Research and development of targeted therapies for cancer treatment has dramatically increased in recent years. Several new targeted therapies have been approved by the Food and Drug Administration (FDA) over the past 5 years. Some of the most recently approved small molecule inhibitors include ivosidenib (Tibsovo®) and dacomitinib (Vizimpro®), and new monoclonal antibodies that have reached the market consist of cemiplimab-rwlc (Libtayo®) and mogamulizumab-kpkc (Poteligeo®). These therapies target specific proteins or receptors involved in cancer cell growth, metastasis, and survival. Unlike treatment with chemotherapeutic agents and radiotherapy, which have non-specific mechanisms that lead to widespread systemic toxicity, targeted therapies exclusively affect specific molecular targets. Targeted therapies support a more personalized approach to cancer treatment and can improve efficacy for many types of cancer. These novel therapies also offer prescribers more options for cancer treatment. Because targeted therapies only target specific proteins or receptors, their mechanisms of action and toxicities often do not overlap with traditional therapies or other targeted therapies. This enables these medications to be used in combination with chemotherapy, radiation therapy, and other targeted therapies, which can enhance treatment efficacy. Targeting a variety of pathways and mechanisms can prevent treatment resistance and treat more aggressive types of cancer. While targeted therapies may offer improved efficacy and limit systemic toxicity, they are also associated with numerous adverse events that can sometimes limit treatment.