Modifying structures to improve PK Background: A CL vs. Vd plot is an excellent tool for providing insight into how a drug's structure might be modified in order to optimize its pharmacokinetics. Instructions: Answer the questions below. Learning Goal: To learn how to modify a drug or lead in order to achieve desired pharmacokinetic properties. Daptomycin is a large antibiotic. Daptomycin violates Lipinski's rules in just about every way possible. Its molecular weight is 1,620 g/mol, well above the 500 g/mol limit of Lipinski. Daptomycin also has far more than 5 hydrogen bond donors and 10 hydrogen bond acceptors. Based on these traits, one might expect that daptomycin has a very low oral bioavailability. That expectation is correct. Daptomycin cannot be formulated as an oral drug and is instead administered intravenously. (See structure on following page.) Please complete the online exercise. OPTIONAL‐Please participate in the online discussion forum.
Chapter 8 ‐ Metabolism Introduction to Chapter 8 Chapter 8 contains six subsections.
Phase I Pt 1
Phase I Pt 2