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The innovation of the pharmacological field brings us new options to manage disorders; those had been resistant to the used treatments. A recent topic in the dermatologic field includes targeted therapy. As reported elsewhere, these drugs show high efficacy for targeting disorders. To continue to use the drugs for wellness for patients, we need to pay attention to prevent, manage and overcome various skin eruptions, unexpected reactivation and recurrence of infection. Targeted therapy with small molecules and monoclonal antibodies is effective for malignant tumors, especially inoperative and advanced cancers, autoimmune-related inflammatory diseases of severe and refractory psoriasis and psoriatic arthritis, and allergic diseases. Small molecules are composed of tyrosine kinase inhibitors (i.e. imatinib, gefitinib, erlotinib), a multikinase inhibitor (sorafenib), a tumor necrosis factor alpha (TNF-α) inhibitor (etanercept), and a proteasome inhibitor (bortezomib). Monoclonal antibodies are classified into chimeric antibodies (i.e. cetuximab, rituximab, infliximab), humanized antibodies (i.e. tocilizumab, trastuzumab, bevacizumab, omalizumab) and human antibodies (i.e. adalimumab, panitumumab).