Johnson-Ansah Hyacinthe, Maneglier Benjamin, Huguet Françoise, Legros Laurence, Escoffre-Barbe Martine, Gardembas Martine, Cony-Makhoul Pascale, Coiteux Valérie, Sutton Laurent, Abarah Wajed, Pouaty Camille, Pignon Jean-Michel, Choufi Bachra, Visanica Sorin, Deau Bénédicte, Morisset Laure, Cayssials Emilie, Molimard Mathieu, Bouchet Stéphane, Mahon François-Xavier, Nicolini Franck, Aegerter Philippe, Cayuela Jean-Michel, Delord Marc, Bruzzoni-Giovanelli Heriberto, Rousselot Philippe
Department of Hematology, CHU Côte de Nacre, 14000 Caen, France.
Pharmacology Department, Centre Hospitalier de Versailles, 78150 Le Chesnay, France.
Pharmaceutics. 2022 Aug 12;14(8):1676. doi: 10.3390/pharmaceutics14081676.
The registered dose for imatinib is 400 mg/d, despite high inter-patient variability in imatinib plasmatic exposure. Therapeutic drug monitoring (TDM) is routinely used to maximize a drug’s efficacy or tolerance. We decided to conduct a prospective randomized trial (OPTIM-imatinib trial) to assess the value of TDM in patients with chronic phase chronic myelogenous treated with imatinib as first-line therapy (NCT02896842). Eligible patients started imatinib at 400 mg daily, followed by imatinib [C]min assessment. Patients considered underdosed ([C]min < 1000 ng/mL) were randomized in a dose-increase strategy aiming to reach the threshold of 1000 ng/mL (TDM arm) versus standard imatinib management (control arm). Patients with [C]min levels ≥ 1000 ng/mL were treated following current European Leukemia Net recommendations (observational arm). The primary endpoint was the rate of major molecular response (MMR, BCR::ABL1IS ≤ 0.1%) at 12 months. Out of 133 evaluable patients on imatinib 400 mg daily, 86 patients had a [C]min < 1000 ng/mL and were randomized. The TDM strategy resulted in a significant increase in [C]min values with a mean imatinib daily dose of 603 mg daily. Patients included in the TDM arm had a 12-month MMR rate of 67% (95% CI, 51−81) compared to 39% (95% CI, 24−55) for the control arm (p = 0.017). This early advantage persisted over the 3-year study period, in which we considered imatinib cessation as a censoring event. Imatinib TDM was feasible and significantly improved the 12-month MMR rate. This early advantage may be beneficial for patients without easy access to second-line TKIs.
伊马替尼的注册剂量为400mg/天,尽管患者间伊马替尼血浆暴露存在高度变异性。治疗药物监测(TDM)通常用于使药物疗效或耐受性最大化。我们决定开展一项前瞻性随机试验(OPTIM-伊马替尼试验),以评估TDM在接受伊马替尼一线治疗的慢性期慢性髓性白血病患者中的价值(NCT02896842)。符合条件的患者开始每日服用400mg伊马替尼,随后进行伊马替尼最低血药浓度([C]min)评估。被认为剂量不足([C]min<1000ng/mL)的患者被随机分为旨在达到1000ng/mL阈值的剂量增加策略组(TDM组)和标准伊马替尼治疗组(对照组)。[C]min水平≥1000ng/mL的患者按照当前欧洲白血病网络的建议进行治疗(观察组)。主要终点是12个月时的主要分子反应率(MMR,BCR::ABL1国际量表≤0.1%)。在133例每日服用400mg伊马替尼的可评估患者中,86例患者的[C]min<1000ng/mL并被随机分组。TDM策略使[C]min值显著增加,伊马替尼平均日剂量为603mg/天。TDM组患者的12个月MMR率为67%(95%CI,51−81),而对照组为39%(95%CI,24−55)(p = 0.017)。这一早期优势在3年研究期内持续存在,在此期间我们将停用伊马替尼视为审查事件。伊马替尼TDM是可行的,并显著提高了12个月的MMR率。这一早期优势可能对难以获得二线酪氨酸激酶抑制剂的患者有益。