Rose Tyler M, Baranek Monika, Kaka Maryam, Shwani Sarah
Roseman University of Health Sciences, College of Pharmacy, 10920 South River Front Parkway, South Jordan, UT 84095, USA.
J Pharm Sci. 2025 Feb;114(2):782-786. doi: 10.1016/j.xphs.2024.12.007. Epub 2024 Dec 25.
The purpose of this review is to better characterize the contribution and properties of FDA-approved drugs that can be found unmodified in nature. Defined inclusion criteria were applied to drugs identified in previous studies and in annual FDA approval reports to compile a comprehensive list of approved drugs found in nature. Databases and scientific literature were searched to identify chemical and drug properties of these entities, including chemical classes, approval years, drug indications, and approved delivery methods. A random sample of FDA-approved drugs not found in nature was also created for comparison. Drugs from nature are estimated to represent 5 % of FDA approved drugs. The most common classes of natural product drugs are alkaloids, oligopeptides, polyphenols, and polyketides. Approvals of unmodified drugs from nature have declined at a rate of about two per decade since the mid-1900s. Compared to non-natural drugs, drugs from nature are more likely to be used as antibacterials and for dermatological conditions. Natural drugs are also less likely to be delivered orally and more likely to have narrow therapeutic indexes. Given the limitations of unmodified natural products as drugs, the pharmaceutical sciences will likely continue to play an important role in improving the drug-likeness of natural scaffolds.
本综述的目的是更好地描述那些在自然界中可直接找到的、已获美国食品药品监督管理局（FDA）批准的药物的贡献和特性。将已定义的纳入标准应用于先前研究及FDA年度批准报告中所确定的药物，以编制一份自然界中已批准药物的综合清单。通过检索数据库和科学文献来确定这些药物的化学和药物特性，包括化学类别、批准年份、药物适应症以及批准的给药方式。还随机抽取了一些在自然界中未发现的、已获FDA批准的药物作为对照。据估计，来自自然界的药物占FDA批准药物的5%。天然产物药物最常见的类别是生物碱、寡肽、多酚和聚酮化合物。自20世纪中叶以来，未经修饰的天然药物的批准数量以每十年约两种的速度下降。与非天然药物相比，来自自然界的药物更有可能被用作抗菌药物以及用于皮肤病治疗。天然药物口服给药的可能性也较小，且更有可能具有较窄的治疗指数。鉴于未经修饰的天然产物作为药物存在局限性，药物科学可能会继续在改善天然药物骨架的类药性质方面发挥重要作用。
