The use of herbal formulations for holistic treatment of lifestyle/ non-communicable diseases and even treating infectious diseases is increasing day by day. Various plants are investigated for their pharmacological potentials. As cancer is the second leading cause of death globally and use of chemical therapeutics suffers from some drawbacks like poor therapeutic performance, multi-drug resistance, and fatal side effects. Finding herbal remedy may overcome these problems, forcing researchers to plant diversity in the treatment of various cancers. The Lepidagathis lutea Dalzell (Acanthaceae) is one of the unexplored endemic plant species to the northern Western Ghats of India. So, the aim of this study is to explore the plant as per modern science. The prepared extract was investigated for broad range phytoceuticalsand tested for itsanti-cancer activity against breast cancer, anti-inflammatory, and anthelmintic activity. The methanolic extract of Lepidagathis lutea Dalzell showed the presence of alkaloids, glycosides, carbohydrates, flavonoids, phytosterol, saponins, and tannins. This extract demonstrated considerable anti-inflammatory and anthelmintic activity. Additionally, the extract showed momentous cytotoxicity against breast cancer (MCF-7) cells with IC50 value of 46.14 μg/mL. Thus, Lepidagathis luteaDalzell is observed as promising herbal remedy for treatment of cancer, inflammation, and helminth infections.