Rapeseed (Brassica napus L.) is a herbaceous annual plant of the Cruciferous family, the Cabbage genus. This oilseed crop is widely used in many areas of industry and agriculture. High-quality oil obtained from rapeseed can be found in many industrial food products. To date, extracts with a high content of biologically active substances are obtained from rapeseed using modern extraction methods. Brassica napus L. seeds contain polyunsaturated and monounsaturated fatty acids, carotenoids, phytosterols, flavonoids, vitamins, glucosinolates and microelements. The data in this review show that rapeseed biocompounds have therapeutic effects in the treatment of various types of diseases. Some studies indicate that rapeseed can be used as an anti-inflammatory, antioxidant, antiviral, hypoglycemic and anticancer agent. In the pharmaceutical industry, using rapeseed as an active ingredient may help to develop new forms drugs with wide range of therapeutic effects. This review focuses on aspects of the extraction of biocompounds from rapeseed and the study of its pharmacological properties.