Petroleum in its various natural forms is known and utilized by mankind since immemorial times. However, its industrial development at a large scale came only in the late XIX century, first as a raw material to produce lighting oil and lubricants, and then, at the turn of the XX century, as a powerful source of energy that partially substituted for coal within a few decades and characterized the entire evolution of the contemporary society. The present paper highlights the valuable documentation on petroleum substances of the pre-industrial era, and illustrates the early studies that paved the way to the modern petroleum industry, addressing in particular the pioneering and empirical technology of the XIX century, the application of scientific methodologies of the early XX century that contributed to the foundation of petroleum engineering, and the intensification of high technology standards at the turn of the XXI century that ensure the ever growing supply of energy necessary to sustain life on earth.