L10 INTRO TO BIOLOGICALS

Questions and Answers

What is one advantage of recombinant insulin over traditional methods?

Recombinant insulin is much easier to purify.

How can recombinant proteins like insulin be modified for faster absorption?

Insulin can be modified, such as insulin lispro, to prevent dimerization, allowing for faster absorption.

What is the purpose of creating long-acting insulin analogues like glargine?

Long-acting insulin analogues like glargine are designed to form aggregates for slower absorption.

What genetic condition primarily affects blood clotting and is linked to Factor VIII or IX mutations?

Haemophilia. Signup and view all the answers

What major concern arose from the purification of clotting factors from human plasma prior to the introduction of recombinant forms?

Contamination with viruses like HIV and Hepatitis C was a major concern. Signup and view all the answers

Why is screening essential for blood donors providing plasma for therapeutic use?

Screening is essential to prevent contamination and ensure the safety of clotting factors. Signup and view all the answers

What differentiates fully synthetic vaccines from biologicals?

Fully synthetic vaccines are not biologicals as they are entirely man-made. Signup and view all the answers

In which year did the replacement of clotting factors from human sources with recombinant forms begin?

<ol start="1984"> <li></li> </ol> Signup and view all the answers

What is the primary therapeutic category of adalimumab and what is its trade name?

Adalimumab is an anti-TNFα therapeutic antibody, and its trade name is Humira. Signup and view all the answers

Explain the role of B lymphocytes in the production of antibodies.

B lymphocytes are responsible for producing antibodies, with each B cell generating a unique antibody specific to an antigen it encounters. Signup and view all the answers

Identify the drug associated with the trade name Keytruda and its mechanism of action.

Keytruda is associated with pembrolizumab, which acts as a programmed cell death protein 1 (PD-1) inhibitor. Signup and view all the answers

How do therapeutic antibodies like Rituximab function in cancer treatment?

Therapeutic antibodies like Rituximab bind to specific antigens on cancer cells, flagging them for destruction by the immune system. Signup and view all the answers

Which drug ranks fifth in sales in 2021 and what is its therapeutic indication?

The drug ranked fifth is ustekinumab, which is indicated for the treatment of psoriasis and Crohn's disease. Signup and view all the answers

Describe how therapeutics like etanercept mimic or obstruct biological pathways.

Etanercept mimics the action of TNFα, acting as a decoy receptor to prevent this cytokine from binding to its actual receptors. Signup and view all the answers

What is the main purpose of the variable domain of an antibody?

The variable domain of an antibody specifically binds to foreign antigens, which is crucial for the antibody's antigen recognition. Signup and view all the answers

What therapeutic action does dulaglutide serve and what class of drug is it?

Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used primarily in type 2 diabetes treatment. Signup and view all the answers

What was the leading drug by sales in 2021 and how much did it generate?

The leading drug was adalimumab, generating $20.69 billion. Signup and view all the answers

Describe the method of variolation and its historical significance.

Variolation involved inserting powdered scabs from smallpox patients into skin scratches to induce immunity, significant for contributing to the eradication of smallpox. Signup and view all the answers

Which drug ranks second in sales in 2021, and what is its trade name?

Pembrolizumab ranks second with the trade name Keytruda. Signup and view all the answers

What year did smallpox get eradicated, and what fundamental technique helped achieve this milestone?

Smallpox was eradicated in 1980, largely due to vaccination derived from variolation techniques. Signup and view all the answers

Identify the drug with the lowest sales in the top 12 drugs listed and its trade name.

The drug with the lowest sales is ibrutinib, marketed as Imbruvica, with $6.47 billion. Signup and view all the answers

What were the estimated annual deaths from smallpox in 18th century Europe?

Smallpox caused approximately 400,000 deaths annually in 18th century Europe. Signup and view all the answers

Mention the combined drug that ranking seventh in 2021 sales and briefly describe its usage.

The combined drug bictegravir/emtricitabine/tenofovir alafenamide, marketed as Biktarvy, is used for HIV treatment. Signup and view all the answers

Name one drug from the list that is primarily an anticoagulant and its sales figure.

Rivaroxaban, sold as Xarelto, is an anticoagulant with sales of $7.52 billion. Signup and view all the answers

What historical event in 1901 is associated with the first Nobel Prize in Medicine?

Emil von Behring was awarded the first Nobel Prize in Medicine for his work on diphtheria antitoxin. Signup and view all the answers

What is the mechanism of action for recombinant proteins used as drugs?

They substitute the function of a protein that is absent or not functioning properly in the body. Signup and view all the answers

Who were the scientists that identified insulin and when did this occur?

Insulin was identified by Frederick Banting and Charles Best between 1920 and 1921. Signup and view all the answers

What type of insulin was used to treat Type I Diabetes Mellitus before the introduction of recombinant insulin?

Cow or pig insulin was used as treatment until 1982. Signup and view all the answers

What major advantage does recombinant insulin have over its animal-derived predecessors?

Recombinant insulin has increased purity and less immunogenicity. Signup and view all the answers

What contribution did James Gillray’s work in 1802 make to discussions about biologicals?

Gillray remarked that biological interventions are not new, highlighting a historical context for vaccines and biologicals. Signup and view all the answers

What role do proteins isolated from tissue play in medical applications?

They can be used as drugs when injected to provide therapeutic effects. Signup and view all the answers

What are some examples of biologicals mentioned in the content?

Examples include insulin, erythropoietin, blood factors, interferons, and growth factors. Signup and view all the answers

What is one major disadvantage of biologicals compared to small molecules in terms of administration?

Biologicals need to be injected, while small molecules can often be taken orally. Signup and view all the answers

Why is the production of biologicals considered laborious and costly?

The production via mammalian cells is slow and typically yields only a few kilograms per year. Signup and view all the answers

Describe one way the efficacy of biologicals can vary among patients.

Efficacy may depend on the patient's immune cells, such as the presence of anti-drug antibodies. Signup and view all the answers

What is the implication of biologicals having a shorter shelf-life?

Biologicals need to be stored very carefully to prevent protein degradation, impacting their availability. Signup and view all the answers

How does the half-life of biologicals differ among various types, such as insulin and therapeutic antibodies?

Insulin has a short half-life, whereas therapeutic antibodies can have a very long half-life. Signup and view all the answers

What is a safety concern associated with biologicals, and how does it differ from traditional pharmaceuticals?

Biologicals have increased immunogenicity, leading to allergic reactions, but they generally have no drug-drug interactions. Signup and view all the answers

Study Notes

Top Selling Drugs of 2021

Adalimumab (Humira): Highest sales at $20.69 billion.
Pembrolizumab (Keytruda): Second most sold with $17.18 billion.
Lenalidomide (Revlimid): Third with $12.82 billion in sales.
Additional notable drugs include Apixaban (Eliquis) at $10.76 billion and Ustekinumab (Stelara) at $9.13 billion.
Biktarvy and Rivaroxaban (Xarelto) also ranked high, with sales of $7.81 billion and $7.52 billion, respectively.

Historical Context of Biologicals

Variolation: Originating in China during the 10th century, involved inserting powdered smallpox scabs to induce immunity.
Smallpox Eradication: Achieved in 1980, previously caused 400,000 deaths annually in 18th century Europe.
Early Biologicals: First Nobel Prize in Medicine awarded in 1901 to Emil von Behring for developing diphtheria antitoxin.

Production and Functions of Recombinant Proteins

Includes therapeutic proteins like insulin, erythropoietin, and blood factors.
Process utilizes isolated proteins from animal tissues or engineered cells in vitro.
Acts as substitutes for non-functioning or absent natural proteins in patients.

Insulin Information

Insulin Discovery: Identified by Banting and Best between 1920-1921; first human treatment occurred in 1922 with ox-pancreas extract.
Recombinant Insulin: Available since 1982, leading to increased purity and reduced allergenic response.
Development of insulin analogues such as Lispro (Humalog) for fast action and Glargine (Lantus) for prolonged action.

Treatment of Hemophilia

Caused by mutations in Factor VIII or IX leading to clotting issues.
Initial treatments used clotting factors from human plasma, replaced by recombinant forms in 1984 to avoid contamination risks.

Importance of Biologicals

Are vital in modern medicine for treating various conditions but have unique challenges.
Difficult to produce at scale, require precise handling and storage to maintain efficacy.

Therapeutic Antibodies

Produced by B lymphocytes; bind specifically to foreign molecules (antigens).
Therapeutic antibodies can mimic or block endogenous pathways for treatment.
Examples include Etanercept and Dulaglutide, which target specific receptors for functional effects.

Challenges of Biologicals

Large molecular size leads to poor gut absorption – requires injections.
Production is costly and complex, often with a shorter shelf-life than small molecules.
Potential for increased immunogenicity and allergic reactions.

Pharmacological Aspects

Half-Life Variation: Ranges widely from short (insulin) to long (therapeutic antibodies).
Safety profile includes reduced toxicity but may trigger immune responses due to their complexity.

These notes encapsulate essential facts regarding the top-selling pharmaceuticals, historical developments in biological therapy, their production, and associated challenges.

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