Normal and abnormal/pathological status of physiological processes in the human organism can be characterized through Volatile Organic Compounds (VOCs) emitted in breath. Recently, a wide range of volatile analytes has risen as biomarkers. These compounds have been addressed in the scientific and medical communities as an extremely valuable metabolic window. Once collected and analysed, VOCs can represent a tool for a rapid, accurate, non-invasive, and painless diagnosis of several diseases and health conditions. These biomarkers are released by exhaled breath, urine, faeces, skin, and several other ways, at trace concentration levels, usually in the ppb_v (μg/L) range. For this reason, the analytical techniques applied for detecting and clinically exploiting the VOCs are extremely important. The present work reviews the most promising results in the field of breath biomarkers and the most common methods of detection of VOCs. A total of 16 pathologies and the respective database of compounds are addressed. An updated version of the VOCs biomarkers database can be consulted at: https://neomeditec.com/VOCdatabase/.