Lipinski's rule of five, Lecture notes of Pharmaceutical Chemistry

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Lipinski's rule of five

Lipinski's rule of five also known as the Pfizer's rule of five

or simply the

Rule of five (RO5) is a rule of thumb to evaluate drug

likeness or determine if a chemical compound with a

certain pharmacological or biological activity has

properties that would make it a likely orally active drug

in humans. The rule was formulated by Christopher A.

Lipinski in 1997, based on the observation that most

medication drugs are relatively small and lipophilic

molecules [Lipinski et al. 1997, 2001 & 2004].

How this rule benefits your project? The rule describes molecular properties important for a drug’s pharmacokinetics in the human body, including their absorption, distribution, metabolism, and excretion (“ADME”). However, the rule does not predict if a compound is pharmacologically active. This rule helps Pharmaceutics/Industrial Pharmacy students in proper selection of the drug and knowing whether the drug is suitable for oral formulations. For Medicinal chemistry students involved in drug designing, CADD, understanding this rule will help you a lot in designing suitable homologues of rugs and fine tuning your drug with suitable modifications

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