Chia seed oil (CSO) has been recently gaining tremendous interest as a functional food. The oil is rich in with polyunsaturated fatty acids (PUFAs), especially, alpha linolenic acid (ALA), linoleic acid (LA), tocopherols, phenolic acids, vitamins, and antioxidants. Extracting CSO through green technologies has been highly efficient, cost-effective, and sustainable, which has also shown to improve its nutritional potential and proved to be eco-friendly than any other traditional or conventional processes. Due to the presence of valuable bioactive metabolites, CSO is proving to be a revolutionary source for food, baking, dairy, pharmaceutical, livestock feed, and cosmetic industries. CSO has been reported to possess antidiabetic, anticancer, anti-inflammatory, antiobesity, antioxidant, antihyperlipidemic, insect-repellent, and skin-healing properties. However, studies on toxicological safety and commercial potency of CSO are limited and therefore the need of the hour is to focus on large-scale molecular mechanistic and clinical studies, which may throw light on the possible translational opportunities of CSO to be utilized to its complete potential. In this review, we have deliberated on the untapped therapeutical possibilities and novel findings about this functional food, its biochemical composition, extraction methods, nutritional profiling, oil stability, and nutraceutical and pharmaceutical applications for its health benefits and ability to counter various diseases.