetics: T- and B-cell suppressors are typically well-absorbed following oral or intravenous administration. Metabolism occurs in the liver, and excretion is mainly through the kidneys.

Contraindications:

  • Known allergy to the drug or its components.

  • Pregnancy and breastfeeding (due to potential harm to the fetus or infant).

  • Kidney or liver dysfunction.

  • Ongoing infections or diagnosed cancers.

2. Interleukin-Receptor Antagonist

2. Interleukin-Receptor Antagonists: This category of drugs functions by blocking the action of interleukins, which are vital signaling molecules in inflammation and immune responses.

DrugIndicationsTherapeutic ActionAdverse Effects
AnakinraRheumatoid arthritisBlocks the interleukin-1 receptor, reducing inflammation and halting joint damage.Headache, sinusitis, nausea, infections, injection-site reactions

 

Therapeutic Action: Interleukin-receptor antagonists work by preventing interleukins from binding to their receptors. This action leads to a reduction in inflammation and tissue damage.

Pharmacokinetics: Anakinra is given via subcutaneous injection and attains maximum blood levels within a few hours. Liver metabolism and primarily urinary excretion are the routes of elimination.

Contraindications:

  • Allergies to anakinra or products made using E. coli.

  • Pregnancy and breastfeeding (due to potential drug transfer to the baby).

  • Kidney dysfunction, existing immunosuppression, or active infections.

3. Monoclonal Antibodies

3. Monoclonal Antibodies: Monoclonal antibodies are manufactured in the lab and are designed to imitate the immune system’s ability to combat pathogens like viruses. They are highly targeted, acting like “guided missiles” of the immune system. These antibodies are engineered to precisely target and attack specific cells or molecules. They are used in the treatment of cancer, autoimmune conditions, and infections. They function like a precise sniper team, focusing on specific targets while sparing the rest of the immune system.

Monoclonal antibodies include adalimumab (Humira), alemtuzumab (Campath), basiliximab (Simulect).

Indications:

  • Prevention of renal transplant rejection

  • Treatment of B-cell chronic lymphocytic leukemia

  • Reduction of the signs and symptoms of Crohn disease

  • Treatment of paroxysmal nocturnal hemoglobinuria, to reduce haemolysis.

  • Treatment of B-cell non-Hodgkin lymphoma in conjunction with rituximab.

  • Treatment of asthma with a very strong allergic component and seasonal allergic rhinitis not occasionally controlled by common medicine.

  • Prevention of serious RSV (Respiratory syncytial virus) infection in high-risk children.

  • Treatment of metastatic breast cancer.

  • Treatment of psoriasis

DrugIndicationsTherapeutic ActionAdverse Effects
AdalimumabRheumatoid arthritis, psoriatic arthritis, ankylosing spondylitisBinds to tumor necrosis factor (TNF)-alpha, reducing its inflammatory effects.Infections, malignancies, injection site reactions
AlemtuzumabChronic lymphocytic leukemiaTargets the CD52 receptor on lymphocytes, causing cell lysis.Infusion reactions, infections, cytopenias
BasiliximabPrevention of kidney transplant rejectionBlocks the interleukin-2 receptor on T-cells, preventing T-cell activation.GI disturbances, infections, hypersensitivity

 

Therapeutic Action: Monoclonal antibodies selectively target and neutralize pathogens or inflammatory molecules, resulting in focused immune suppression.

Pharmacokinetics: These medications are typically administered intravenously. Their half-life varies depending on the specific monoclonal antibody. Metabolism and excretion occur via the reticuloendothelial system.

Contraindications:

  • Known allergy to the monoclonal antibody or murine-derived products.

  • Fluid overload.

  • Use with caution in patients with fever; manage fever before starting treatment.