Background <p>Cancer is a lethal disease worldwide that damages bodily tissues, linked with predisposing variables including inheritance, social, infections thus, requiring curative measures and behavioral modifications. But currently, researchers are working to find targeted drug therapy with limited side effects, that are associated with previous approaches. Plant based novel drug Halofuginone (HaF), by blocking prolyl tRNA synthetase exhibits promising diverse clinical activities, against fibrosis, cancer, metabolic, and infectious disorders. However, the drug is quite neurotoxic and gastrotoxic requiring thorough investigational analyses as per preclinical studies at Phase-II clinical trials.</p> Methods <p>The present study explored various databases, software and monographs to establish therapeutic aspects of this drug to address gaps by highlighting the potential impact of salt reformation on improving its properties.</p> Results <p>Hence, our study invites the researchers to look upon novel Halofuginone derivatives with other possible halogen salts like HCl, to enhance its pharmacokinetics and pharmacodynamics qualities.</p> Conclusions <p>Moreover, the study summarizes the possibilities of other formulations of Halofuginone for safe utility in pharmacotherapeutics for future research in this area, provided its toxicity concerns are adequately addressed through innovative strategies.</p> Graphical abstract <p></p>