Delving into the Latest Updates on Ormeloxifene with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ormeloxifene (INN), Centron, Choice 7

+ [1]

Target

ER

Mechanism

ERs modulators(Estrogen receptors modulators)

Therapeutic Areas

Urogenital DiseasesOther Diseases

Active Indication

ContraceptionUterine Hemorrhage

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

(01 Jan 1991),

ContraceptionUterine Hemorrhage

Regulation-

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Structure/Sequence

Molecular FormulaC30H35NO3

InChIKeyXZEUAXYWNKYKPL-ZTMACLEXSA-N

CAS Registry31477-60-8

ABSTRACTIntroduction:India is committed to achieving universal health care for all by 2030. The objective of social marketing is to promote public health and its goal is to improve health for all, but there are some challenges like irregular availability, quality issue, inadequacy of marketing causes under- utilization of the government supplied health consumables.Objectives:Present study aims to find out the usage pattern and assess the perceived satisfaction level of beneficiaries of using various socially marketed health consumables at government settings and explore the perception of healthcare personnel regarding barriers to its usage in a rural area of India.Materials and Methods:A community-based, Mixed-Methods study (Convergent parallel design) was done in the service area of the Rural Health Unit and Training Centre (RHU&TC), Singur of Hooghly district, West Bengal, between January 2023 and December 2023, where the quantitative component was carried out by face-to-face interview among 150 beneficiary household respondents selected by two-stage cluster sampling; and qualitative component was done by 4 Key informant interviews (KII) among healthcare personnel (medical officer, public health nurse, pharmacist). Statistical data were analyzed by descriptive statistics using SPSS 16 version and Microsoft Excel for the quantitative part, and thematic analysis was done for the qualitative part. Institutional Ethics Committee clearance was obtained.Results:Ever use of government-supplied contraceptives like Chhaya (Ormeloxifene), Antara (Injectable contraceptive), emergency contraceptive pills, and intrauterine contraceptive devices (IUCD) was done by only 15.3%, 10.7%, 7.3%, 32% of eligible beneficiary households, respectively. The major reasons cited for irregular use were unawareness of availability of the products (Chhaya = 76.3%, Antara = 64.9%, EC pills = 46.7%), poor faith regarding quality (Male condom = 40%, Generic medicines = 70%), inadequate promotion (IUCD = 53.9%). The majority of users of male condoms (90%), IFA tablets (52.9%), ORS (51.1%), and generic medicines (55.7%) were not satisfied after using those products. Key informant interviews among healthcare personnel revealed avoidance of using modern contraceptive methods and frequent unavailability of some socially marketed health consumables were the predominant causes of reduced uptake of those products by beneficiaries.Conclusions:Proper social marketing strategies, adequate promotion, regular awareness campaigns, and tailored training of field healthcare workers are required to improve the acceptability, availability, and marketing of these health consumables.

01 Oct 2024·Journal of Medical Virology

The antimicrobial protein RNase 7 directly restricts herpes simplex virus infection of human keratinocytes

Article

Author: Rademacher, Franziska ; Klug, Ilona ; Harder, Jürgen ; Zeitvogel, Jana ; Döhner, Katinka ; Werfel, Thomas ; Sodeik, Beate ; Gläser, Regine

AbstractApproximately 22% of moderately to severely affected atopic dermatitis (AD) patients have a history of eczema herpeticum, a disseminated rash primarily caused by herpes simplex virus type 1 (HSV‐1). Reduced activity of antimicrobial peptides may contribute to the increased susceptibility of AD patients to HSV‐1. We previously demonstrated that the antimicrobial protein RNase 7 limits HSV‐1 infection of human keratinocytes by promoting self‐DNA sensing. Here, we addressed whether RNase 7 has any effect on HSV‐1 infection when infecting keratinocytes without exogenously added costimulatory DNA, and which step(s) of the infection cycle RNase 7 interferes with. We quantified viral gene expression by RT‐qPCR and flow cytometry, viral genome replication by qPCR, virucidal effects by plaque titration, and plaque formation and the subcellular localization of incoming HSV‐1 particles by microscopy. Recombinant RNase 7 restricted HSV‐1 gene expression, genome replication, and plaque formation in human keratinocytes. It decreased HSV‐1 immediate‐early transcripts independently of the induction of interferon‐stimulated genes. Its main effect was on intracellular infection processes and not on extracellular virions or virus binding to cells. RNase 7 reduced the amount of cell‐associated capsids and the HSV‐1 envelope glycoprotein D at 3 but not at 0.5 h postinfection. Our data show that RNase 7 directly restricts HSV‐1 infection of human keratinocytes, possibly by promoting the degradation of incoming HSV‐1 particles. This suggests that RNase 7 may limit HSV‐1 spread in the skin and that mechanisms that reduce its activity in the lesional skin of AD patients may increase their susceptibility to eczema herpeticum.

01 Jul 2024·Phytotherapy Research

7‐Hydroxyflavone improves nonalcoholic fatty liver disease by acting on STK24

Article

Author: Liao, Qichao ; Zhang, Yurou ; Zhou, Lei ; Jiang, Tianyu ; Qi, Xinyi ; Li, Yixing ; Liu, Siqi ; Xiao, Yang

AbstractThe escalating incidence of nonalcoholic fatty liver disease (NAFLD) is closely associated with a high‐fat diet, leading to a decline in quality of life and significant health impairment. 7‐Hydroxyflavone (7‐HY) is a flavonoid known for its anti‐inflammatory, anticarcinogenic, and antioxidant effects. This study aims to assess the ameliorative effects of 7‐HY on NAFLD induced by a high‐fat diet and elucidate underlying mechanisms. Oleic acid/palmitic acid‐induced HepG2 cells and C57BL/6 mice on a high‐fat diet were utilized as in vitro and in vivo models. In animal experiments, 7‐HY was utilized as a dietary supplement. The 15‐week in vivo experiment monitored body weight, body fat percentage, glucose tolerance, insulin tolerance, and metabolic indexes. Commercial kits assessed triglyceride (TG) and total cholesterol levels in cells, liver tissue, and blood. Discovery Studio identified potential targets of 7‐HY, compared with NAFLD‐associated targets in the GeneCards database. Results indicated 7‐HY mitigated fat accumulation, hepatic steatosis, and oxidative stress induced by a high‐fat diet. Furthermore, 7‐HY showed potential efficacy in ameliorating abnormal glucose metabolism and promoting energy metabolism. Reverse target finding and molecular docking demonstrated a robust interaction between 7‐HY and serine/threonine kinase 24 (STK24). Subsequent experimental results confirmed 7‐HY's ability to inhibit TG deposition in HepG2 cells through interaction with STK24. In conclusion, 7‐HY demonstrated the capacity to alleviate high‐fat diet‐induced NAFLD, presenting a novel strategy for the prevention and treatment of NAFLD.

100 Deals associated with Ormeloxifene

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External Link

KEGG	Wiki	ATC	Drug Bank
D08301	Ormeloxifene	G03XC04	DB13310

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Contraception	-	-	01 Jan 1991
Uterine Hemorrhage	-	-	01 Jan 1991

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


EHA2023	Not Applicable	Acute Myeloid Leukemia	-	CPX-351	(zzfikmnupd) = hdszoyigsg iiinqtkvdn (orbkilwwjo ) View more	-	08 Jun 2023
				7+3 chemotherapy	(zzfikmnupd) = cvvakemhod iiinqtkvdn (orbkilwwjo ) View more
EHA2022	Not Applicable	High Risk Myelodysplastic Syndrome	76	CPX-351	(hocyuznohm) = defcodpazk pfgxrcbphm (txuomjwety ) View more	-	12 May 2022
				FLAG-IDA	(hocyuznohm) = rtvdhjihce pfgxrcbphm (txuomjwety )
EHA2022	Not Applicable	Acute Myeloid Leukemia	189	Standard dose anthracycline	hlkxyruage(fadurtlyqe) = mzfculziqr ubaiceroag (fmkxljyukj )	-	12 May 2022
				Higher dose anthracycline	hlkxyruage(fadurtlyqe) = pdsastvvtb ubaiceroag (fmkxljyukj )
EHA2020	Not Applicable	FLT3 positive Acute Myeloid Leukemia	9	7+3-Ida and midostaurin	hfedoowuje(mzheprjzru) = Early mortality rate (30-days) was noted to be 22% (n=2). Death was secondary to disease complication of sepsis and respiratory failure mquvbizjan (ntbprlxgri ) View more	-	14 May 2020
EHA2019	Phase 3	Acute Myeloid Leukemia Consolidation	309	CPX-351	(fobvlyjnfu) = rmkpnizrta cxgmqqvlje (jqfcbeddyn ) View more	Positive	14 Jun 2019
				7+3	(fobvlyjnfu) = prhwvpledx cxgmqqvlje (jqfcbeddyn ) View more
EHA2019	Phase 3	Acute Myeloid Leukemia Consolidation	309	CPX-351	(rclxtmlbhk) = qkmktezbhq fehdsedwuc (jiqslwmbap )	-	16 May 2019
				7+3	(rclxtmlbhk) = qwwihocjeg fehdsedwuc (jiqslwmbap )
EHA2017	Phase 3	Acute Myeloid Leukemia Consolidation	-	CPX-351	ixrfjnpglk(hpcwcoxfnf) = no clinically meaningful differences in the rates of grade ≥3 treatment-emergent adverse events, including febrile neutropenia (68% vs 71%, respectively) and infections (55% vs 51%) yymdfabgaa (rnktmbvymq )	Positive	18 May 2017
				7+3 chemotherapy
ASCO2016	Not Applicable	Acute Myeloid Leukemia	100	7+3	(xbibqtmrez) = kejrxfzxgc zbrwooxrlr (kszqnyzllu ) View more	Positive	20 May 2016
				7+3 plus nilotinib	(xbibqtmrez) = miwslnejil zbrwooxrlr (kszqnyzllu ) View more