Pterostilbene (PTS), a natural analog of resveratrol (RSV), has gained significant attention for its potential therapeutic effects 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 like NF-κB and PI3K/Akt underscores its diverse strategies in addressing diseases. PTS also shows a favorable pharmacokinetic profile with better oral bioavailability compared to other stilbenoids, enhancing its therapeutic potential. However, more extensive clinical trials are needed to establish its safety and efficacy in diverse patient populations. The review covers the pharmacokinetics, antioxidant activity, anti-inflammatory effects, antifibrotic effects, and antitumor properties of PTS, providing a comprehensive overview of its current knowledge and applications in inflammatory and oncological diseases.Pterostilbene (PTS), a natural analog of resveratrol (RSV), has gained significant attention for its potential therapeutic effects 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 like NF-κB and PI3K/Akt underscores its diverse strategies in addressing diseases. PTS also shows a favorable pharmacokinetic profile with better oral bioavailability compared to other stilbenoids, enhancing its therapeutic potential. However, more extensive clinical trials are needed to establish its safety and efficacy in diverse patient populations. The review covers the pharmacokinetics, antioxidant activity, anti-inflammatory effects, antifibrotic effects, and antitumor properties of PTS, providing a comprehensive overview of its current knowledge and applications in inflammatory and oncological diseases.