A new near-infrared light-controlled drug delivery system based on caged gold nanorods (CGNRs) is demonstrated. The loading and release process of drug payloads into/from CGNR nanocarriers were systematically investigated. The drug-loaded CGNR constructs could enable combined chemotherapy and photo-thermal effects in killing tumor cells upon light irradiation, therefore, enhance the killing efficiency. In conjunction with visibility under quenching-free dark-field imaging, CGNRs may serve as multifunctional theranostic reagents towards cancer diagnostics and therapeutics.