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