Muscle mass and strength decline with age. When severe, the loss is called sarcopenia. Sarcopenia is drawing attention worldwide, especially in highly aged societies, as a disease that should be treated. At present, we have limited tools to combat sarcopenia (e.g. resistance training and nutritional intervention), but accumulating knowledge of the molecular and cellular mechanisms of sarcopenia is accelerating the development of pharmacological therapies for sarcopenia. Because sarcopenia is a complicated pathological condition caused and modified by many aging-related factors, such as inactivity, loss of motor neurons, poor nutrition, decline of anabolic hormones, chronic inflammation, oxidative stress, impaired stem cell function, and comorbidity, the proposed target molecules or pathways for pharmacological intervention are diverse. Here we review recent progress in drug development with emphasis on small-molecule compound-based therapies and review the literature to identify new therapeutic targets to prevent, delay, or reverse sarcopenia.