Chronic kidney disease (CKD) is one of the most common diseases endangering human health and life. By 2030, 14 per 100,000 people may die from CKD. Renal fibrosis (RF) is an important intermediate link and the final pathological change during CKD progression to the terminal stage. Therefore, identifying safe and effective treatment methods for RF has become an important goal. In 2018, the World Health Organization introduced traditional Chinese medicine into its effective global medical program. Various phytoconstituents that affect the RF process have been extracted from different plants. Here, we review the potential therapeutic capabilities of active phytoconstituents in RF treatment and discuss how phytoconstituents can be structurally modified or combined with other ingredients to enhance efficiency and reduce toxicity. We also summarize phytoconstituent delivery strategies to overcome renal barriers and improve bioavailability and targeting.