This article reviews the impacts on the in vivo prediction of oral bioavailability (BA) and bioequivalence (BE) based on Biopharmaceutical classification systems (BCS) by the food-drug interaction (food effect) and the gastrointestinal (GI) environmental change. Various in vitro and in silico predictive methodologies have been used to expect the BA and BE of the test oral formulation. Food intake changes the GI physiology and environment, which affect oral drug absorption and its BE evaluation. Even though the pHs and bile acids in the GI tract would have significant influence on drug dissolution and, hence, oral drug absorption, those impacts largely depend on the physicochemical properties of oral medicine, active pharmaceutical ingredients (APIs). BCS class I and III drugs are high soluble drugs in the physiological pH range, food-drug interaction may not affect their BA. On the other hand, BCS class II and IV drugs have pH-dependent solubility, and the more bile acid secretion and the pH changes by food intake might affect their BA. In this report, the GI physiological changes between the fasted and fed states are described and the prediction on the oral drug absorption by food-drug interaction have been introduced.

Belumosudil is a selective rho‐associated coiled‐coil‐containing protein kinase 2 inhibitor in clinical use for the treatment of chronic graft‐versus‐host disease. The current tablet formulation may be inappropriate for children or adults with dysphagia and/or upper gastrointestinal manifestations of chronic graft‐versus‐host disease. This study (NCT04735822) assessed the taste and palatability of oral suspensions of belumosudil, evaluated the relative bioavailability of an oral suspension versus the tablet formulation, and characterized the effect of food on the pharmacokinetics of an oral suspension. Addition of sweetener and/or flavor vehicle improved the taste. Relative bioavailability of 200‐mg doses of the oral suspension and tablet in the fed state was similar for belumosudil and its metabolites (KD025m1 and KD025m2), but absorption was faster with the oral suspension (median time to maximum concentration: 2 vs 3 hours). Administration of the oral suspension with food increased exposure compared with fasted administration, with maximum observed concentration being increased by 16% and area under the concentration‐time curve from time 0 to the last measurable concentration (AUC0‐last) by 19%. Safety and tolerability were consistent with the known safety profile of belumosudil. These results may support administration of a 200‐mg belumosudil oral suspension with or without food.

<h4>Background</h4>Food-drug interactions are common in orally administered therapies. In order to achieve optimal therapeutic efficacy and safety, it is important for patients to understand the most appropriate way to take their medications in accordance with their diet.<h4>Objectives</h4>To evaluate the impact of food on the oral bioavailability of novel cardiovascular and antidiabetic drugs, including sacubitril/valsartan, direct oral anticoagulants, sodium-glucose cotransporter-2 inhibitors, semaglutide, vericiguat, pitavastatin, and bempedoic acid.<h4>Methods</h4>PubMed, Scopus, and Cochrane Library databases were searched from inception to May 2024, following the guidelines of the PRISMA-ScR (Preferred Reporting Items for Systematic Reviews and Meta-Analyses Extension for Scoping Reviews) statement. The search strategy employed keywords including 'food drug interactions', 'food effect', 'bioavailability', and 'bioequivalence', combined with the names of the investigated drugs. Eligible publications comprised clinical pharmacokinetic studies and randomized clinical trials evaluating the effect of food on drug bioavailability.<h4>Results</h4>A total of 36 publications met the inclusion criteria. For most drugs, food was found to reduce the maximum concentration and delay the rate of absorption of the active substance without significantly affecting overall drug exposure. Therefore, these drugs can generally be administered regardless of meals. Semaglutide is recommended to be administered on an empty stomach, and pitavastatin demonstrated higher bioavailability in the fasted state. In contrast, vericiguat and higher doses of rivaroxaban are better absorbed when taken with food. For patients with swallowing difficulties, rivaroxaban, apixaban, and edoxaban may be crushed and administered either via a nasogastric tube or orally mixed with applesauce.<h4>Conclusion</h4>For a substantial proportion of novel cardiovascular and antidiabetic therapies, dosing without strict regard to meals is supported by available evidence. This level of flexibility may facilitate patient adherence and contribute to improved therapeutic outcomes in clinical practice.

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