This book discusses recent advances in biology, chemistry, and pharmacology at both the preclinical and clinical stage of transient receptor potential vanilloid subtype 1 (TRPV1) drug discovery research. Chapters explore the impact and drug targeting of TRPV1 in inflammation, migraine, arthritis, and cancer; as well as the development of analgesic drugs. The TRPV1 receptor is not limited to pain only, and the book covers its role in chronic cough, bladder disorders, and asthma. The book features data relevant to the therapeutic potential of TRPV1 and the medicinal chemistry involved in designing TRPV1 antagonists.