Molecular-targeted drugs are agents that act on molecules which are specifically expressed in cancer, or on molecules whose expression is increased in cancer compared to normal tissue, and suppress the growth, infiltration and metastasis of cancer while affecting normal tissue as little as possible by selectively impairing function in cancer tissue. The major molecular targets in cancer therapy include oncogene products, growth factors and their receptors, signal-transducing molecules, hormone receptors, cell cycle-related proteins, telomerase-related molecules, apoptosis-related molecules, angiogenesis-related molecules, anticancer drug resistance/sensitivity factors, transcription factors, and molecules related to infiltration and metastasis. This paper reports on the molecular-targeted drugs currently considered for bladder cancer.