Peptide Pharmacology

Understanding the pharmacological behavior of peptides — how the body affects the peptide and how the peptide affects the body — is critical for therapeutic development. This section covers PK/PD principles specific to peptide drugs.

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Peptide Pharmacokinetics

Absorption, distribution, metabolism, and excretion (ADME) of therapeutic peptides, including compartmental modeling and key PK parameters.

→ Volume of distribution and clearance

→ Half-life determinants for peptides

→ Non-compartmental vs compartmental analysis

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Peptide Pharmacodynamics

Concentration-effect relationships, efficacy and potency (EC₅₀, Emax), receptor occupancy theory, and PK/PD modeling for peptide drugs.

→ Hill equation and sigmoid Emax models

→ Receptor occupancy-biomarker relationships

→ Therapeutic index and safety margins

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ADME Properties of Therapeutic Peptides

Peptide-specific ADME considerations — proteolytic stability, renal clearance, tissue penetration, and metabolic pathways unique to peptide drugs.

→ Protease-mediated degradation pathways

→ Renal filtration and reabsorption

→ Tissue distribution determinants

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Peptide Bioavailability Strategies

Approaches to improve peptide bioavailability — chemical modifications, formulation technologies, and prodrug strategies for enhanced systemic exposure.

→ PEGylation and lipidation

→ Cyclization and stapling

→ Permeation enhancers and carriers

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Peptide Drug–Drug Interactions

Mechanisms of peptide drug interactions — CYP enzyme modulation, transporter-mediated interactions, protein binding displacement, and pharmacodynamic interactions.

→ CYP induction and inhibition by peptides

→ Drug transporter interactions (OATP, P-gp)

→ Regulatory DDI study requirements