Neuropathic pain is a pathological pain state with a broad symptom scope that affects patients worldwide suffering from nerve injuries, chemotherapy, or diseases. However, the treatment possibilities are still limited due to a low efficacy and sometimes severe side effects of available therapeutics, highlighting an emerging need for novel analgesics. In addition, the development of a FKBP51-based treatment was unfortunately hampered in the past, due to the lack of a specific and potent FKBP51 inhibitor. Nevertheless, a highly potent and selective FKBP51 inhibitor called SAFit2 was developed recently. SAFit2 reduced nerve injury-induced mechanical hypersensitivity in a mouse model as it counteracted the enhanced neuronal activity and ameliorated neuroinflammation after nerve injury. Moreover, SAFit2 restored endogenous lipid levels in nervous tissue. Based on these recent results, SAFit2 constitutes as a novel and promising drug candidate for the treatment of nerve injury-induced neuropathic pain.