Delving into the Latest Updates on Estradiol Dipropionate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Estradiol dipropionate (JAN), Ovahormon

Target

ER

Action

agonists

Mechanism

ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Oestrogen deficiency

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC24H32O4

InChIKeyJQIYNMYZKRGDFK-RUFWAXPRSA-N

CAS Registry113-38-2

To explore how estrogen deficiency impacts the blood pressure (BP) and sympathetic nerve activity (SNA), and how it impacts the production of the key pro-inflammatory mediators such as Tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6). It is hypothesized that estrogen deficiency increases BP, SNA and the pathway activities of the key pro-inflammatory mediators. Those effects are impacted through the downregulation of the estrogen receptor.

Start Date01 Sep 2025

Sponsor / Collaborator

Hershey Medical Center

CTIS2024-517969-16-00

/ Not yet recruitingPhase 1

- CIM24001

Start Date12 Mar 2025

Sponsor / Collaborator-

100 Clinical Results associated with Estradiol Dipropionate

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100 Translational Medicine associated with Estradiol Dipropionate

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100 Patents (Medical) associated with Estradiol Dipropionate

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968

Literatures (Medical) associated with Estradiol Dipropionate

09 Jan 2025·Histology and histopathology

Structure and hormonal output of the adrenal gland after experimental estrogenization of male rats.

Article

Author: Šošić-Jurjević, Branka ; Ajdžanović, Vladimir ; Ćosić, Pavle ; Manojlović-Stojanoski, Milica ; Trifunović, Svetlana ; Miler, Marko ; Filipović, Branko

Orchidectomy and estrogenization of the male represent a procedure that is applicable in sex reassignment or in prostate cancer therapy. This approach has an influence on the hypothalamic-pituitary-adrenal axis and thus affects cardiovascular function and metabolism. We utilized orchidectomized rats to evaluate the effects of estradiol on the structure and hormonal output of the adrenal gland. Adult Wistar rats were divided into sham-operated (SO; n=7), orchidectomized (Orx; n=7), and estradiol-treated orchidectomized (Orx+E; n=7) groups. Estradiol-dipropionate (0.625 mg/kg b.m.) was administered subcutaneously for three weeks, while the SO and Orx groups received vehicle alone. Set objectives were achieved using histochemistry/immunohistochemistry, stereology, and immunoassays. In Orx+E rats, the hormonal milieu was characterized by decreased testosterone and increased ACTH, compared with the Orx group. Also, orchidectomy and estradiol treatment provoked a significant increase in adrenal cortex volume and volume of ZF per se, with increased cell and nuclei volumes in all three adrenocortical zones (ZG, ZF, and ZR), in comparison with Orx rats. Concentrations of aldosterone in blood, as well as corticosterone in blood and adrenal tissue were increased, while circulating DHEA was decreased (with increased immunoexpression of adrenocortical CYP 17 enzyme), all in Orx+E compared with Orx animals. The wide zonal distribution of VEGF and the pronounced blood supply within the ZF of Orx+E animals acted to support the synthesis and secretion of corticosteroids. These results seem cautionary in the context of young male estrogenization, given the negative impact of high mineralocorticoids and glucocorticoids on cardiovascular function and metabolism.

01 Jan 2023·Animal Science Journal

Effect of pseudopregnancy duration in nonpregnant sows on induced lactation

Article

Author: Sakatsume, Yoshihiro ; Tachino, Hirokazu ; Noguchi, Michiko ; Kasazaki, Takayuki ; Suzuki, Takehito

AbstractThis study was conducted to examine the effects of different pseudopregnancy periods in nonpregnant sows on artificial lactation induction efficiency and milk composition. Sixteen pseudopregnant sows (n = 4 per group) were treated with 5 mg of estradiol dipropionate at 28 (Group D38), 35 (Group D45), 42 (Group D52), and 49 (Group D59) days after the end of estrus, followed by prostaglandin F2α as 0.175‐mg cloprostenol twice at 12 h intervals 10 days later. The overall success rate of lactation induction was 81.3%. The lactation rates were significantly higher in Groups D38, D45, and D59 (100.0%) than in Group D52 (25.0%). The milk immunoglobulin (Ig) G concentration was significantly higher in Group D38 than in Group D59. However, IgA levels and milk compositions (protein, ash, and lactose) did not differ among the groups. Lactation induction was successful between 38 and 59 days of pseudopregnancy. Apart from IgG, pseudopregnancy length did not affect milk components from 38 to 59 days of pseudopregnancy.

01 Jul 2022·Arabian Journal of Chemistry

Investigation of fragmentation behaviors of steroidal drugs with Li+, Na+, K+ adducts by tandem mass spectrometry aided with computational analysis

Author: Akhtar, Naheed ; Tehreem, Syeda ; Ali, Arslan ; Ghulam Musharraf, Syed ; Mohammad Zaki Shah, Syed ; Uddin, Jalal ; Usama Yaseen Jeelani, Syed ; El-Seedi, Hesham R. ; Zareena, Bibi ; Khadim, Adeeba

In this study, we have investigated the fragmentation of the widely used steroidal pharmaceutical drugs (n = 14), complexed by a singly charged proton or alkali metal ion (Li⁺, Na⁺, K⁺) using Ion trap and quadrupole time-of-flight mass spectrometers.Spectra were collected by LC-MS/MS anal. using system automated collision energy i.e., of 25-60 eV.Theor. calculations were also calculated using DFT software.The metal complexes showed different fragmentation pathways not commonly observed for protonated compoundsThere was a distinct difference observed in the relative intensities of some common fragments for free vs. metalated drugs.Some major fragments from protonated and lithium adducts showed close resemblance, while sodium and potassium adducts showed different fragments.Theor. calculations showed a distinct difference in the position of attachment of proton and metals.This adducts ion fragmentation information will be helpful for the identification of these compounds in complex samples.

17

News (Medical) associated with Estradiol Dipropionate

13 Mar 2025

·pmlive.com

NICE recommends Gideon Richter’s Ryeqo as first daily pill for endometriosis

The National Institute for Health and Care Excellence (NICE) has recommended Gideon Richter’s Ryeqo (relugolix, estradiol and norethisterone) as the first long-term daily pill for endometriosis. NICE has recommended in final draft guidance that the relugolix combination therapy be used on the NHS in England to treat the symptoms of endometriosis in adults of reproductive age who have had medical or surgical treatment for the chronic condition. The health technology assessment agency’s decision follows an earlier negative recommendation and comes after Gideon provided new evidence on the Ryeqo’s effectiveness and value for money. Affecting approximately 1.5 million women in the UK, endometriosis occurs when tissue similar to the lining of the uterus grows elsewhere in the body. Patients can experience a range of symptoms, including dysmenorrhoea (painful cramping, usually in the lower abdomen), heavy bleeding and pelvic pain. Ryeqo is designed to block the specific hormones that contribute to endometriosis while also providing necessary hormone replacement in a single daily tablet. NICE estimates that around 1,000 patients per year could benefit from the therapy. Helen Knight, director of medicines evaluation at NICE, said Ryeqo “marks a potential step-change in how we manage endometriosis”. She continued: “Instead of travelling to clinics for injections, there is now a daily tablet that can be taken at home. The treatment can also be stopped and started more easily, which is particularly important for those planning to have children and for managing side effects.” Among the clinical evidence supporting NICE’s recommendation were positive results from the late-stage SPIRIT programme, in which significantly more patients achieved pain reduction with Ryeqo versus placebo at 24 weeks. In the SPIRIT 1 study, 75% of patients responded to Ryeqo for their dysmenorrhoea compared to 27% in the placebo arm. The same result was seen in SPIRIT 2, with 75% of dysmenorrhoea responders in the Ryeqo cohort compared to 30% for placebo. Additionally, 59% and 66% of patients responded to Ryeqo for their non-menstrual pelvic pain (NMPP) in SPIRIT 1 and 2, respectively, compared to 40% and 43% of those receiving placebo. Positive long-term efficacy data from the SPIRIT open-label extension study, which showed that dysmenorrhoea and NMPP reduction was sustained over two years with Ryeqo treatment, also supported the agency’s decision.

Clinical ResultDrug Approval

05 Sep 2024

·pmlive.com

MHRA authorises first in new class of treatment for endometriosis symptoms

The Medicines and Healthcare Products Regulatory Agency (MHRA) has granted a licence for Gedeon Richter’s Ryeqo for adults with endometriosis symptoms, making it the first in a new class of treatments authorised in the UK for this patient population. Those eligible to receive the combination therapy, which consists of non-peptide gonadotrophin-releasing hormone receptor antagonist relugolix 40mg, estradiol 1mg and norethisterone acetate 0.5mg taken in a single once-daily tablet, will be of reproductive age and have a history of previous medical or surgical treatment for their endometriosis. Affecting approximately 176 million women worldwide, endometriosis is a chronic condition that occurs when tissue similar to the lining of the uterus grows outside of the uterus. Patients can experience a range of symptoms, including dysmenorrhoea (painful cramping, usually in the lower abdomen), heavy bleeding and pelvic pain, and the disease can be associated with sub-fertility or infertility. The MHRA’s decision was supported by positive results from the late-stage SPIRIT programme, in which significantly more patients achieved pain reduction with Ryeqo versus placebo at 24 weeks. In the SPIRIT 1 study, 75% of patients responded to Ryeqo for their dysmenorrhoea compared to 27% in the placebo arm. The same result was seen in the SPIRIT 2 trial, with 75% of dysmenorrhoea responders in the Ryeqo cohort compared to 30% for placebo. Additionally, 59% and 66% of patients responded to Ryeqo for their non-menstrual pelvic pain (NMPP) in SPIRIT 1 and 2, respectively, compared to 40% and 43% of those receiving placebo. Dysmenorrhoea and NMPP reduction was also sustained over two years with Ryeqo treatment, according to results from a long-term extension study. David Jordan, medical director UK and Ireland, Gedeon Richter, said: “The MHRA’s decision to licence relugolix combination therapy in endometriosis is fantastic news and we are delighted the need for more treatment options has been recognised. “We have been working hard to bring a new way of treating the condition to clinicians and women suffering with painful symptoms and we believe this authorisation will be a welcome step for redefining care.” Jordan added that the company is now engaging with the relevant health authorities throughout the UK “with a view to securing NHS reimbursement as soon as possible.”

Clinical ResultDrug Approval

11 Jul 2024

·www.drugs.com

Testosterone Tied to Incidence, Progression of Metabolic Syndrome

THURSDAY, July 11, 2024 -- Testosterone is associated with a greater risk for development and progression of metabolic syndrome, particularly in transmasculine individuals, according to a study published online July 2 in JAMA Network Open . Leila Hashemi, M.D., from the David Geffen School of Medicine in Los Angeles, and colleagues assessed whether gender-affirming hormone treatment (GAHT) by proxy steroid is associated with development and progression of metabolic syndrome. The analysis included 645 transgender participants and 645 matched cisgender participants. The researchers found that metabolic syndrome z-scores changed significantly over time and differed significantly across groups. Transmasculine participants had the greatest percentage increase in mean z-scores after versus before the index GAHT date (298.0 percent), followed by cisgender females (108.3 percent), cisgender males (49.3 percent), and transfeminine persons (3.0 percent). "In both cisgender and transgender individuals, estradiol was associated with reduced metabolic syndrome risk, whereas testosterone was associated with increased risk. These findings are relevant for the management of metabolic syndrome risk factors in cisgender and transgender individuals," the authors write. "It is also important to note that exogenous sex hormones are not equivalent to endogenous sex hormones, nor is the body in which they operate the same as one never exposed to the opposing sex hormones." Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

Clinical Result

100 Deals associated with Estradiol Dipropionate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01617	Estradiol Dipropionate	G03CA03	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Oestrogen deficiency	-	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04036500 (CTgov)	Early Phase 1	-	11	Estradiol	hawvjwupbt(rbbmfczcsb) = kslfiddoev rirtsejxyb (glyegozsfv, ajkpvnzpqt - xjzimnifir) View more	-	01 Apr 2025
NCT04283656 (IDENTIFY, CTgov)	Phase 1	HIV Infections	8	Estradiol 2mg+Spironolactone 100mg+Doravirine/Lamivudine/Tenofovir (Treatment C)	clepffvqnx(yehjeczspl) = qinwkhxrtx fiwpabsvou (qivwsxocqr, dojkgwpomv - ezeqtauygo) View more	-	26 Mar 2025
				Doravirine/Lamivudine/Tenofovir (Treatment A)	clepffvqnx(yehjeczspl) = zccizchyuy fiwpabsvou (qivwsxocqr, jfuwglgsyk - gslnhtcoyy) View more
ENDO2023	Not Applicable	-	22	Sublingual Estradiol (SLE)	(utflvcxxtu) = dixakwfoyr truxazuhaq (jdfgsgfmlz ) View more	Negative	05 Oct 2023
NCT04051320 (CTgov)	Phase 2	Depression, Postpartum \| Irritable Mood	23	Estradiol 2 Mg tablet+Micronized progesterone+Leuprolide Acetate 3.75 MG/ML (Hormone Sensitive Women (HS+))	sbnrordvjk(hskcroorja) = drowuluayd xriwgijaur (wmcpdymrji, aqhepbtbpz - lsfmkhjpnx) View more	-	25 Aug 2023
				Estradiol 2 Mg tablet+Micronized progesterone+Leuprolide Acetate 3.75 MG/ML (Hormone Insensitive Women (HS-))	sbnrordvjk(hskcroorja) = bfjgjknvyo xriwgijaur (wmcpdymrji, evqxbslqka - oqordkugsv) View more
NCT02122198 (CTgov)	Not Applicable	Cognitive Dysfunction \| Endothelial dysfunction \| Impairment of Executive Functions	17	Placebo (Placebo)	ncdjuhyzyf(zalemtcntw) = rketmosixs jxqlnjylzi (xwrsjxwtol, syfvuackhs - zjosbubdag) View more	-	10 Jan 2022
				Medroxyprogesterone+Estradiol+Leuprolide acetate (GnRH Agonist)	ncdjuhyzyf(zalemtcntw) = wypxmccziz jxqlnjylzi (xwrsjxwtol, jkgmjfzjxj - xvcujvviki) View more
NCT03493126 (CTgov)	Phase 4	Vulvovaginal atrophy \| Perineal pain	59	Estradiol (Estradiol)	smpjaababx(mxklncsief) = avguycrgjq hpzfebpcgd (bqnkukerms, jsorfehwrw - azrtxoqtzv) View more	-	22 Dec 2021
				Placebo (Placebo)	smpjaababx(mxklncsief) = vutwplzhro hpzfebpcgd (bqnkukerms, ptmtlfgthq - sfridujllb) View more
NCT03003949 (Changes, CTgov)	Phase 4	-	82	Placebo Oral Capsule (Placebo Patch and Placebo Capsule)	kdnqgmlexl(qltpumgupf) = ygcwzxrhuq dkvithnwbc (qetbraalsa, nysknlihza - gzrftpnssr) View more	-	26 Mar 2021
				Estradiol+Progesterone Capsule (Estradiol Patch and Progesterone Capsule)	kdnqgmlexl(qltpumgupf) = wtroiibnay dkvithnwbc (qetbraalsa, txvpahjdrt - hxhglzyzaq) View more
NCT00687739 (POWER, CTgov)	Phase 3	Oestrogen deficiency \| Obesity	79	placebo+leuprolide acetate (GnRHag+PL)	qwlycvozlo(lvrzyukpod) = ngbkqkzxmu btpxluegwa (onjhobeqjn, bnyqzmvoks - gpwfyisaaz) View more	-	09 Dec 2019
				placebo+leuprolide acetate (GnRHag+PL+ex)	qwlycvozlo(lvrzyukpod) = stznmpqxbi btpxluegwa (onjhobeqjn, hpiwmxbwfa - fllznqwnil) View more
NCT01709318 (P06109 \| MK-8175A/MK-8342B-012, CTgov)	Phase 2	Hemorrhage \| Contraception	666	Estradiol+E2+NOMAC (Nomegestrol Acetate-17β-Estradiol (NOMAC-E2) 500/300 μg/Day)	maoeybfvfc(wpolnrioqi) = kmgmehtmku noiptvemol (ayhvxiittf, zwkozvqqee - czdmbbulxx) View more	-	05 Dec 2019
				Estradiol+E2+NOMAC (Nomegestrol Acetate-17β-Estradiol (NOMAC-E2) 700/300 μg/Day)	maoeybfvfc(wpolnrioqi) = ditryrxsck noiptvemol (ayhvxiittf, naxjwpruvx - axlnqyoojb) View more
NCT02255175 (PEERS, CTgov)	Phase 4	-	64	Estradiol+Progesterone (Perimenopausal Women, Depressed)	evraaqzlxp(lnazdtesel) = oqsqyisjzp zjgdxpduru (ioaxaixtrz, jqxflxelbb - uugbzfzwuy) View more	-	12 Nov 2019
				Estradiol+Progesterone (Perimenopausal Women, Non-depressed)	evraaqzlxp(lnazdtesel) = xeegruifso zjgdxpduru (ioaxaixtrz, lepgqomkyl - pxjvbtayvh) View more