Introduction Antineoplastic drugs, also known as hazardous drugs, are used to treat cancer. Healthcare workers’ exposure to these agents may lead to DNA damage and adverse reproductive effects. Exposure to antineoplastic drugs can be assessed via biological monitoring.

Objectives To conduct a literature review of studies examining biological monitoring of healthcare workers exposed to antineoplastic drugs to identify trends and knowledge gaps.

Methods The literature search was performed on three databases: Proquest, Web of Science and PubMed. For inclusion, an article had to be in English and published between 2005 and 2020. Search terms included ‘antineoplastic drugs’ or ‘hazardous drugs’ AND ‘occupational’ or ‘healthcare workers’ or ‘pharmacist’ or ‘nurse’ AND ‘blood’ or ‘urine’ or ‘biomarkers’.

Results Overall, the literature review resulted in 70 unique articles - 30 examined urine as the matrix, 31 had non-urine samples and nine papers collected both urine and non-urine samples. Regarding the urine sampling studies, researchers collected either spot samples or 24-hr voids. Cyclophosphamide was the most common analyte (69%) with a detection limit ranging from 0.09 to 0.20 ng/ml. Approximately 75% of the articles reported at least one urine sample had detectable levels of drug. In some instances, urinary drug contamination was found even though workers wore personal protective equipment. For those studies that collected other matrices, blood and exfoliated buccal cells were the most common specimens. A majority (81%) reported that there was a statistically significant difference in results between exposed and non-exposed populations. Many studies reported that safe work practices, which includes the use of personal protective equipment, may not be adequate to protect healthcare workers.

Conclusion There is value in conducting biological monitoring to assess healthcare workers’ exposure to antineoplastic drugs. However, because of the variability in sampling and analytical methods, standardization is recommended to ensure biological monitoring results are comparable.