This contributed book provides a comprehensive exploration of chemical and immunological strategies in cancer therapeutics, emphasizing precision medicine approaches for targeted and effective treatments. It integrates cutting-edge advancements in drug discovery, covering a diverse range of anticancer agents, from natural compounds and metal-based complexes to synthetic inhibitors and nanocarriers. The chapters cover topics such as the rational design and optimization of cancer therapeutics, employing molecular modeling, structure-activity relationship analysis, and AI-driven drug discovery. Additionally, the book highlights immunological interventions, such as immune checkpoint inhibitors and host-directed therapies, showcasing their growing relevance in personalized cancer treatment. Readers will discover diverse perspectives from expert contributing authors, offering a balanced perspective on the potential and limitations of these compounds in cancer therapeutics. This book is intended for researchers, academics, clinicians, and industry professionals engaged in oncology, pharmacology, medicinal chemistry, and natural product research. By combining theoretical insights with practical applications, it aims to advance understanding, inspire innovation, and facilitate the translation of promising cancer therapeutics from the lab to clinical settings.