This review highlights the significance of hypoxia-inducible factor-1 (HIF-1) in cancer development and progression, emphasizing its role as a therapeutic target. HIF-1 is a transcription factor that regulates oxygen homeostasis in response to hypoxic conditions, and its expression is significantly upregulated in cancer cells. HIF-1 plays a crucial role in various cancer-related processes, including cell division, survival, proliferation, angiogenesis, and metastasis. The review outlines emerging therapeutic strategies targeting HIF-1, including small molecule inhibitors, RNA interference, and nanotechnology-based approaches. These strategies aim to block HIF-1 activation pathways, such as transcription, protein synthesis, stabilization, dimerization, DNA binding, and transactivation. The use of nanocarriers to deliver HIF-1 inhibitors and gene silencing using siRNA is also discussed. Despite the potential of HIF-1 as a therapeutic target, challenges and limitations remain, including the lack of hypoxia specificity, selectivity issues, and the need for personalized medicine. The review concludes by emphasizing the complexity of HIF-1 regulation and its extensive influence on cancer processes, highlighting the potential for more effective cancer treatments.This review highlights the significance of hypoxia-inducible factor-1 (HIF-1) in cancer development and progression, emphasizing its role as a therapeutic target. HIF-1 is a transcription factor that regulates oxygen homeostasis in response to hypoxic conditions, and its expression is significantly upregulated in cancer cells. HIF-1 plays a crucial role in various cancer-related processes, including cell division, survival, proliferation, angiogenesis, and metastasis. The review outlines emerging therapeutic strategies targeting HIF-1, including small molecule inhibitors, RNA interference, and nanotechnology-based approaches. These strategies aim to block HIF-1 activation pathways, such as transcription, protein synthesis, stabilization, dimerization, DNA binding, and transactivation. The use of nanocarriers to deliver HIF-1 inhibitors and gene silencing using siRNA is also discussed. Despite the potential of HIF-1 as a therapeutic target, challenges and limitations remain, including the lack of hypoxia specificity, selectivity issues, and the need for personalized medicine. The review concludes by emphasizing the complexity of HIF-1 regulation and its extensive influence on cancer processes, highlighting the potential for more effective cancer treatments.