This article delves into the concepts of personalized medicine and proteoforms, emphasizing the importance of proteomics at the level of proteoforms (proteoformics) for developing new and better drugs and diagnostics. It highlights how personalized medicine can reduce adverse effects, enhance drug efficacy, and optimize treatment outcomes. The article discusses the challenges and benefits of targeting proteins through proteoformics, which involves studying the morphological diversity of proteins and their impact on physiological and pathological processes. Key aspects include the identification and quantification of proteoforms, structural analysis, functional research, and data analysis using bioinformatics and computational tools. The article also explores the historical context of drug revolutions, from penicillin and aspirin to the current era of genomics-based personalized drug therapy, which aims to revolutionize medication habits and treatment methods. It outlines the experimental procedures for analyzing proteoforms, including top-down mass spectrometry (TD-MS) and two-dimensional gel electrophoresis (2DGE) combined with mass spectrometry (2DE-MS). The article concludes by discussing the contributions of personalized drug therapy, such as improving therapeutic effects, reducing adverse reactions, optimizing drug selection and dosages, and accelerating the development of new drugs. It also addresses the relationship between personalized medicine and personalized drug therapy, emphasizing their interconnectedness and mutual benefits. Finally, the article examines current typical personalized drugs targeting proteins, including anticancer drugs, protease inhibitors, protein structure modifiers, and immunotherapeutic agents, while acknowledging the disadvantages of using proteins as personalized drug targets, such as the complexity of proteoforms and the need for further research and experimental verification.This article delves into the concepts of personalized medicine and proteoforms, emphasizing the importance of proteomics at the level of proteoforms (proteoformics) for developing new and better drugs and diagnostics. It highlights how personalized medicine can reduce adverse effects, enhance drug efficacy, and optimize treatment outcomes. The article discusses the challenges and benefits of targeting proteins through proteoformics, which involves studying the morphological diversity of proteins and their impact on physiological and pathological processes. Key aspects include the identification and quantification of proteoforms, structural analysis, functional research, and data analysis using bioinformatics and computational tools. The article also explores the historical context of drug revolutions, from penicillin and aspirin to the current era of genomics-based personalized drug therapy, which aims to revolutionize medication habits and treatment methods. It outlines the experimental procedures for analyzing proteoforms, including top-down mass spectrometry (TD-MS) and two-dimensional gel electrophoresis (2DGE) combined with mass spectrometry (2DE-MS). The article concludes by discussing the contributions of personalized drug therapy, such as improving therapeutic effects, reducing adverse reactions, optimizing drug selection and dosages, and accelerating the development of new drugs. It also addresses the relationship between personalized medicine and personalized drug therapy, emphasizing their interconnectedness and mutual benefits. Finally, the article examines current typical personalized drugs targeting proteins, including anticancer drugs, protease inhibitors, protein structure modifiers, and immunotherapeutic agents, while acknowledging the disadvantages of using proteins as personalized drug targets, such as the complexity of proteoforms and the need for further research and experimental verification.