The World Health Organization (WHO) is giving more prominence to promoting traditional medicine, particularly, in third‐world countries. The global market of medicinal plants is estimated at over US$ 60.0 billion which is expected to grow up to US$ 5.0 trillion by the year 2050. In Pakistan, the bill for the import of medicinal plants was worth US$ 31.0 million, whereas the export of medicinal plants could hardly reach US$ 6.0 million. In the world, 30% of the pharmaceutical preparations are manufactured from plants. Keeping in view the potential of the global and local market, we conducted our current research work entitled Phytochemical and pharmacological investigations of Lespedesea gerardiana” The present dissertation comprises: Pharmacological/Biological activities of crude methanolic extract (Crd. MeOH Ext.),various fractions and phytochemical study of L. gerardiana. Crd. MeOH Ext. and various fractions of the plant were investigated for various pharmacological/biological activities including, Brine‐shrimp lethality, Haemagglutination, and Insecticidal and Antioxidant assay.