Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A researcher extracts a biologically active compound from a medicinal
plant and observes a reproducible physiological effect in an animal
model. At this stage of drug discovery, what is the most important next
objective?
A. Submit a New Drug Application
B. Identify and characterize the active chemical constituent
,C. Begin Phase III clinical trials
D. Determine the final commercial dosage form
Correct Answer:
B. Identify and characterize the active chemical constituent
Rationale:
B is correct because an extract can contain many constituents, so
isolating and characterizing the compound responsible for the biological
activity is an essential step toward developing a defined drug candidate.
This allows investigators to determine its structure, activity, and
suitability for further optimization.
A is incorrect because an isolated lead compound still requires
extensive preclinical and clinical evaluation before an application for
marketing approval can be submitted.
C is incorrect because Phase III trials occur much later, after preliminary
human studies have established initial safety and evidence of efficacy.
D is incorrect because formulation development is important later and
depends on having a sufficiently characterized candidate.
Question 2
A medicinal chemist modifies the chemical structure of a lead
compound repeatedly and compares how each structural change alters
biological activity. Which concept is being used?
A. Structure-activity relationship analysis
B. Therapeutic drug monitoring
C. Pharmacovigilance
D. Randomization
, Correct Answer:
A. Structure-activity relationship analysis
Rationale:
A is correct because structure-activity relationship (SAR) analysis
examines how changes in molecular structure influence biological
activity. SAR information helps medicinal chemists identify structural
features that are important for potency, selectivity, and other desirable
properties.
B is incorrect because therapeutic drug monitoring involves measuring
drug concentrations in patients to guide therapy.
C is incorrect because pharmacovigilance focuses on detecting and
evaluating adverse effects after drugs are used clinically.
D is incorrect because randomization is a clinical-trial design method
rather than a medicinal chemistry strategy.
Question 3
A compound binds to a biological target with high affinity but produces
substantial toxicity in early testing. Which conclusion is most
appropriate?
A. High target affinity guarantees successful drug development
B. The compound should automatically proceed to clinical trials
C. Target binding must be considered together with selectivity and
overall drug properties
D. Toxicity proves that the biological target is invalid