Influence of the UGT1A1 gene polymorphism on treatment with sacituzumab govitecan. Narrative review

Objective: Sacituzumab govitecan is an antineoplastic therapy composed of a monoclonal antibody directed to the Trop2 antigen, conjugated to SN-38, an active metabolite of irinotecan that inhibits topoisomerase I. It is indicated for the treatment of metastatic triple-negative breast cancer in patie...

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Detalles Bibliográficos
Autores: Legido Perdices, Eva María, Do Pazo Oubiña, Fernando, Prado Mel, Elena, Miarons, Marta, García, Betel Del Rosario, Gutiérrez Nicolás, Fernando
Tipo de recurso: artículo
Fecha de publicación:2025
País:España
Institución:Conselleria de Salut i Consum del Govern de les Illes Balears
Repositorio:Docusalut
Idioma:español
OAI Identifier:oai:docusalut.com:20.500.13003/25203
Acceso en línea:https://hdl.handle.net/20.500.13003/25203
Access Level:acceso abierto
Palabra clave:Anticuerpo conjugado
Conjugated antibody
Cáncer de mama triple negativo
Polimorfismos UGT1A1
Sacituzumab govitecan
Toxicidad
Toxicity
Triple-negative breast cancer
UGT1A1 polymorphisms
Descripción
Sumario:Objective: Sacituzumab govitecan is an antineoplastic therapy composed of a monoclonal antibody directed to the Trop2 antigen, conjugated to SN-38, an active metabolite of irinotecan that inhibits topoisomerase I. It is indicated for the treatment of metastatic triple-negative breast cancer in patients who have received at least two prior lines of treatment, with at least one in the metastatic context. SN-38 is eliminated by glucuronidation mediated by uridine diphosphate-glucuronosyltransferase-1A1 (UGT1A1) enzymes, present in the liver. Mutations in the UGT1A1 gene decrease the expression of these enzymes, which increases the concentration of SN-38 and, consequently, increases the toxicity of the drug, especially in the form of neutropenia and diarrhea. This study aims to analyze the relationship between UGT1A1 gene polymorphisms and toxicity associated with treatment with sacituzumab govitecan, in addition to reviewing the usefulness of genetic screening prior to starting therapy. Methods: A non-systematic literature review was conducted on the impact of UGT1A1 gene polymorphisms on the safety of sacituzumab govitecan treatment in patients with triple-negative breast cancer. The search included primary and secondary literature sources and communications from oncology conferences. Results: Patients treated with sacituzumab govitecan with the UGT1A1*28/*28 mutated genotype are more likely to experience grade more than 3 hematologic adverse events: neutropenia (approximate incidence of 60% compared to 40% for 1/*1 and 1/*28 genotypes), febrile neutropenia (18% homozygotes vs. 5% heterozygotes and 3% wild-type), grade more than 3 anemia (15% vs. 6% and 4%, respectively); as well as grade more than 3 diarrhea (24% vs. 13% and 6%, respectively). Additionally, treatment discontinuation rates are higher in *28/*28 individuals (6% compared to 1% heterozygotes and 2% wild-type). Conclusions: Patients homozygous for the UGT1A1*28 allele are at significantly increased risk of developing serious adverse events. Despite the clear relationship between UGT1A1 polymorphisms and sacituzumab-govitecan toxicity, the review suggests that there is insufficient consensus on the need for systematic genetic screening. However, the findings indicate that such screening could be useful for identifying patients at risk and personalizing sacituzumab govitecan therapy.