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. 2014 May 22;10:1197–1212. doi: 10.3762/bjoc.10.118

Table 1.

“Drugability” attributes of peptide therapeutics compared with small molecules.

Virtues Drawbacks

high activity, specificity and selectivity low metabolic stability
few side-effects short circulating half-life
no/less toxic degradation products rapid body clearance if <5,000 Da [9]
no drug–drug interactions low (oral) bioavailability, mainly parenteral administration needed
more in vivo predictability poor membrane permeability
large interaction sides sometimes reduced water solubility
biological and chemical variety risk of immunogenic effects
able to target protein–protein interactions expensive synthesis