Abstract: Research efforts on non coding RNAs have grown exponentially in the past decade. We are now beginning to witness the achievements that have been made in better understanding the roles of miRNAs in human diseases such as cancer and cardiovascular diseases. miRNAs show great promise as biomarkers for cancer diagnosis and prognosis. In addition, miRNAs, due to their critical function as either oncogenes or tumor suppressor genes and their broad impact on target genes and pathways, have great potential as therapeutic agents for novel cancer drug development. Several miRNA molecules and mimics are getting close to clinical trials. In this review, we summarize and highlight some of the important findings relating to miRNA and anticancer therapeutic development.