ArticleThe AAPS journal2026
Calculating Receptor Occupancy using TMDD Models - What has to be Considered?
Article in The AAPS journal, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Target-mediated drug disposition (TMDD) models are often used to describe drug-receptor interactions and help derive receptor occupancy (RO), i.e., the ratio of drug-receptor complex to total receptors, which is important for understanding drug responses especially in early clinical development. A full TMDD model can be complex, and data may not always be sufficient for fitting the model. In such cases, approximations of the full TMDD model (e.g., Michaelis-Menten, rapid-binding or quasi-steady-state models) are used, and RO is calculated often using the Michaelis-Menten constant (
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