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In: Biology

Prodrugs: a. What are the attributes of a good prodrug? b. Cite 4 examples of marketed...

Prodrugs:

a. What are the attributes of a good prodrug?

b. Cite 4 examples of marketed prodrugs?

Solutions

Expert Solution

ANSWER:

Attributes of a Good Prodrug:

An ideal prodrug are expected to feature the following properties:

  • Have an appreciable chemical stability across a pH Range (stability at physiological pHs).
  • Weak (or no) activity against any pharmacological targets.
  • Adequately high aqueous solubility and passive permeability.
  • The released carrier is non-toxic (have no unwanted pharmacological effects).
  • Have resistance to the process of hydrolysis during the phase of absorption.
  • High transcellular absortion.
  • Post-absorption, rapid and quantitative breakdown to yield parent (active) components.

Examples for marketed Prodrugs:

  • Fospropofol (Anaesthetic)
  • Lansoprazole (proton pump inhibitors)
  • Valacyclovir (antiviral)
  • Nepafenac (anti-inflammatory)

other examples may include dabigatran etexilate (approved in 2010), isavuconazonium (2015), selexipag (2015), latanoprostene bunod (2017), benzhydrocodone (2018) etc

gladiator answered 1 year ago
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