Delving into the Latest Updates on Norethisterone Enanthate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

NORETHISTERONE ENANTHAS, Norethisterone oenanthate

+ [4]

Target

PR

Mechanism

PR agonists(Progesterone receptor agonists)

Therapeutic Areas

Urogenital Diseases

Active Indication

InfertilityUterine Hemorrhage

Inactive Indication-

Originator Organization

Zhejiang Xianju Pharmaceutical Co., Ltd.

Active Organization

Zhejiang Xianju Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC27H38O3

InChIKeyAPTGJECXMIKIET-WOSSHHRXSA-N

CAS Registry3836-23-5

A Phase III, Multi-center, Prospective, Randomized, Double Blind, Single Dummy, Active Controlled, Comparative Clinical Study to Evaluate the Efficacy, Safety and Tolerability of Norethisterone CR Tablets 15 mg versus Norethisterone Tablets 5 mg to Arrest Bleeding in Women with Heavy Menstrual Bleeding (HMB) / Abnormal Uterine bleeding (AUB) due to Hormonal Imbalance.

Start Date03 Jun 2019

Sponsor / Collaborator

Synokem Pharmaceuticals Ltd.

100 Clinical Results associated with Norethisterone Enanthate

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100 Translational Medicine associated with Norethisterone Enanthate

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100 Patents (Medical) associated with Norethisterone Enanthate

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302

Literatures (Medical) associated with Norethisterone Enanthate

01 Nov 2023·American Journal of Reproductive Immunology

Contraceptive effects on the cervicovaginal microbiome: Recent evidence including randomized trials

Review

Author: Heffron, Renee ; Happel, Anna‐Ursula ; Jaspan, Heather B. ; Balle, Christina

AbstractBackgroundUntil recently, most data regarding the effects of non‐barrier contraceptives on the mucosal microbiome have derived from observational studies, which are potentially biased due to behavioral confounders that may mask their true biological effects.Method of StudyThis narrative review summarises recent evidence of the effect of contraceptives on the cervicovaginal microbiome, emphasising data obtained through randomized trials.ResultsGood quality data describe that initiation of long‐acting progestin‐only contraceptives, including levonorgestrel (LNG)‐implant and the injectables depot‐medroxyprogesterone acetate (DMPA‐IM) and norethisterone enanthate (NET‐EN) do not alter the mucosal microbial environment. Likewise, no strong evidence exists that the use of oral contraceptive pills (OCPs) is associated with alterations of the vaginal microbiome or increased risk of bacterial sexually transmitted infections (STIs). Limited data on the effect of intravaginal rings (IVRs) on the mucosal environment exist and show conflicting effects on the vaginal microbiota. Copper intrauterine device (Cu‐IUD) initiation has been associated with bacterial vaginosis (BV) acquisition, including in a randomized trial. LNG‐IUDs may have similar affects but need to be evaluated further.ConclusionDifferent synthetic hormones have divergent effects on the microbiome and therefore novel hormonal methods need to be rigorously evaluated. Furthermore, the addition of antiretrovirals into multipurpose technologies may alter the effects of the hormonal component. There is thus a critical need to improve our understanding of the biological effects of contraceptive hormones and delivery methods with different pharmacokinetic and chemical properties on the mucosal microbiome in rigorous trials, to inform the development of novel contraceptives and improve individual family planning guidance.

01 Aug 2021·American Journal of Reproductive ImmunologyQ3 · MEDICINE

Genital and systemic immune effects of the injectable, contraceptive norethisterone enanthate (NET‐EN), in South African women

Q3 · MEDICINE

Article

Author: Mchunu, Nobuhle ; Molatlhegi, Refilwe P. ; Zondi, Mthobisi M. ; Ngcapu, Sinaye ; Govender, Katya ; Samsunder, Natasha ; Leslie, Alasdair ; Ngcobo, Samkelisiwe ; Liebenberg, Lenine J. P. ; Adamson, John H. ; Sivro, Aida ; Mabhula, Amanda ; Karim, Quarraisha Abdool ; Passmore, Jo‐Ann S. ; McKinnon, Lyle R. ; Karim, Salim S. Abdool

AbstractProblemInjectable hormonal contraceptives (IHC) have been associated with altered mucosal and systemic milieu which might increase HIV risk, but most studies have focused on DMPA and not NET‐EN, despite the growing popularity and lower HIV risk associated with the latter in observational studies.Method of studyWe used high‐performance liquid chromatography in combination with tandem triple quadrupole mass spectrometry (HPLC‐LC‐MS/MS) to measure steroid hormones in plasma samples of CAPRISA004 study participants. Concentrations of 48 cytokines were measured in the cervicovaginal lavage (CVL) and plasma, and their expression was compared between participants with detectable NET‐EN (n = 201) versus non‐detectable IHC (n = 90). Each log10 cytokine concentration was tested as an outcome in linear‐mixed models, with NET‐EN detection as the main explanatory variable. Multivariable models were adjusted for potential confounders.ResultsIn bivariate analysis, detectable NET‐EN was associated with reduced cervicovaginal M‐CSF (P = 0.008), GM‐CSF (P = 0.025) and G‐CSF (P = 0.039), and elevated levels MIF (P = 0.008), IL‐18 (P = 0.011), RANTES (P = 0.005) and IL‐1Rα (P < 0.001). Lower G‐CSF (P = 0.011) and elevated IL‐1Rα (P = 0.008) remained significant in adjusted models. Multivariable analyses of plasma samples obtained from NET‐EN‐detectable women showed a significant increase in IP‐10 (P = 0.026) and reductions in TNF‐β (P = 0.037), RANTES (P = 0.009), and M‐CSF (P < 0.001). While similar growth factor reduction in CVL was noted for both DMPA and NET‐EN, similar trends were not observed for endogenous progesterone.ConclusionsDetectable NET‐EN was associated with reduced growth factors in the plasma and genital tract; particularly G‐CSF and M‐CSF. Our results suggest that while NET‐EN is not inflammatory, it may have important immunological effects.

01 Jul 2021·American Journal of Reproductive ImmunologyQ3 · MEDICINE

Effect of injectable progestin‐only contraceptives, depot medroxyprogesterone acetate and norethisterone enanthate, on cytokine production during T‐cell activation

Q3 · MEDICINE

Article

Author: Mhlanga, Felix ; Mbizvo, Mike ; Stoner, Kevin A. ; Meyn, Leslie A. ; Chirenje, Zvavahera M. ; Maramba, Aaron ; Achilles, Sharon L. ; Hillier, Sharon L. ; Matubu, Allen T.

AbstractProblemThere is paucity of human data about the effects of depot medroxyprogesterone (DMPA) and norethisterone enanthate (Net‐En) use on systemic immune function, which may have implications for reproductive tract infection susceptibility and transmissibility. We sought to evaluate the impact of injectable contraceptive use on T‐cell responsiveness using T cells exposed in vivo and tested ex vivo.MethodsPeripheral blood mononuclear cells were obtained from healthy, HIV‐negative women after 30, 90 and 180 days of DMPA, norethisterone enanthate (Net‐En) or copper intrauterine device (Cu‐IUD) contraceptive use. Cells were stimulated ex vivo with phorbol myristate acetate and ionomycin, stained and analysed using flow cytometry. Mixed‐effects linear models were used to evaluate change in proportions of T cells producing IFN‐γ, TNF‐α, IL‐4 and IL‐13.ResultsCompared with baseline, decreased proportions of IFN‐γ–producing CD4+ and CD8+ T cells (p = .003, p = .006, respectively) and TNF‐α–producing CD4+ and CD8+ T cells (p = .039, p = .034, respectively) were observed after 180 days of DMPA use. Decreased IL‐4–producing CD4+ and CD8+ T cells (p = .045 and p = .024, respectively) were noted after 180 days of Net‐En use. Decreased IL‐4–producing CD4+ T cells were observed after 30 days (p = .035) and not after 180 days of DMPA use (p = .49). There were no changes in proportion of T cells producing IL‐13 in DMPA users, nor any changes in IFN‐γ, TNF‐α and IL‐13 in Net‐En and Cu‐IUD users.ConclusionIn vivo exposure of CD4+ and CD8+ T cells to typical pharmacologic concentrations of DMPA does not cause broad suppression to stimuli; however, depletion of specific cytokine‐producing T cells may occur after prolonged DMPA use.

100 Deals associated with Norethisterone Enanthate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Norethisterone Enanthate	G03AC01 G03DC02	DB14678

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Infertility	CN	Zhejiang Xianju Pharmaceutical Co., Ltd.	-
Uterine Hemorrhage	CN	Zhejiang Xianju Pharmaceutical Co., Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


MDP 301 (IAS2018)	Not Applicable	Herpes Simplex	621	Depo-medroxyprogesterone acetate (DMPA)	rhrvhhnnsz(ulihbrwvhl) = tifijwnmoc gsqmljnblo (qecpqdwray )	-	01 Jan 2018
				Norethisterone enanthate (Net-EN)	rhrvhhnnsz(ulihbrwvhl) = mxdybtfcjh gsqmljnblo (qecpqdwray )
IAS2016	Not Applicable	HIV Infections	232	Depot medroxyprogesterone acetate (DMPA)	oxttevgwgm(spsdjvcnnz): Unadjusted HR = 0.67 (95% CI, 0.24 - 1.85); Adjusted HR = 0.71 (95% CI, 0.26 - 1.97) View more	-	01 Jan 2016
				Norethisterone enanthate (NET-EN)