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奥拉帕利胶囊和片剂剂型在治疗卵巢癌方面的药理学问题:它们真的是同一种药物吗?

Pharmacological issues concerning olaparib capsule and tablet formulations in treating ovarian cancer: Are they really the same drug?

作者信息

Perego Gianluca, Nozza Renata, Oggionni Emanuela, Cabiddu Mary, Scolari Cinzia, Omati Elena, Castelli Emanuela A, Petrelli Fausto

机构信息

Pharmacy Unit, Asst Bergamo Ovest, University of Milan, School of Hospital Pharmacy, Milano, Italy.

Oncology Unit, Asst Bergamo Ovest, Treviglio (BG), Italy.

出版信息

J Oncol Pharm Pract. 2020 Jun;26(4):967-971. doi: 10.1177/1078155219900913. Epub 2020 Feb 10.

Abstract

Olaparib is a first-in-class PARP inhibitor that has demonstrated efficacy as maintenance therapy in patients with ovarian cancer. It has been approved as a capsule formulation and after the publication of data from SOLO2 study became available also as tablet formulation. Due to different pharmacokinetic properties, these different formulations cannot be considered bioequivalent nor interchangeable. The tablet formulation has improved bioavailability, reducing pill burden and offering a more convenient dosage regimen. Furthermore, olaparib tablet formulation had a manageable tolerability profile if compared to capsule one, with most of adverse events of mild or moderate severity. Under this light, olaparib tablet formulation is a useful maintenance strategy for recurrent, platinum-sensitive ovarian cancer, providing a more convenient dosing option than the capsule formulation.

摘要

奥拉帕利是一种一流的聚(ADP-核糖)聚合酶(PARP)抑制剂,已证明其作为卵巢癌患者维持治疗的有效性。它已被批准为胶囊制剂,在SOLO2研究数据公布后,也有片剂制剂。由于不同的药代动力学特性,这些不同的制剂不能被认为具有生物等效性,也不能相互替代。片剂制剂具有更高的生物利用度,减轻了服药负担,并提供了更方便的给药方案。此外,与胶囊制剂相比,奥拉帕利片剂制剂的耐受性易于管理,大多数不良事件为轻度或中度严重程度。鉴于此,奥拉帕利片剂制剂是复发性铂敏感卵巢癌的一种有用的维持治疗策略,比胶囊制剂提供了更方便的给药选择。

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