Tissue specificity is the essential need of the hour to cut down clinical abnormalities. Allowing desired drug concentration to reach the target site is the current trend of the drug delivery system. Laminin is an active component of the basal lamina and present in most cells and organs has shown great utility in this case. It is a heterotrimeric glycoprotein containing an α-chain, a β-chain, and a γ-chain and found in different isoforms. Laminin influences cell differentiation, migration, adhesion, neurite outgrowth, and angiogenesis. The active peptides screened from the whole-length laminin have been incorporated to develop targeted or tissue-specific approaches. This is because full-length laminin has many active sites and triggers various downstream signaling and functions. Laminin-derived peptides along with various carriers or vectors ensure specific binding to target tissues. The particular therapeutic or diagnostic agent is successfully targeted to the diseased site because of the affinity of peptide sequence towards the cell membrane receptors. Promising applications of laminin-derived peptides are observed in diagnostics, therapy, chemotherapy, and gene therapy. It helps in tumor imaging, delivers cancer therapeutics, and serves as a biomarker. Implant surfaces coated with laminin-derived peptides enhance attachment and biocompatibility and decreases peri-implant inflammation. Having able to influence angiogenesis, it has been found to serve the purpose in the tissue healing process too. Many other effective applications of laminin-derived peptides might be developed with advancing days, but to date, it accounts as one of the promising theranostic approaches.