Pharmacological Mechanisms and Clinical Applications of Oxycodone in Cancer Pain Management: A Narrative Review

Cancer pain significantly impairs quality of life in oncology patients and remains inadequately managed globally. This narrative review examines the pharmacokinetic and pharmacodynamic properties of oxycodone, the impact of CYP2D6 genetic polymorphism on its metabolism, and the EGFR-dependent bidirectional effects of oxycodone on cancer cell biology. Critically, these bidirectional tumor cell effects were observed exclusively under supraphysiological in vitro concentrations (0.01-10 µM), far exceeding clinical therapeutic plasma levels (nM range), and are insufficient to alter current clinical guidelines. We further evaluate oxycodone's effects on tumor angiogenesis and immune function, and summarize clinical evidence from postoperative analgesia studies in breast, colorectal, gastric, lung, and liver cancer patients, supporting oxycodone as a preferred option for perioperative analgesia in abdominal and thoracic cancer surgery. The limitations of oxycodone in chronic neuropathic and bone metastasis pain are discussed, alongside recent advances in oxycodone formulation development and novel analgesics in China. Individualized treatment strategies integrating pharmacogenomic profiles and multimodal approaches are encouraged.

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Publication Details

Journal
Drug Design Development and Therapy
Published
2026-04-01
DOI
https://doi.org/10.2147/dddt.s594973
Primary Topic
Pain Management and Opioid Use
Type
article
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article

Pharmacological Mechanisms and Clinical Applications of Oxycodone in Cancer Pain Management: A Narrative Review

Yuanlin Xia, Guihua Huang
Drug Design Development and Therapy
Pain Management and Opioid Use
article

Pharmacological Mechanisms and Clinical Applications of Oxycodone in Cancer Pain Management: A Narrative Review

Yuanlin Xia, Guihua Huang
article en

Abstract

Cancer pain significantly impairs quality of life in oncology patients and remains inadequately managed globally. This narrative review examines the pharmacokinetic and pharmacodynamic properties of oxycodone, the impact of CYP2D6 genetic polymorphism on its metabolism, and the EGFR-dependent bidirectional effects of oxycodone on cancer cell biology. Critically, these bidirectional tumor cell effects were observed exclusively under supraphysiological in vitro concentrations (0.01-10 µM), far exceeding clinical therapeutic plasma levels (nM range), and are insufficient to alter current clinical guidelines. We further evaluate oxycodone's effects on tumor angiogenesis and immune function, and summarize clinical evidence from postoperative analgesia studies in breast, colorectal, gastric, lung, and liver cancer patients, supporting oxycodone as a preferred option for perioperative analgesia in abdominal and thoracic cancer surgery. The limitations of oxycodone in chronic neuropathic and bone metastasis pain are discussed, alongside recent advances in oxycodone formulation development and novel analgesics in China. Individualized treatment strategies integrating pharmacogenomic profiles and multimodal approaches are encouraged.

Drug Design Development and TherapyVol. Volume 20
Guizhou Provincial People's Hospital (CN)
Good health and well-being
Openalex Percentile: Top 31%
Pain Management and Opioid Use
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