Institute of Endocrinology, Beilinson Hospital, Petach-Tikva, and Sackler School of Medicine, Tel Aviv University, Israel.
Arch Med Res. 2023 Dec;54(8):102883. doi: 10.1016/j.arcmed.2023.102883. Epub 2023 Sep 7.
Prolactinomas are the most common functional pituitary tumors, accounting for 40% of all pituitary adenomas. Medical treatment with dopamine agonists (DA), mainly cabergoline, is considered the primary therapy for these patients. Prolactin normalization is achieved in 80-90% of prolactinomas treated with cabergoline. Patients resistant to the standard dose can escalate the dose of cabergoline up to the maximum tolerated dose. The expression of dopamine (D2) receptors and dopamine affinity is decreased in aggressive and resistant prolactinomas. Patients with aggressive and DA-resistant adenomas or with rare PRL-secreting carcinomas can be treated off-label with temozolomide (TMZ), a DNA alkylating agent. TMZ is effective in 40-50% of treated lactotroph tumors showing at least a partial response. However, patients tend to escape from the effect of TMZ after a limited time of response. Other therapeutic options include aromatase inhibitors, the somatostatin receptor ligand pasireotide, peptide receptor radionuclide therapy (PRRT), immune-checkpoint inhibitors, tyrosine-kinase inhibitors, or everolimus, the mammalian target of rapamycin inhibitor. These experimental treatments were effective in some patients carrying refractory prolactinomas showing usually partial tumor control. However, the number of treated patients with any of these new therapeutic options is very limited and treatment results are inconsistent, thus additional experience with more patients is required.
催乳素瘤是最常见的功能性垂体肿瘤，占所有垂体腺瘤的 40%。用多巴胺激动剂（DA），主要是卡麦角林进行医学治疗被认为是这些患者的主要治疗方法。用卡麦角林治疗的催乳素瘤中，有 80-90%的催乳素恢复正常。对标准剂量有抗药性的患者可以将卡麦角林的剂量增加到最大耐受剂量。在侵袭性和耐药性催乳素瘤中，多巴胺（D2）受体和多巴胺亲和力的表达减少。对于具有侵袭性和 DA 耐药性的腺瘤或罕见的 PRL 分泌性癌患者，可以使用替莫唑胺（TMZ）进行治疗，TMZ 是一种 DNA 烷化剂。TMZ 在至少部分反应的治疗性催乳素瘤中有效率为 40-50%。然而，患者在有限的反应时间后往往会逃避 TMZ 的作用。其他治疗选择包括芳香酶抑制剂、生长抑素受体配体帕瑞肽、肽受体放射性核素治疗（PRRT）、免疫检查点抑制剂、酪氨酸激酶抑制剂或雷帕霉素，哺乳动物雷帕霉素靶蛋白抑制剂。这些实验性治疗在一些具有难治性催乳素瘤的患者中有效，这些患者通常显示部分肿瘤控制。然而，接受任何这些新的治疗方法的患者数量非常有限，治疗结果不一致，因此需要更多的患者来获得更多的经验。
