Table 1.

PK-PD model components and related mechanisms of action of drugs.

Drug	PK model components	PD model components	Contribution of PK-PD modeling
Paliperidone palmitate	One-compartment model with First-order elimination First-order absorption Zero-order absorption Flip-flop kinetics	Dopamine D2 receptor occupancy regulation (Kapur et al., 2000)	Optimized formulation and dose regimen Accelerated the clinical trial
Liposomal doxorubicin	Two-compartment model for doxorubicin One-compartment model for liposome Flip-flop kinetics	Biophase model (Sheiner et al., 1979) Cell-killing kinetic model (Jusko, 1973)	Evaluated the influence of drug-, carrier-, and system-specific parameter on anti-tumor efficacy
Erythropoiesis stimulating agents	Two-compartment model First-order absorption Flip-flop kinetics TMDD model (Mager and Jusko, 2001a)	The operational model of agonism (Black and Leff, 1983) Precursor-Pool dependent indirect response model (Sharma et al., 1998) Transit compartment model (Mager and Jusko, 2001b)	Quantified minimal-effect concentration Explained the relationship between in vivo binding affinity and effect
Brentuximab-vedotin	Two-compartment model with first-order elimination	Emax model (Wagner, 1968) Biophase model (Sheiner et al., 1979) Transit compartment model (Mager and Jusko, 2001b)	Predicted the clinical response by preclinical data