Covering: up to March 2022Bisditerpenoids, or diterpenoid dimers, are a group of natural products with high structural variance, deriving from homo- or hetero-dimeric coupling of two diterpenoid units. They usually possess complex architectures resulting from the diversity of monomeric diterpenoids as building blocks and the dimerization processes. These compounds have attracted the attention of synthetic and biological scientists owing to the rarity of their natural origin and their significant biological activities. Herein, we provide a review highlighting some of the interesting bisditerpenoids reported since 1961 and showcase the chemical diversity in both their structures and biosynthesis, as well as their biological functions. This review focuses on the biosynthetic dimerization pathways of interesting molecules and their biomimetic synthesis, which may act as useful inspiration for the discovery and synthesis of more bisditerpenoids and further pharmacological investigations.