Mother Nature is a source of numerous invaluable bioactive secondary metabolites and lead molecules, which form the backbone of numerous ancient medicinal systems all around the world. Nepeta leucophylla Benth. is an aromatic medicinal plant found in the western Himalayas at elevation of >2000 m. It is one of the less explored species of the genus Nepeta found in the western Himalayas. Traditionally, the plant is used as a remedy for malarial fever and to prepare herbal tea. Plants are also used for the cure of different ailments in livestock by local tribes in Himalayas, but there is no documented proof for the same. Apart from these, N. leucophylla is also known to show antibacterial, antifungal, antiviral, antioxidant, and anticancer potential. Flavonoids, phenolic acid, terpenoids, steroids, and hydrocarbons are the key classes of secondary metabolites isolated from the different parts of the plant. This chapter represents the status of species with respect to its distribution, taxonomy, traditional uses with more emphasis on phytochemical composition, pharmacology, and future prospective.