Ginkgo biloba (GB) has enormous bioactives with anti‐bacterial, anti‐oxidant, anti‐cancer, and immune‐stimulating properties, with global sales exceeding $10 billion. The terpene trilactones (ginkgolides A, B, and C) and flavonoids (mostly quercetin, isorhamnetin, and kaempferol) have received the most significant focus in GB research to date, whereas other bioactive compounds such as ginkgols and bilobols with various bioactivities such as anti‐viral, anti‐oxidant, and anti‐tumor actions have received less attention. Therefore, for the first time, this review focused on GB ginkgols, bilobols extraction, and bioactivities. This review showed that petroleum ether and acetone extraction had successfully extracted ginkgols and bilobols. Furthermore, bioactivities such as anti‐tumor activity and so on have been demonstrated for ginkgols, and bilobols, providing theoretical justification for ginkgols and bilobol as raw material for nutraceuticals, functional foods, pharmaceuticals, and cosmeceuticals. Future research could look into other biological applications (such as anti‐oxidant, antitoxins, anti‐radiation, anti‐microbial, and antiparasite) and their applications in the pharmaceutical, cosmetic, and nutraceutical industries. Besides, the primary research should be on developing green and effective methods for preparing ginkgols and bilobols and fully utilizing their pharmacological activity. This will also provide a new avenue for efficiently utilizing these bioactive compounds.