R&D and Medical Affairs, Almirall US, Malvern, Pennsylvania, USA.
JDR Dermatology Research/Thomas Dermatology, Nevada, USA.
Dermatol Ther. 2022 Mar;35(3):e15275. doi: 10.1111/dth.15275. Epub 2021 Dec 30.
Tetracycline-class antibiotics are frequently prescribed by dermatologists, commonly for acne vulgaris. Gastrointestinal absorption of first and second-generation tetracycline-class antibiotics, including doxycycline and minocycline, may be reduced by co-administration with food, resulting in potentially lower clinical efficacy. Development of novel compounds and formulations that are not impacted by diet could improve compliance, absorption, and effectiveness among patients. The objective of this study is to investigate weight-based dosing protocols and the impact of food intake, including high-fat meals, on the absorption, and clinical efficacy of sarecycline, a novel oral narrow-spectrum third-generation tetracycline-class antibiotic approved by the Food and Drug Administration for acne vulgaris treatment. Data from 12 clinical studies were analyzed using population pharmacokinetic modeling, exposure-response modeling and pharmacodynamics to evaluate sarecycline dosing recommendations. The extent of exposure is estimated to decrease by 21.7% following co-administration of a sarecycline tablet with a high-fat meal. Based on the PopPK-PD model, this is equivalent to a decrease in efficacy of 0.9 inflammatory lesions, which is not clinically meaningful. Sarecycline can be administered using weight-based dosing with or without food. Co-administration with high-fat food has a limited impact on clinical efficacy. The pharmacokinetics of oral sarecycline may provide added convenience and support ease of use and improved compliance for acne vulgaris patients.
四环素类抗生素经常被皮肤科医生开给患者,通常是治疗寻常痤疮。包括多西环素和米诺环素在内的第一代和第二代四环素类抗生素,与食物同服时可能会降低胃肠道吸收,从而导致潜在的临床疗效降低。开发不受饮食影响的新型化合物和制剂可以提高患者的依从性、吸收和疗效。本研究旨在研究基于体重的给药方案以及食物摄入(包括高脂肪餐)对新型口服窄谱第三代四环素类抗生素萨瑞环素(已被食品药品监督管理局批准用于治疗寻常痤疮)吸收和临床疗效的影响。使用群体药代动力学建模、暴露-反应建模和药效学分析了来自 12 项临床研究的数据,以评估萨瑞环素的给药建议。与高脂肪餐同服时,萨瑞环素片剂的暴露程度估计会降低 21.7%。根据 PopPK-PD 模型,这相当于疗效降低 0.9 个炎症病变,这在临床上没有意义。萨瑞环素可以基于体重给药,无论是否与食物同服。与高脂肪食物同服对临床疗效的影响有限。口服萨瑞环素的药代动力学可能会为患者提供额外的便利,并支持寻常痤疮患者使用的易用性和提高依从性。