Intracellular Pharmacokinetics of Antidiabetic Drugs: A Focused Narrative Review of Subcellular Distribution (2015–2025)
Year: 2026
Type: review
Abstract: Background/Objectives: The efficacy of antidiabetic drugs is determined by intracellular target exposure rather than solely by plasma concentrations. This review synthesizes current evidence regarding subcellular drug distribution and its clinical significance. Methods: A structured review of the literature published between 2015 and 2025 identified 73 relevant studies. Data were categorized by drug class, factors influencing distribution, and analytical methodologies. Results: Drug distribution patterns differ by class. Biguanides accumulate in mitochondria, thiazolidinediones localize in cell nuclei, and GLP-1 agonists are found in endosomes. Variations in transporter genes, such as OCT1, influence the extent of drug delivery to these subcellular targets. Conclusions: Investigations into intracellular drug movement elucidate their mechanisms of action. However, standardized human studies are required before these findings can inform clinical practice or regulatory decisions.
Source: Diseases
Author: Duaa Abdullah Bafail
Institution: King Abdulaziz University
Language: English
Subfield: Endocrinology, Diabetes and Metabolism
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $2,172
Funder: King Abdulaziz University
OpenAlex ID: W7128422102