Background <p>Together with inadequate treatment and the long-term adverse effects of presently available cancer medications, the rising incidence of lung cancer cases has made it a global burden. The current methods for curing cancer include surgery, radiation, chemotherapy, and immunotherapy; these methods have serious adverse effects, toxicities, and drug resistance.</p> Objective <p>Because of their admirable selectivity and reduced toxicity, anti-cancer peptides have emerged as a leading therapeutic approach for the treatment of cancer.</p> Methodology <p>Compared to antibodies, peptides have a weaker affinity and a shorter half-life in the body. On the other hand, peptides outperform antibodies in terms of tissue penetration and cell internalization. This study offers current data on therapeutic peptide-based medications that have a lot of potential for treating lung cancer in the near future. Linkers have been used to create peptide–drug conjugates by conjugating tumor-homing peptides with payloads like small-molecule or chemotherapeutic medications. Furthermore, peptides preferentially attach to proteins and cell surface receptors, inhibiting their biological function or acting as hormone analogs. Additionally, peptides that are ingested by cells attach to intracellular proteins and disrupt connections between proteins.</p> Result <p>Peptides thus show a lot of promise for use as multipurpose agents in cancer treatment.</p> Conclusion <p>Peptides thus represent admirable promises for use as multipurpose agents in cancer therapy.</p> Graphical Abstract <p>Peptide-based drugs in lung cancer treatment and overcome chemoresistance</p>