Department of Pharmaceutics, Faculty of Pharmacy, Parul University, Vadodara, India.
Recent Pat Anticancer Drug Discov. 2021;16(3):333-349. doi: 10.2174/1574892816666210120113256.
Pemetrexed is a folate analogue metabolic inhibitor for mammalian cells. Pemetrexed is toxic to several cancer cells by interfering with their new biosynthesis of nucleotides, thus causing cell apoptosis. Presently, Pemetrexed is given to patients with Non-Small Cell Lung Cancer (NSCLC).
This review focuses on the recent patents of Pemetrexed. This assessment includes patents grouped in segments like crystalline form patent, composition related patents, product patents, as well as a method of treatment. The aim of this review is to simplify inventors with existing patents in a single place.
Data were searched from several available databases, including paid databases which include Orbit® and SciFinder®. Free databases include Worldwide Espacenet® (EPO), Patentscope® (WIPO), InPASS (Indian patent database) and Google Patents.
Some new polymorph and composition-related inventions of Pemetrexed have been recently patented as its orange-book listed patents will soon expire in May 2022. Further, because of the problem of oxidation through the development and continuing storage of Pemetrexed composition, several excipients are experimented with within these patents to stabilize the same. Nevertheless, there is a need for further development of an improved composition of Pemetrexed with improved characteristics.
Wide research has been conducted on different processes for preparing Pemetrexed and formulation thereof. Such type of active research may clear the track for the generic companies in the United States, producing the formulation at low prices and providing universal health care at economical prices.
培美曲塞是一种叶酸类似物代谢抑制剂，可抑制哺乳动物细胞的核苷酸从头合成，从而导致细胞凋亡。目前，培美曲塞被用于治疗非小细胞肺癌（NSCLC）患者。
本综述重点介绍了培美曲塞的最新专利。这些评估包括按结晶形式专利、组合物相关专利、产品专利以及治疗方法等进行分组的专利。本综述的目的是将现有专利集中在一个地方，为发明者提供便利。
数据从多个可用数据库中检索，包括付费数据库，如 Orbit® 和 SciFinder®；免费数据库包括 WorldWide Espacenet®（EPO）、Patentscope®（WIPO）、InPASS（印度专利数据库）和 Google Patents。
由于橙皮书中列出的专利将于 2022 年 5 月到期，因此最近有一些培美曲塞的新多晶型物和组合物相关发明已获得专利。此外，由于培美曲塞组合物在开发和持续储存过程中存在氧化问题，这些专利中尝试了几种赋形剂来稳定其性质。然而，仍需要进一步开发具有改进特性的培美曲塞改良组合物。
人们对制备培美曲塞及其制剂的不同工艺进行了广泛研究。这种积极的研究可能为美国的仿制药公司铺平道路，以低廉的价格生产制剂，并以经济实惠的价格提供全民医疗保健。
