Delving into the Latest Updates on Barusiban with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

OXTR

Mechanism

OXTR antagonists(Oxytocin receptor antagonists)

Therapeutic Areas

Cardiovascular DiseasesUrogenital DiseasesOther Diseases

Active Indication-

Inactive Indication

Implantation complicationInfertilityInfertility, Female+ [3]

Originator Organization

Ferring BV

Active Organization-

Inactive Organization

Ferring Pharmaceuticals A/S

Ferring Pharmaceuticals SA

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC40H63N9O8S

InChIKeyUGNGRKKDUVKQDF-IHOMMZCZSA-N

CAS Registry285571-64-4

Sequence Code 528327495

A Randomised, Double-blind, Parallel Groups, Placebo-controlled, Multi-centre Study Assessing the Effects of a Selective Oxytocin Antagonist (Barusiban) and a Mixed Oxytocin Antagonist - Vasopressin V1a Antagonist (Atosiban) Administered Intravenously on Luteal Phase Uterine Contractions in Oocyte Donors Supplemented With Vaginal Progesterone

The main purpose of this clinical research trial was to evaluate the effects of barusiban and atosiban compared to placebo on luteal phase uterine contractions in oocyte donors supplemented with progesterone.

Start Date01 Nov 2007

Sponsor / Collaborator

Ferring Pharmaceuticals A/S

100 Clinical Results associated with Barusiban

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100 Translational Medicine associated with Barusiban

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100 Patents (Medical) associated with Barusiban

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15

Literatures (Medical) associated with Barusiban

01 Dec 2021·Reproductive BioMedicine OnlineQ3 · MEDICINE

Is oxytocin receptor antagonist administration around embryo transfer associated with IVF treatment success? A systematic review and meta-analysis

Q3 · MEDICINE

Review

Author: Griesinger, Georg ; Neumann, Kay

A systematic literature review and meta-analysis was conducted to evaluate whether the administration of an oxytocin receptor antagonist (OTR-a) around embryo transfer is associated with live birth and pregnancy achievement in IVF treatment. Multiple databases were searched for randomized controlled trials (RCT) comparing the outcome of IVF treatment with administration of an OTR-a before, during or after embryo transfer versus administration of placebo/nil. The literature search identified 11 eligible RCT. The active compound was intravenous atosiban (n = 7), subcutaneous barusiban (n = 1) and oral nolasiban (n = 3). Clinical pregnancy rate was significantly higher in women receiving an OTR-a around embryo transfer (relative risk [RR] 1.31, 95% confidence interval [CI] 1.13-1.51, P = 0.0002, I² = 61%, n = 11 studies, n = 3611); however, live birth rate was not statistically significantly affected (RR 1.09, 95% CI 0.98-1.20, P = 0.11, I² = 25%, n = 5 studies, n = 2765). A sensitivity analysis on low risk of bias studies likewise indicates a higher clinical pregnancy chance (RR 1.11, 95% CI 1.01-1.22, P = 0.03, I² = 5%, n = 5 RCT, n = 2765). OTR-a administration in IVF treatment has the potential to increase IVF efficacy, although the treatment effects observed so far are small and have not been sufficiently corroborated.

23 Jun 2020·Biology of ReproductionQ2 · BIOLOGY

Barusiban, a selective oxytocin receptor antagonist: placental transfer in rabbit, monkey, and human†

Q2 · BIOLOGY

Article

Author: Reinheimer, Torsten M ; Helmer, Hanns ; Petricevic, Ljubomir ; Saleh, Leila ; Knöfler, Martin

AbstractThe use of drugs in pregnancy always raises concerns regarding potential fetal exposure and possible adverse effects through their accumulation in fetal tissues and organs. Barusiban is an oxytocin antagonist under development for potential use as tocolytic in preterm-labor patients. It displays greater affinity for the oxytocin receptor compared to vasopressin V1A receptor and would thus not interfere with vasopressin-induced effects of the V1A receptor. Barusiban placental transfer was determined in the rabbit and cynomolgus monkey and in an ex vivo human cotyledon model. In the rabbit, there was an approximately 5% transfer of barusiban from the maternal to the fetal blood, without significant accumulation in any of the investigated fetal tissues. In the cynomolgus monkeys, the mean fetal plasma barusiban concentration was 9.1% of the maternal level. This was similar to the percentage of barusiban transfer in the human placental single cotyledon, which once equilibrated ranged between 9.3 and 11.0% over the observation period. The transfer of the small-molecule antipyrine as a comparator in this human model was approximately three times greater. The similarity in the degree of transfer in the cynomolgus monkey and human cotyledon, while being less in the rabbit, may reflect the species-specific placental barrier structure between the maternal and fetal compartments. In conclusion, limited placental transfer of barusiban occurred in all three models. The similarity of barusiban transfer in the cynomolgus and the human placental single cotyledon suggests the latter ex vivo model to be useful in assessing future drug candidates to be used in pregnant women.

01 Jan 2019·Methods in Molecular Biology

Design of Oxytocin Analogs

Review

Author: Wiśniewski, Kazimierz

The neurohypophyseal hormone oxytocin (OT) and related modulators of the oxytocin receptor (OTR) have been the subject of intensive research for nearly seven decades. Despite having rather poor drug-like properties, OT is used as a treatment for labor induction, postpartum hemorrhage, and lactation support. The potential use of OT in the treatment of central nervous system (CNS)-related diseases has recently renewed interest in the pharmacology of OT. Oxytocin is one of the most extensively studied cyclic peptides and since the elucidation of its structure in 1953 thousands of peptidic OT analogs with antagonistic and agonistic properties have been synthesized and biologically evaluated. Among them are atosiban, a mixed oxytocin receptor (OTR)/vasopressin 1a receptor (V_1aR) antagonist used as a tocolytic agent approved (in certain countries), and carbetocin, a longer acting OTR agonist on the market for the treatment of postpartum hemorrhage. Many other OT analogs with improved pharmacological properties (e.g., barusiban, Antag III) have been identified. These peptides have been tested in clinical trials and/or used as pharmacological tools. In this chapter, the modifications of the OT molecule that led to the discovery of these compounds are reviewed.

100 Deals associated with Barusiban

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Barusiban	-	DB12292

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Obstetric Labor, Premature	Phase 2	PL	Ferring Pharmaceuticals A/S	01 Nov 2003
Obstetric Labor, Premature	Phase 2	LT	Ferring Pharmaceuticals A/S	01 Nov 2003
Obstetric Labor, Premature	Phase 2	BE	Ferring Pharmaceuticals A/S	01 Nov 2003
Obstetric Labor, Premature	Phase 2	FI	Ferring Pharmaceuticals A/S	01 Nov 2003
Obstetric Labor, Premature	Phase 2	CZ	Ferring Pharmaceuticals A/S	01 Nov 2003
Infertility, Female	Phase 2	ES	Ferring Pharmaceuticals SA	-
Infertility, Female	Phase 2	CA	Ferring Pharmaceuticals SA	-
Infertility, Female	Phase 2	PL	Ferring Pharmaceuticals SA	-
Infertility, Female	Phase 2	CZ	Ferring Pharmaceuticals SA	-
Infertility, Female	Phase 2	BE	Ferring Pharmaceuticals SA	-