El Bouchikhi Ihssane, Azami Idrissi Hajar, Lazraq Ahmed, El Makhzen Badreddine, Ahakoud Mohamed, Berrady Rhizlane, Ouldim Karim, Bouguenouch Laila, El-Azami-El-Idrissi Mohammed
Laboratory of Biomedical & Translational Research, Faculty of Medicine, Pharmacy and Dentistry of Fez, Sidi Mohamed Ben Abdellah University, 30000, Fez, Morocco; Medical Genetics & Oncogenetics Laboratory, Hassan II University Hospital, 30000, Fez, Morocco; Multidisciplinary Laboratory of Research & Innovation, Polydisciplinary Faculty of Khouribga, Sultan Moulay Slimane University, 25000, Kouribga, Morocco.
Laboratory of Biomedical & Translational Research, Faculty of Medicine, Pharmacy and Dentistry of Fez, Sidi Mohamed Ben Abdellah University, 30000, Fez, Morocco; Medical Genetics & Oncogenetics Laboratory, Hassan II University Hospital, 30000, Fez, Morocco.
Cancer Genet. 2024 Nov;288-289:40-42. doi: 10.1016/j.cancergen.2024.08.083. Epub 2024 Sep 3.
Tyrosine Kinase Inhibitors (TKI), such as Imatinib, are known for their effectiveness in achieving complete remission from Chronic Myeloid Leukemia (CML), a malignancy caused by a reciprocal translocation between the terminal fragments of the long arms of chromosomes 9 and 22 that leads to the famous chimeric BCR::ABL1 gene. Mutations in this fusion gene may induce resistance to TKI treatment, which requires prescribing a second-, or third-generation TKI medication. We report here a case of a Moroccan CML patient with secondary resistance to the frontline TKI treatment (Imatinib), in which, BCR::ABL1 cDNA sequencing reveals the novel mutation p.K375M at the ABL1 Kinase Domain. In-silico prediction tools confirm the pathogenicity of the p.K375M substitution. Homology analysis indicated that the residue is highly conserved and located in a stable region. This potentially pathogenic mutation is likely to disrupt the BCR::ABL1-Imatinib binding, leading to the observed resistance. To overcome the treatment resistance, Imatinib should be substituted with a second-generation TKI medication, such as Dasatinib, Bosutinib, or Nilotinib. The present study further widens the spectrum of TKI resistance mutations and emphasizes particularly the crucial role of molecular investigation in personalizing treatment for CML patients, ensuring efficient follow-up and appropriate healthcare.
酪氨酸激酶抑制剂(TKI),如伊马替尼,因其在实现慢性髓性白血病(CML)完全缓解方面的有效性而闻名,CML是一种由9号和22号染色体长臂末端片段相互易位导致著名的嵌合BCR::ABL1基因的恶性肿瘤。该融合基因中的突变可能会诱导对TKI治疗的耐药性,这就需要开具第二代或第三代TKI药物。我们在此报告一例对一线TKI治疗(伊马替尼)产生继发性耐药的摩洛哥CML患者,其中BCR::ABL1 cDNA测序揭示了ABL1激酶结构域的新突变p.K375M。计算机预测工具证实了p.K375M替代的致病性。同源性分析表明该残基高度保守且位于一个稳定区域。这种潜在的致病突变可能会破坏BCR::ABL1与伊马替尼的结合,导致观察到的耐药性。为克服治疗耐药性,应将伊马替尼替换为第二代TKI药物,如达沙替尼、博舒替尼或尼洛替尼。本研究进一步拓宽了TKI耐药突变的范围,并特别强调了分子研究在CML患者个体化治疗、确保有效随访和适当医疗保健方面的关键作用。