PURPOSE: A composition containing photoactive multimeric fullerenes for photothermal therapy is provided to prevent cytotoxicity because the composition is easily discharged to the outside of the body and decomposed by cleavable ester bond. CONSTITUTION: A composition for photothermal therapy contains monomeric fullerenes which are conjugated by cleavable ester bond and contains photoactive multimeric fullerenes with photoactive molecules and targeted materials. A photothermal therapy for animals exclusive of human comprises the steps of: administering the composition to a test subject; and percutaneously irradiating the test subject by light at 500-800 nm. A method for preparing the photoactive multimeric fullerenes comprises the steps of: preparing biocompatible polymers containing ester groups and having a functional group at both ends; introducing a reactive group to one end of the photoactive molecule and the targeted material for functionalization; making the biocompatible polymers react with monomeric fullerenes in a solvent; and adding a reactant of the introduction step to prepare photoactive multimeric fullerenes.본 발명은 광열치료용 조성물로서 다수의 플러렌(Fullerene) 단량체들이 절단성 에스테르 결합되고, 광활성 분자 및 표적지향성 물질이 결합된 광반응성 플러렌 다량체를 포함한다. 상기 다량체는 다수의 플러렌 단량체들을 절단성 에스테르 결합을 통해 가교화하고 있어서 혈청안정성과 생체로부터의 배출 및 제거 특성을 개선하였다. 또한, 광활성 분자가 포함되어 있어서 광흡수성을 개선하고 진동에너지를 보강(upregulate)하였으며, 표적지향성 물질을 포함함으로써 특정 표적에 선택적 맞춤 치료의 가능성을 높였다.