Take this quiz and find out!
1. Which of the following statements regarding the pharmacokinetics and pharmacodynamics of transporters is not correct?
- Because drug exposure is greatly affected by transporters and their inhibitors, tissue concentrations and consequential pharmacodynamic concerns should be addressed during drug development.
- A composite of the physicochemical properties (e.g., solubility or logP) and the experimental observation (e.g., permeability rate or metabolic stability) can help predict probable drug disposition mechanisms of a new molecular entity via the Biopharmaceutics Drug Disposition Classification System (BDDCS).
- High permeability rate drugs (BDDCS class 1 and 2 drugs) are prone to elimination via metabolism because they have a tendency to be readily reabsorbed, and metabolism is the only elimination option.
- The free drug hypothesis, which assumes unbound concentrations are the same across a biological membrane, is valid independent of transporter effects.
2. Which of the following transporters was first described as a mechanism to confer chemoresistance to cancer cells?
- MDR1
- BCRP
- MRP1
- MRP2
3. An example of a solute carriers transporter family is:
- multidrug resistance associated protein family
- multidrug and toxin extrusion transporter family
- dicarboxylate transporter family
- heavy metal transporter family
4. Vesicle assays—To conduct vesicle studies for efflux transporters (ABC family), which of the following is a key reagent to be added in the incubation?
- Sucrose
- Calcium phosphate
- NADPH
- ATP
5. In vitro and in vivo experiment analyses require in silico tools to make in-depth observations and reasonable predictions. Which of the following statements regarding in silico method is CORRECT?
- Commercial software packages are guaranteed to work with most types of experiments via simple plug-in of the physicochemical properties of the drug-like molecules.
- PBPK modeling is the most advanced method that considers all the intrinsic and extrinsic factors; therefore, simple modification on published PBPK models works for all purposes.
- Pharmacophore modeling to design new drug substrate is completely unreliable because the transporters are expressed in the lipid bilayer membrane as dynamic parts.
- To improve applicability of in silico models, already-validated PK model components that are separately developed can be combined to avoid additional validation effort.
- None of the above. No models are perfect, but some models are useful to serve specific purposes with correct assumption and validation.
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ANSWERS: D, A, B, D, E