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. 2022 Feb 24;111(4):774–785. doi: 10.1002/cpt.2548

Table 3.

PET outcome measures for calculation or estimation of target occupancy

Outcome measure Estimation
Definition Rate constants Distribution volumes Occupancy calculation
BP ND (specific to nondisplaceable binding potential) B max/K Df ND k 3/k 4 a V T/V ND − 1 b BP ND baseline − BP ND drug / BP ND baseline
V T V S+V ND K 1/k 2 (1+k 3/k 4) V T drug − V T baseline = OCC ● (V T − V ND)
λk3 c λ = K 1/k 2 K1/k2  ● k 3 λk3  baseline − λk3  drug / λk3  baseline

B max, max number of available receptors(targets); K D, dissociation rate constant; PET, positron emission tomography; V ND, nondisplaceable distribution volume (usually measured in a reference region); V S, distribution volume of the radioligand bound to the target.

a

k 3/k 4 can be estimated with 2‐tissue compartment model (TCM) or with simplified reference tissue model (SRTM).

b

V T and V ND can be estimated with 1‐TCM or 2‐TCM or with linear or multilinear graphical analysis (Logan plot or multilinear analysis) or with reference Logan or MRTM in case a reference region in the brain is present.

c

λk3 is the outcome measure conventionally used in case of an irreversible radioligand.