It is formed in the liver by the metabolism of cocaine by hydrolysis, catalysed by carboxylesterases, and subsequently excreted in the urine.

In 2005, scientists found surprisingly large quantities of benzoylecgonine in Italy's Po River and used its concentration to estimate the number of cocaine users in the region.

[4] In 2006, a similar study was performed in the Swiss ski town of Saint-Moritz using wastewater to estimate the daily cocaine consumption of the population.

[5] A study done in the United Kingdom found traces of benzoylecgonine in the country's drinking water supply, along with carbamazepine (an anticonvulsant) and ibuprofen (a common non-steroidal anti-inflammatory drug), although the study noted that the amount of each compound present was several orders of magnitude lower than the therapeutic dose and therefore did not pose a risk to the population.

[7] Research is being conducted on degradation options such as advanced oxidation and photocatalysis[8] for this metabolite in an effort to reduce concentrations in waste and surface waters.