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The present article is devoted to the synthesis and investigation of biological and physico-chemical properties of the bacteriopurpurinimide derivative that was used as a photosensitizer. These substances have an ability to accumulate selectively in the malignant tumours. Also this class of photosensitizers is of particular interest because of their strong light absorbtion spectrum in red and NIR-region in the “window of tissue transparency”. This property affords to treat deep-seated tumours at the depth of 2 cm. In this study it was implemented the method of photodynamic therapy of cancer. The photosensitizer for this study was prepared as the nanostructured water-soluble micellar dispersion of O-propyloxime-N-propoxybacteriopurpurinimide methyl ester. The photodynamic therapy using this substance provided the highly effective photoinduced antitumour in vitro and in vivo activity, 100% regression of the tumour and 90% cure of animals.