Spine gourd (Momordica dioica Roxb.), also known as teasel gourd, is a dioecious climbing creeper native to tropical regions and is known for its bitterness attributed to cucurbitacins, with emerging significance in natural remedy development. This chapter covers nutritional and biochemical composition, bioactive compounds, and health benefits from fruits, leaves, seeds, and roots, including anti-tumor and immunomodulatory properties. Comprehensive framework includes foundational background, integrated nutritional and biochemical profiling across plant tissues, systematic bioactive compound identification and characterization, nutraceutical properties documentation with targeted health benefits extraction from distinct fruit, leaf, seed, and root, assessment of miscellaneous therapeutic applications, specialized post-harvest management and advanced processing technologies. It is explored that strategic alignment with global pharmaceutical and nutraceutical market demands can be effectively achieved by researchers and industry professionals through engagement with future research directions presented in this chapter.