Bitter gourd (Momordica charantia L.), characterized by its distinct bitterness, is valued for managing diabetes and enhancing digestive health due to its bioactive compounds. Thematic scope of this chapter encompasses historical significance, specialized post-harvest protocols for pulp, detailed nutritional composition mapping, targeted extraction methodologies for bioactive polysaccharides and protein fractions, diversified processing technologies for beverage and functional product development, physicochemical characterization and bioactive compounds extraction from seeds, multifaceted nutraceutical properties including antioxidant potential, anti-diabetic mechanisms, antimicrobial and antibacterial efficacy, tissue-healing attributes, anti-HIV and antiviral activities, anticancer and anti-tumoral effects, antihypertensive and reno-protective mechanisms. It is conveyed that integrated knowledge of bitter gourd’s therapeutic mechanisms, extraction methodologies, and product formulations can be beneficial for the healthcare professionals to understand the scientific innovations for the commercial exploitation.