Photodynamic therapy (PDT) and chemotherapy have been extensively developed as effective approaches against cancer. Herein, we constructed organic nanorods by rational co-assembly of photosensitizer, di-iodinated borondipyrromethene (BDP-I₂), and chemical anticancer drug, paclitaxel (PTX). The physico- and photochemical properties of the obtained nanorods were carefully investigated. BDP-I₂ was selected for its high singlet oxygen (¹O₂) quantum yields. And the corresponding ¹O₂ generation ability and photodynamic effect were evaluated both in vitro and in vivo. The accelerated endosomal escape of the nanorods induced by the photodynamic effect enhanced the chemotherapeutic efficacy of PTX. We believe that this synergetic nanomedicine represents a new development for antitumor chemophotodynamic therapy.