The aim of the study was the pharmacokinetic and pharmacogenetic analysis of analgetic efficacy and safety of transdermal fentanyl for cancer patients. Material and methods. A comprehensive search for journal articles published between 2012 and 2017 was carried out using PubMed, Scopus, Web of Science, and E-library databases. Results. The analysis of the data showed that pharmacokinetic and pharmacogenetic factors can influence the interindividual variability of analgesic therapy with fentanyl TTC for cancer patients, predetermining phenotypic differences in the efficacy and safety of analgesia. Enforced polypharmacotherapy with the use of inducers or inhibitors of the CYP3A4 isoenzyme activity can significantly change the effectiveness of analgesic therapy and result in undesirable side effects of strong opioids. Contradictory data on the effect of some single nucleotide polymorphisms of metabolic genes, transport genes and mu-opioid receptor genes dictate the necessity of further studies in this field. Conclusion. To date, there is no single explanation for interindividual variability of analgesic therapy with fentanyl TTS. A comprehensive assessment of the pharmacokinetic and pharmacogenetic factors affecting the efficacy and safety of analgesic therapy with potent opioids is a tool of a personalized approach for anesthesia in clinical oncology. © 2018 Tomsk National Research Medical Center of the Russian Academy of Sciences. All rights reserved.