Pterostilbene (PTS), a naturally occurring analog of resveratrol (RSV), has shown significant therapeutic potential in treating inflammatory and oncological diseases. This review highlights the pharmacological properties, mechanisms of action, and therapeutic potential of PTS. PTS exhibits anti-inflammatory, antioxidant, and antitumor properties, making it a promising candidate for clinical applications. Its influence on regulatory pathways such as NF-κB and PI3K/Akt underscores its diverse strategies in addressing diseases. PTS also has a favorable pharmacokinetic profile with better oral bioavailability compared to other stilbenoids, enhancing its therapeutic potential. PTS is more effective than RSV in reducing liver damage by targeting the NF-κB/NLRP3 signaling pathway and mitigating inflammation and oxidative stress. PTS has demonstrated neuroprotective effects, reducing oxidative stress and inflammation in neurodegenerative diseases. It also exhibits antifibrotic effects by inhibiting the TGF-β1/TbR/Smads signaling pathway and reducing fibrosis in various organs. PTS has shown anticancer properties, inhibiting cancer cell migration and invasion, and modulating DNA methylation and histone modification. PTS promotes autophagy in tumors, which helps in cancer cell death. PTS also inhibits epithelial-mesenchymal transition and apoptosis in tumors, reducing tumor growth and metastasis. PTS exerts a regulatory role in tumor stem cells, inhibiting their self-renewal and differentiation. PTS improves tumor drug resistance by enhancing autophagy and reducing chemotherapy resistance. PTS is more effective than RSV in suppressing HeLa cell growth, colony survival, and metastasis. PTS has also shown potential in treating obstructive sleep apnea by reducing oxidative stress and correcting immune imbalances. PTS is safe and well-tolerated, with no observable toxic side effects even at high doses in animal studies. PTS has a favorable safety profile and is a promising candidate for further clinical development.Pterostilbene (PTS), a naturally occurring analog of resveratrol (RSV), has shown significant therapeutic potential in treating inflammatory and oncological diseases. This review highlights the pharmacological properties, mechanisms of action, and therapeutic potential of PTS. PTS exhibits anti-inflammatory, antioxidant, and antitumor properties, making it a promising candidate for clinical applications. Its influence on regulatory pathways such as NF-κB and PI3K/Akt underscores its diverse strategies in addressing diseases. PTS also has a favorable pharmacokinetic profile with better oral bioavailability compared to other stilbenoids, enhancing its therapeutic potential. PTS is more effective than RSV in reducing liver damage by targeting the NF-κB/NLRP3 signaling pathway and mitigating inflammation and oxidative stress. PTS has demonstrated neuroprotective effects, reducing oxidative stress and inflammation in neurodegenerative diseases. It also exhibits antifibrotic effects by inhibiting the TGF-β1/TbR/Smads signaling pathway and reducing fibrosis in various organs. PTS has shown anticancer properties, inhibiting cancer cell migration and invasion, and modulating DNA methylation and histone modification. PTS promotes autophagy in tumors, which helps in cancer cell death. PTS also inhibits epithelial-mesenchymal transition and apoptosis in tumors, reducing tumor growth and metastasis. PTS exerts a regulatory role in tumor stem cells, inhibiting their self-renewal and differentiation. PTS improves tumor drug resistance by enhancing autophagy and reducing chemotherapy resistance. PTS is more effective than RSV in suppressing HeLa cell growth, colony survival, and metastasis. PTS has also shown potential in treating obstructive sleep apnea by reducing oxidative stress and correcting immune imbalances. PTS is safe and well-tolerated, with no observable toxic side effects even at high doses in animal studies. PTS has a favorable safety profile and is a promising candidate for further clinical development.