Lab-on-a-chip (LOC) as an alternative biosensing approach concerning cost efficiency, parallelization, ergonomics, diagnostic speed, and sensitivity integrates the techniques of various laboratory operations such as biochemical analysis, chemical synthesis, or DNA sequencing, etc. on miniaturized microfluidic single chips. Meanwhile, LOC tools based on molecularly imprinted biosensing approach permit their applications in various fields such as medical diagnostics, pharmaceuticals, etc., which are user-, and eco-friendly sensing platforms for not only alternative to the commercial competitor but also on-site detection like point-of-care measurements. In this review, we focused our attention on compiling recent pioneer studies that utilized those intriguing methodologies, the microfluidic Lab-on-a-chip and molecularly imprinting approach, and their biomedical applications.