Аннотация:New phototherapeutic agents based on synthetic porphyrintype tetrapyrroles and small-molecule-targeted tyrosine kinase inhibitor Erlotinib have been synthesized based on the scheme involving ‘click’ reaction between bis(4-azidophenyl)-containing zinc porphyrinate derivative and N-(3 ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-quinazoline. The final compound and its precursors weretested as potential photosensitizers for targeted photodynamic therapy (PDT), the conjugate having shown photoinduced cytotoxicity IC50 for NKE cells 0.86±0.017 µm and for A431 cells 0.54±0.011 µm.