催乳素瘤是最常见的功能性脑垂体肿瘤，占所有垂体腺瘤的40％。药物治疗主要采用多巴胺受体激动剂（DA），主要是卡贝肌动。催乳素瘤患者约80-90％经过卡贝肌动治疗后催乳素水平可以得到正常化。对于标准剂量无效的患者，可以逐渐增加卡贝肌动剂量，直到达到可耐受的最大剂量。侵袭性和耐药催乳素瘤的多巴胺（D2）受体及多巴胺亲和力表达减少。侵袭性和抗多巴胺治疗的腺瘤或罕见的泌乳素分泌癌患者可以使用替莫唑胺（TMZ）这种DNA烷化剂进行离标治疗。TMZ对于40-50％的乳垂体细胞瘤治疗有效，并且至少部分病变得到缓解。然而，患者在反应有限的时间后往往会失去对TMZ的疗效。其他治疗选择包括芳香化酶抑制剂、生长抑素受体配体帕西利肽、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哺乳动物雷帕霉素靶点的依维莫司。这些实验性治疗对部分难治性催乳素瘤的患者有效，通常可以部分控制肿瘤。然而，接受这些新的治疗选择的患者人数非常有限且治疗效果不一致，因此需要进一步积累更多患者的经验。 版权所有 © 2023。Elsevier Inc.出版。

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.Copyright © 2023. Published by Elsevier Inc.