Bispecific antibodies (bsAbs), which is capable of simultaneous binding to two different targets, are considered the most promising solution to increase therapeutic activity by retargeting a large variety of payloads to cancer cells. However, the potential application of those antibody formats has been significantly limited due to the difficulty in producing large amounts of homogenous preparations of bispecific antibodies; none of them has met so far all the requirements to become a standard format for clinical applications. Being the smallest fully functional antibody fragments, nanobodies (single domain antibodies) have many outstanding physical properties such as high production yields and good stability, and may accelerate the way toward this goal.