After the introduction of first generation MSNs for drug delivery with some challenges such as large particle sizes, irregular morphologies and aggregations, second generation provided uniform spherical morphologies, tunable pore/particle sizes and compositions. Henceforth, organic-inorganic hybrid mesoporous silica nanosystems have grown rapidly and utilized for active and passive targeting of tumorigenic cells especially conjugated with organic polymers followed by third generation counterparts with improved functionalities for cancer therapy. The aim of this review article is to focus on the advancements in mesoporous silica based organic-inorganic hybrid nanoparticles developed as drug carriers targeting cancer cells. Brief introduction to the state-of-the-art in passive and active targeting methods is presented. Specifically, therapeutic, diagnostic and theranostic applications are discussed with emphases on triggered and ligand conjugated organic-inorganic hybrid mesoporous silica nanomaterials. Although mesoporous silica nanoparticles perform well in preclinical tests, clinical translation progresses slowly as appropriate doses needs to be evaluated for human use along with biocompatibility and efficiency depending on surface modifications.