It was discovered that interposing a suitable aromatic amidation linker in making a prodrug to serve as a [gamma]-glutamylation drug provides stability even in a close to physiological environment, recognition by GGT, and very rapid release of the pharmacologically active drug, and the invention was achieved. Specifically, a drug represented by general formula (1) to which a [gamma]-glutamyl aromatic amide has been bonded releases the pharmacologically active drug rapidly in tissues expressing a high level of GGT and can become a drug having a high therapeutic effect.本發明中發現:藉由在製作γ-麩胺醯基化藥劑之前驅藥化中,介隔適當之芳香族醯胺化連接子,而即便於接近生理環境之條件下亦穩定,被GGT所識別,而非常迅速地釋放藥理活性型藥劑,從而達成本發明。即,鍵結有γ-麩胺醯基芳香族醯胺之藥劑於GGT高度表現之組織中迅速地釋放藥理活性型藥劑,而可成為治療效果較高之藥劑。
