Abstract: The present invention relates to the field of medicine, particularly to oncology and provides a pharmaceutical composition intended for the photodynamic therapy of malignant tumors, comprising a therapeutically effective amount of at least one of derivatives of fullerene C60 selected from the group consisting of a compound in which a fullerene C60 molecule covalently binds to one molecule of an amino acid or a dipeptide, or its pharmaceutically acceptable derivative, or a complex of a compound with biocompatible synthetic polymers or biopolymers and tetrapyrroles, or a conjugate of a compound with an amino compound. Said compounds after accumulation in cells and photoirradiation transform molecular oxygen into singlet oxygen, generate free radicals, and also trigger biological processes inhibiting the vital activity of tumor cells.