A Randomized, Double-blind, Placebo-controlled, Multicenter Trial Exploring the Efficacy and Safety of Intra-nasal Administration of Merotocin in Increasing Milk Production in Maternal Subjects With Preterm Delivery and Inadequate Milk Production

Induction and support of lactation in women with preterm delivery and inadequate milk production.

开始日期2021-05-28

申办/合作机构

Ferring Pharmaceuticals A/S

100 项与 Merotocin 相关的临床结果

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100 项与 Merotocin 相关的转化医学

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100 项与 Merotocin 相关的专利（医药）

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项与 Merotocin 相关的文献（医药）

2024-06-01·Breastfeeding Medicine

No Measurable Transfer of Oxytocin-Receptor Agonist Merotocin Detected in Human Breast Milk

Article

作者: Holmqvist, Carina ; Bagger, Yu ; Urban, Lorien E ; Hale, Thomas W ; Lorch, Ulrike ; Jonker, Daniël M ; Baker, Teresa

Objective: The study aimed to assess the transfer of merotocin from systemic circulation to breast milk in early postpartum women and women with established lactation. Methods: This was a two-part, multicenter, open-label, parallel-group study. Merotocin was administered as a single 90-minute intravenous (iv) infusion mimicking the intranasal pharmacokinetic profile. In Part A, 12 early postpartum women received doses of either 4 μg (n = 6) or 16 μg (n = 6) of merotocin within 4 days of delivery. In Part B, six women with established lactation received 20 μg of merotocin. The total concentration of merotocin in plasma and breast milk and its metabolites excreted in breast milk were measured at various time points. Adverse events (AEs) were also assessed for both parts of the study. Results: In both early postpartum and established lactation groups (mean age, 26.3 years; 83.3% Caucasian), merotocin and its metabolites in breast milk were below the limit of quantification (25.0 pg/mL) at all time points. Sixteen treatment-emergent AEs occurred in early postpartum women only, including seven events of uterine spasm and three of breast engorgement. There was one moderate event, whereas all the other events were considered mild. Conclusion: Merotocin was undetectable in breast milk after single iv administration of up to 20 μg in early postpartum women and women with established lactation.

2017-06-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Potent and selective oxytocin receptor agonists without disulfide bridges

4区 · 医学

Article

作者: Shimizu, Yuji ; Adachi, Yusuke ; Asami, Taiji ; Sakimura, Katsuya ; Nakayama, Masaharu ; Terao, Yasuko ; Yano, Takahiko

Oxytocin (OT) is a neuropeptide involved in a wide variety of physiological actions, both peripherally and centrally. Many human studies have revealed the potential of OT to treat autism spectrum disorders and schizophrenia. OT interacts with the OT receptor (OTR) as well as vasopressin 1a and 1b receptors (V_1aR, V_1bR) as an agonist, and agonistic activity for V_1aR and V_1bR may have a negative impact on the therapeutic effects of OTR agonism in the CNS. An OTR-selective agonistic peptide, FE 202767, in which the structural differences from OT are a sulfide bond instead of a disulfide bond, and N-alkylglycine replacement for Pro at position 7, was reported. However, the effects of amino acid substitutions in OT have not been comprehensively investigated to compare OTR, V_1aR, and V_1bR activities. This led us to obtain a new OTR-selective analog by comprehensive amino acid substitutions of OT and replacement of the disulfide bond. A systematic amino acid scanning (Ala, Leu, Phe, Ser, Glu, or Arg) of desamino OT (dOT) at positions 2, 3, 4, 5, 7, and 8 revealed the tolerability for the substitution at positions 7 and 8. Further detailed study showed that trans-4-hydroxyproline (trans-Hyp) at position 7 and γ-methylleucine [Leu(Me)] at position 8 were markedly effective for improving receptor selectivity without decreasing the potency at the OTR. Subsequently, a combination of these amino acid substitutions with the replacement of the disulfide bond of dOT analogs with a sulfide bond (carba analog) or an amide bond (lactam analog) yielded several promising analogs, including carba-1-[trans-Hyp⁷,Leu(Me)⁸]dOT (14) with a higher potency (7.2pM) at OTR than that of OT and marked selectivity (>10,000-fold) over V_1aR and V_1bR. Hence, we investigated comprehensive modification of OT and obtained new OT analogs that exhibited high potency at OTR with marked selectivity. These OTR-selective agonists could be useful to investigate OTR-mediated effects on psychiatric disorders.

100 项与 Merotocin 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Merotocin	-	DB12932

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
泌乳障碍	临床2期	-	Ferring BV	-
非产褥期溢乳	临床前	美国	Ferring Pharmaceuticals A/S	2021-05-28
早产	临床前	美国	Ferring Pharmaceuticals A/S	2021-05-28

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02545127 (MERMAID, CTgov)	临床2期	非产褥期溢乳 \| 早产	4	Merotocin (Merotocin (a Selective Oxytocin-receptor Agonist))	鏇願壓膚夢獵簾簾廠窪(顧襯觸蓋艱選夢餘鹹願) = 蓋窪觸壓蓋壓艱顧構鬱淵壓願鬱鬱製餘糧網簾 (蓋築觸範願遞築願遞選, 壓鬱獵簾鏇糧衊壓膚範 ~ 壓鹽繭糧網範衊壓願齋) 更多	-	2024-02-07
				Placebo (Placebo)	鏇願壓膚夢獵簾簾廠窪(顧襯觸蓋艱選夢餘鹹願) = 鬱鹽蓋製觸觸繭鑰壓選淵壓願鬱鬱製餘糧網簾 (蓋築觸範願遞築願遞選, 醖積壓廠蓋鹹醖餘顧觸 ~ 觸鑰築願壓蓋齋壓廠網) 更多