Department of Medicine 1, Endocrinology, Friedrich-Alexander University Erlangen-Nürnberg, 91054, Erlangen, Germany.
Department of Hepatology and Gastroenterology, Charité-Universitätsmedizin Berlin, Humboldt University, Berlin, Germany.
Cancer Chemother Pharmacol. 2019 Feb;83(2):375-385. doi: 10.1007/s00280-018-3734-1. Epub 2018 Dec 8.
Octreotide SC depot is a novel, ready-to-use formulation administered via a thin needle. In a phase 1 study in healthy volunteers, this formulation provided higher bioavailability of octreotide with faster onset and stronger suppression of IGF-1 in healthy volunteers versus long-acting intramuscular (IM) octreotide. This phase 2 study evaluated the pharmacokinetics, efficacy, and safety of octreotide SC depot in patients with acromegaly and functioning NETs, previously treated with octreotide IM.
Adult patients with acromegaly or functioning NETs treated for ≥ 2 months with octreotide IM [10/20/30 mg every 4 weeks (q4w)] received the last dose of octreotide IM treatment in study period 0 and were randomized 28 days later to receive octreotide SC depot 10 mg q2w, or 20 mg q4w for 3 months (period 1). The primary objective was to characterize the PK profile of octreotide SC depot after each injection vs PK for octreotide IM (period 0).
Twelve patients were randomized to receive octreotide SC depot 10 mg q2w (acromegaly n = 3; NET n = 1) or 20 mg q4w (acromegaly n = 4; NET n = 4). Plasma levels of octreotide were higher with octreotide SC depot as compared to octreotide IM. Adverse events were reported in 6 and 8 patients during period 0 and period 1, respectively; most common in period 1 were gastrointestinal disorders.
Octreotide SC depot provided higher exposure (AUC) than octreotide IM, maintained biochemical control in patients with acromegaly and symptom control in patients with functioning NETs, and was well tolerated with a safety profile consistent with octreotide IM. CLINICALTRIALS.
NCT02299089.
奥曲肽 SC depot 是一种新型的即用型制剂，通过细针给药。在一项健康志愿者的 1 期研究中，与长效肌内（IM）奥曲肽相比，这种制剂使奥曲肽具有更高的生物利用度，起效更快，对 IGF-1 的抑制作用更强。这项 2 期研究评估了奥曲肽 SC depot 在先前接受 IM 奥曲肽治疗的肢端肥大症和功能性 NET 患者中的药代动力学、疗效和安全性。
接受 IM 奥曲肽治疗≥2 个月的肢端肥大症或功能性 NET 成年患者[10/20/30mg 每 4 周（q4w）]在研究期 0 内接受最后一次 IM 奥曲肽治疗，并在 28 天后随机分为接受奥曲肽 SC depot 10mg q2w 或 20mg q4w 治疗 3 个月（第 1 期）。主要目的是描述每次注射后的奥曲肽 SC depot 药代动力学特征与 IM 奥曲肽的药代动力学特征（期 0）。
12 名患者被随机分为接受奥曲肽 SC depot 10mg q2w（肢端肥大症 n=3；NET n=1）或 20mg q4w（肢端肥大症 n=4；NET n=4）。与 IM 奥曲肽相比，奥曲肽 SC depot 的奥曲肽血浆水平更高。在期 0 和期 1 期间，分别有 6 名和 8 名患者报告了不良事件；在期 1 中最常见的是胃肠道疾病。
奥曲肽 SC depot 提供了比 IM 奥曲肽更高的暴露（AUC），维持了肢端肥大症患者的生化控制和功能性 NET 患者的症状控制，且具有良好的耐受性，安全性与 IM 奥曲肽一致。临床试验。
.gov 标识符：NCT02299089。
