Malignant tumor has been a severe hazard to human beings globally. Conventional solemodal therapies, such as chemotherapy, surgical resection, and radiotherapy still inevitably confront hurdles such as off-target effects, low bioavailability, and remarkable systematic toxicity. One of the most encouraging approaches to address these issues is the synergistic therapy owing to its high therapeutic efficiency, low risk of relapse and fewer side effects. The combination of chemotherapy and photothermal therapy (PTT) with prominent merits of noninvasiveness, spatiotemporal controllability, and low toxicity has led to a burst research vitality for multimodal nanomedicine. In this regard, PTT can exert the hyperthermia effects to ablate tumor cells, and the local hyperthermia can preferentially enhance permeability and fluidity of cell membranes to augment cellular uptake of drugs. Accordingly, the chemophotothermal synergistic therapy can overcome the impediments of each monotherapy and profit from additive or synergistic effects with boosted therapeutic efficiency. However, current chemo-photothermal synergistic therapy is largely subject to (1) non-specific targeted delivery and poor accumulation of drugs at lesion sites; (2) inability of controllable drug release on demand; (3) absence of an efficient navigating modality for therapy monitoring. The emergence of precise theranostics signals the immense potential to overcome these intractable predicaments, which aims to effectively target the specific location, subsequently activate the drug release or trigger the phototherapy, as well as monitor the treatment process in real-time through visual navigation, thus enhancing therapeutic efficacy and patient comfort to realize on demand personalized therapy. Approaches for targeted delivery typically comprise passive targeting and active targeting. Therapeutics encapsulated in nanocarriers may passively accumulated at the tumor sites due to the enhanced permeability and retention (EPR) effect, generally superior than the standard chemodrugs. Active targeting strategies involve the incorporation of targeting ligands (i.e. antibodies, peptides, aptamers, and small molecules such as glucose or folic acid) on the surface of drug delivery nanocarriers. These ligands can identify corresponding receptors that are overexpressed or clustered on tumor cells or in the tumor microenvironments, thus facilitating specific homing, improving enrichment at the tumor sites, and enhancing cellular internalization of drugs. Besides, surface engineering of the nanocarriers is an elegant approach to actively target desired tumor cells. For instance, biomimetic nanocarriers cloaked with cell membrane have gained widespread attention for their remarkable biointerfacing property, which is regarded as a top-down approach to bypass the strenuous group modification procedures. The reserved cell membrane proteins are beneficial to increasing immune escape, prolonging blood circulation lifetime, and facilitating tumor specific targeting ability, leading to the enrichment of therapeutic accumulation and the cytotoxic immunomodulatory effects, thereby greatly enhancing therapy efficiency. Non-specific and premature release or activation of payloads is an additional obstacle that impairs the therapy efficiency. Developing stimuli-responsive nanocarriers that respond to exogenous stimuli (i.e. light, temperature, electric fields, magnetic field, and ultrasound) and/or endogenous stimuli (i.e. pH, cytoplasmic glutathione (GSH), ion, enzyme, and reactive oxygen species) for releasing or triggering the payloads on demand in a precise temporal/spatial controllable manner offers an engaging approach to overcome the concern of premature release from nanocarriers in systemic blood circulation. Compared to systemic administration, stimuliresponsive nanocarriers precisely and flexibly trigger local controllable activation of therapeutics that can notably augment pharmacological benefit in the tumor region and lessen detrimental side effects in the normal tissues. In addition to targeted delivery and controllable release, in vivo imaging navigation greatly facilitates precise theranostics. Various medical imaging techniques, such as fluorescence imaging (FLI), photothermal imaging (PTI), photoacoustic imaging (PAI), ultrasound imaging (USI), magnetic resonance imaging (MRI), computed tomography (CT), and positron emission tomography (PET), have the capability to monitor treatment in real-time and on-site, which could visualize the drug biodistribution to help determine the optimal drug dose and treatment regimen for individual patient, thus avoiding insufficient treatment that would result in incomplete tumor regression, or overtreatment that would be accompanied by deleterious side effects. Although promising, integrating the collective merits of multiple functional modalities into one single system to actualize synergistic augment of individual moiety for providing effective precise therapy remains challenging.