Cabergoline is an ergot derivative long-acting dopamine receptor 2 (DR2) selective agonist administered orally and widely used for the treatment of prolactin-secreting adenomas and Parkinson’s disease DR2 is expressed in most somatotroph adenomas. In acromegaly, cabergoline is used off-label and its role is limited by the relatively modest efficacy for achieving hormonal remission and thus, it is largely indicated in patients with mild elevation of GH/IGF-I postoperatively. It can be given as monotherapy, usually at a higher weekly dose than usually required to treat prolactinomas, but also as an add-on treatment in patients partially responding to the somatostatin receptor ligands octreotide or lanreotide. IGF-1 normalization with cabergoline can be achieved in about a third of the patients. Low baseline IGF-1 level (below 1.5 x ULN) before cabergoline initiation is a good predictor for remission. Combination treatment with the GH receptor antagonist pegvisomant can also be beneficial. The inexpensive, well-tolerated and convenient oral administration of cabergoline makes it an attractive medical therapy for active acromegaly.

中文翻译：

---

卡麦角林治疗肢端肥大症的现实价值

卡麦角林是一种麦角衍生物长效多巴胺受体2（DR2）选择性激动剂，口服给药，广泛用于治疗催乳素分泌腺瘤和帕金森病，DR2在大多数生长激素细胞腺瘤中表达。在肢端肥大症中，卡麦角林是超说明书使用的，其作用因实现激素缓解的效果相对有限而受到限制，因此，它主要适用于术后 GH/IGF-I 轻度升高的患者。它可以作为单一疗法，通常每周剂量高于治疗催乳素瘤所需的剂量，也可以作为对生长抑素受体配体奥曲肽或兰瑞肽部分反应的患者的附加治疗。大约三分之一的患者可以通过卡麦角林实现 IGF-1 正常化。卡麦角林开始治疗前的低基线 IGF-1 水平（低于 1.5 x ULN）是缓解的良好预测指标。与 GH 受体拮抗剂培维索孟联合治疗也可能有益。卡麦角林口服给药便宜、耐受性良好且方便，使其成为治疗活动性肢端肥大症的一种有吸引力的药物。