ABSTRACT

Introduction

Nintedanib (N.T.B) is an orally administered tyrosine kinase inhibitor that has been approved recently by U.S.F.D.A for idiopathic pulmonary fibrosis (I.P.F) and systemic sclerosis-associated interstitial lung disease (S.Sc-I.L.D). N.T.B is also prescribed in COVID-19 patients associated with I.P.F. However, it has an extremely low bioavailability of around 4.7%, and hence, researchers are attempting to address this drawback by different approaches.

Areas covered

This review article focuses on enlisting all the formulation attempts explored by researchers to increase the bioavailability of N.T.B while also providing meaningful insight into the unexplored areas in formulation development, such as targeting of the lymphatic system and transdermal delivery. All the patents on the formulation development of N.T.B have also been summarized.

Expert opinion

N.T.B has the potential to act on multiple diseases that are still being discovered, but its extremely low bioavailability is a challenge that is to be dealt with for obtaining the full benefit. Few studies have been performed aiming at improving the bioavailability, but there are unexplored areas that can be used, a few of which are explained in this article. However, the ability to reproduce laboratory results when scaling up to the industry level is the only factor to be taken into consideration.

中文翻译：

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尼达尼布给药的进展与挑战

摘要

介绍

尼达尼布 (NTB) 是一种口服酪氨酸激酶抑制剂，最近已被美国食品药品监督管理局批准用于特发性肺纤维化 (IPF) 和系统性硬化相关的间质性肺病 (S.Sc-ILD)。NTB 也用于与 IPF 相关的 COVID-19 患者。然而，它的生物利用度极低，约为 4.7%，因此，研究人员正试图通过不同的方法解决这一缺点。

覆盖区域

这篇综述文章重点介绍了研究人员探索的所有制剂尝试，以提高 NTB 的生物利用度，同时还提供对制剂开发中未探索领域的有意义的见解，例如靶向淋巴系统和透皮给药。也总结了所有关于NTB配方开发的专利。

专家意见

NTB 具有对多种尚在发现的疾病起作用的潜力，但其极低的生物利用度是获得全部益处需要应对的挑战。很少有研究旨在提高生物利用度，但仍有一些尚未探索的领域可以使用，本文对其中一些进行了解释。然而，在扩大到工业水平时重现实验室结果的能力是唯一需要考虑的因素。