Chemodynamic therapy can convert endogenous hydrogen peroxide (H2O2) at tumor localization into the toxic hydroxyl radical (˙OH) destroying tumor cells. Photodynamic therapy as a noninvasive method utilizes photosensitizers (PSs) to convert O2 into cytotoxic reactive oxygen species (e.g., 1O2) upon laser irradiation, which is dependent on the content of oxygen. The combination of the two therapeutic strategies on a single platform can enhance the anticancer effect. Herein, we report a porphyrin-ferrocene theranostic agent for combined photodynamic and chemodynamic therapy. Compared to monotherapy, the as-prepared porphyrin-ferrocene conjugates exhibit superior efficiency and potency in killing cancer cells at low drug doses. This study suggests the rational design of molecular structures as multifunctional therapeutics for potential clinic application.