Monday, January 8, 2018

Lipinski Rules


Common routes of drug administration include - oral, nasal, sublingual, inhalation etc.  However, when patient convenience is considered, oral drug administration is the best way.

The below rules are principally from highly publicized work of Pfizer's Chris Lipinski.

A molecule has higher chances to be successful as oral drug (like tablets, capsules, emulsions, suspensions etc) if it satisfies Lipinski's 'rule of 5'.  Remember that, there are only 4 rules - but go by the name 'rule of 5' (not 5 rules).  These four rules are physicochemical properties of that molecule;  


Numbers shown above (5, 10, 500 and 5) are all multiples of 5; therefore the name 'rule of 5'. 

As mentioned above, these rules will help us to know if the drug can be made into oral formulations.   Remember that, by just satisfying these rules a compound doesn't become pharmacologically active.   However, compounds satisfying these rules have great chance of good pharmacokinetics, ADME profile.

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