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1.4 PHARMACOKINETICS OPTIMIZATION IN DRUG DISCOVERY

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A successful lead optimization of PK aims at maximizing the bioavailability and half‐life, reducing clearance and toxic metabolites and minimizing the risk for drug–drug and food–drug interactions. A comprehensive preclinical pharmacokinetic evaluation would ensure that compounds do not fail in the clinic (Singh, 2006). Table 1.4 summarizes the PK optimizations and describes how and why they should be done.

Physiologically Based Pharmacokinetic (PBPK) Modeling and Simulations

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