Emerging nanotechnology has already developed various innovative nanomedicines. Nanomicelles, self-assemblies of block copolymers, are promising nanomedicines for targeted drug delivery and imaging. Stimulus-responsive targeted nanomicelles are designed to release drugs based on stimuli such as pH, temperature, redox potential, magnetism and ultrasound. This article will focus on recent advancements in the design of stimulus-responsive targeted nanomicelles loaded with anticancer drugs to fulfill the challenges associated with cancer cells (e.g., multidrug resistance) for the effective treatment of cancer. The significant toxicity issues and a possible future perspective associated with nanomicelles are also discussed here.