Drug Discovery Review 2

Classifying a drug is difficult because:

• Drugs can have multiple physiological effects.

• Drugs can be sorted by the receptor they target but most consumers don’t understand receptor biology.

• Two chemically similar drugs can have different effects.

• All of these are true.

An antibiotic can take billions of dollars to come to market but resistance may be developed in about five years. Based solely on economics, this drug is:

• Economical and desirable.

• Economical and undesirable.

• Uneconomical and undesirable.

• Uneconomical and desirable.

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Why might it be important to alter a compound that perfectly binds to its target receptor?

• To increase its affinity.

• To bypass metabolic pathways.

• If it already binds perfectly, it does not need to be altered.

• None of these are true.

Which of the following statements best describes the importance of optimizing binding affinity in drug design?

• A high binding affinity is always preferred as it ensures that the drug will be effective at extremely high doses, increasing its market value.

• Optimizing binding affinity is crucial because it allows for the drug to achieve its therapeutic effects at lower concentrations, potentially reducing the risk of side effects.

• Low binding affinity is preferred for all drugs because it ensures quick dissociation from the target, minimizing potential toxicity.

• Binding affinity is not a significant consideration in drug design, as the body's immune system ultimately determines the drug's efficacy.

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In class, we discussed fentanyl and carfentanil. The only difference between the two is carfentanil has an ester group; carfentanil is more lethal than fentanyl at lower doses. Why?

• The ester group is an additional functional group which increases its affinity in opioid receptors.

• This is not significant, but it is a cool fact.

• The additional ester group adds a functional group which lowers its affinity in opioid receptors.

• The ester group makes no difference as both drugs are deadly; they have the same physiological effect.

True or False: Drugs that interact with the same family of receptors must have similar affinities.

• True

• False

In the Drug Discovery lab, do we use the target selection method or phenotypic screening method? Why?

• Target selection, because it proves that manipulating the molecular target can provide therapeutic benefit for patients.

• Phenotypic screening, because it proves that the compounds are able to provide a therapeutic benefit using an in vivo model

• Target selection, because it can provide information of the complex biological interactions that occur, for example: when a lower dose of a drug performs better than a higher dose

• Phenotypic screening, because it can capture the biological complexity of a compound and identify if a compound has the desired phenotype of a potential antibiotic

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Which of the following statements best describes why the therapeutic index (TI) is an important factor when comparing potential antibiotics?

• A high therapeutic index indicates that the antibiotic is more likely to cause adverse side effects.

• A low therapeutic index means that the antibiotic is more effective at lower doses.

• A high therapeutic index indicates a large margin between effective and toxic doses, making the antibiotic safer for patient use.

• A low therapeutic index suggests the antibiotic has a lower risk of resistance development.

Which of the following is the equation for determining therapeutic index?

• TI= TD50-ED50

• TI= ED50-TD50

• TI= TD50/ED50

• TI= ED50/TD50

Calculate the therapeutic index.

• 1.79

• 0.56

• 2.67

• 1.24