Owing to its unique physicochemical properties such as high surface area, notable biocompatibility, robust mechanical strength, high thermal conductivity, and ease of functionalization, 2D-layered graphene has received tremendous attention as a futuristic nanomaterial and its-associated research has been rapidly evolving in a variety of fields. With the remarkable advances of graphene especially in the biomedical realm, in vivo evaluation techniques to examine in vivo behavior of graphene are largely demanded under the hope of clinical translation. Many different types of drugs such as the antisense oligomer and chemotherapeutics require optimal delivery conveyor and graphene is now recognized as a suitable candidate due to its simple and high drug loading property. Termed as 'radio-graphene', radioisotope-labeled graphene approach was recently harnessed in the realm of biomedicine including cancer diagnosis and therapy, contributing to the acquisition of in vivo information for targeted drug delivery. In this review, we highlight current examples for bioapplication of radiolabeled graphene with brief perspectives on future strategies in its extensive bio-or clinical applications.