Liposomes represent one of the most successful nano-drug delivery systems among enormous nano-carriers. Although great progress has been made in conventional liposomes, the emerging shortcomings still impair the therapeutic index. The proposal of stimuli-responsive phospholipid-drug conjugates (PDCs)-based nanovesicles solves the challenges that conventional liposomes are faced with, showing great potential for cancer diagnosis and therapy. Herein, we intend to overview the current progress and unique advantages of stimuli-responsive PDCs-based nanovesicles. First, the challenges of conventional liposomes and the development of PDCs-based nanovesicles are summarized. Next, the stimuli-responsive elements used in current stimuli-responsive PDCs-based nanovesicles are outlined. Then, the unique superiorities of stimuli-responsive PDCs-based nanovesicles for drug delivery and theranostics are highlighted in detail. Finally, the future opportunities and challenges of stimuli-responsive PDCs-based nanovesicles for clinical translation are put forward.