Delving into the Latest Updates on Ethinylestradiol/Levonorgestrel with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Compound Levonorgestrel, Compound Levonorgestrel Pills, EE/LNG

+ [80]

Target

ER x PR

Action

agonists

Mechanism

ERs agonists(Estrogen receptors agonists), PR agonists(Progesterone receptor agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

DysmenorrheaContraception

Inactive Indication

HemorrhageHepatitis CMetrorrhagia+ [1]

Originator Organization

Pfizer Inc.

Active Organization

Exeltis USA, Inc.Teva Branded Pharmaceutical Products R&D LLC

China Resources Zizhu Pharmaceutical Co., Ltd.

+ [6]

Inactive Organization

Wyeth AB

Wyeth Pharmaceuticals LLC

Bayer AG

+ [3]

License Organization

Exeltis USA, Inc.

Insud Pharma SL

Afaxys, Inc.

+ [1]

Drug Highest PhaseApproved

First Approval Date

United States (10 May 1982),

Contraception

Regulation-

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Structure/Sequence

Molecular FormulaC41H52O4

InChIKeyORKBYCQJWQBPFG-WOMZHKBXSA-N

CAS Registry39366-37-5

The main objectives of this study are to determine the effect of elenestinib on the pharmacokinetic parameters (how the drug is absorbed, distributed, and processed by the body) of midazolam, and to determine the effect of elenestinib on the pharmacokinetic parameters of levonorgestrel/ethinyl estradiol, when given as a combined oral contraceptive.
Healthy adult participants will receive midazolam and levonorgestrel/ethinyl estradiol with and without elenestinib and have blood samples taken.

Start Date03 Feb 2026

Sponsor / Collaborator

Blueprint Medicines Corp.

NCT07272889

/ Not yet recruitingPhase 1

A Phase 1, Open-Label Study to Evaluate the Effect of Multiple Oral Doses of Bemnifosbuvir/Ruzasvir Fixed-dose Combination on the Single-Dose Pharmacokinetics of a Combined Oral Contraceptive (Ethinyl Estradiol/ Levonorgestrel) in Healthy Adult Female Participants of Non-Childbearing Potential

Drug-drug interaction study between Ethinyl Estradioll/Levonorgestrel and Bemnifosbuvir/Ruzasvir

Start Date01 Dec 2025

Sponsor / Collaborator

Atea Pharmaceuticals, Inc.

100 Clinical Results associated with Ethinylestradiol/Levonorgestrel

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100 Translational Medicine associated with Ethinylestradiol/Levonorgestrel

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100 Patents (Medical) associated with Ethinylestradiol/Levonorgestrel

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689

Literatures (Medical) associated with Ethinylestradiol/Levonorgestrel

01 Nov 2025·ATHEROSCLEROSIS

Targeting LDL aggregation decreases atherosclerotic lipid burden in a humanized mouse model of familial hypercholesterolemia: Crucial role of ApoB100 conformational stabilization

Article

Author: Caruana, P ; Tondo, M ; Pepe, A ; Céspedes, M V ; Martínez, A ; Borràs, C ; Escola-Gil, J C ; Prades, R ; Cenarro, A ; Llorente-Cortés, V ; Garcia, E ; Civeira, F ; Benitez-Amaro, A ; Bochicchio, B ; La Chica Lhoëst, M T

BACKGROUND AND AIMS:

Low-density lipoprotein (LDL) aggregation is nowadays considered a therapeutic target in atherosclerosis. DP3, the retro-enantio version of the sequence Gly¹¹²⁷-Cys¹¹⁴⁰ of LRP1, efficiently inhibits LDL aggregation and foam cell in vitro formation. Here, we investigate whether DP3 modulates atherosclerosis in a humanized ApoB100, LDL receptor (LDLR) knockout mice (Ldlr^-/-hApoB100 Tg) and determine the potential LDL-related underlying mechanisms.

METHODS:

Tg mice were fed an HFD for 21 days to induce atherosclerosis and then randomized into three groups that received a daily subcutaneous administration (10 mg/kg) of i) vehicle, ii) DP3 peptide, or iii) a non-active peptide (IP321). The in vivo biodistribution of a fluorescent-labeled peptide version (TAMRA-DP3), and its colocalization with ApoB100 in the arterial intima, was analyzed by imaging system (IVIS) and confocal microscopy. Heart aortic roots were used for atherosclerosis detection and quantification. LDL functionality was analyzed by biochemical, biophysical, molecular, and cellular studies.

RESULTS:

Intimal neutral lipid accumulation in the aortic root was reduced in the DP3-treated group as compared to control groups. ApoB100 in LDLs from the DP3 group exhibited an increased percentage of α-helix secondary structures and decreased immunoreactivity to anti-ApoB100 antibodies. LDL from DP3-treated mice were protected against passive and sphingomyelinase (SMase)-induced aggregation, although they still experienced SMase-induced sphingomyelin phospholysis. In patients with familial hypercholesterolemia (FH), DP3 efficiently inhibited both SMase-induced phospholysis and aggregation.

CONCLUSIONS:

DP3 peptide administration inhibits atherosclerosis by preserving the α-helix secondary structures of ApoB100 in a humanized ApoB100 murine model that mimicks the hallmark of human hypercholesterolemia.

01 May 2025·Acta Biomaterialia

A highly transparent dopamine-copolymerized hydrogel with enhanced ROS-scavenging and tissue-adhesive properties for chronic diabetic wounds

Article

Author: Zhang, Haiqi ; Wang, Jinze ; Ma, Lie ; Hu, Hongtao

Chronic diabetic wounds with complex symptoms represent a major challenge in clinical practice, causing a serious threat to human health and life. Excessive oxidative stress and persistent inflammatory responses are the important reasons for the long-term difficult healing of diabetic wounds. Designing wound dressing materials with intrinsic antioxidant performance, high transparency, adhesiveness, and favorable mechanical properties is of great significance for promoting wound healing, especially in movable parts. Here, a dopamine-copolymerized highly transparent antioxidant hydrogel was developed for the treatment of chronic diabetic wounds. The hydrogel was easily prepared via free radical polymerization using acrylated dopamine monomer (ADA), acrylamide (AM), and phenylboronic acid modified dextran (DP). The dynamic phenylborate ester bonds formed between the catechol of polydopamine and phenylboronic acid effectively mitigated the darkening of the hydrogel color caused by the auto-oxidation of catechol, resulting in the PAM/PDA/DP hydrogel (DP3) with durable transparency. In addition, this hydrogel had good adhesiveness and mechanical properties, as well as desirable reactive oxygen species (ROS)-scavenging performance. Furthermore, in vivo results demonstrated that DP3 hydrogel can stimulate the polarization of macrophages toward anti-inflammatory M2 phenotype, increase the secretion of anti-inflammatory factors, so as to smooth the transition of wound healing from the inflammatory phase to the proliferative phase, and accelerate the repair of diabetic wounds by promoting angiogenesis and collagen deposition. Therefore, the DP3 hydrogel holds great potential for remolding the tissue regeneration microenvironment and serving as a promising dressing for chronic diabetic wounds. STATEMENT OF SIGNIFICANCE: Polydopamine (PDA)-based hydrogels have been widely explored. However, existing PDA-based hydrogels suffer from low content of catechol groups and inferior transparency, and are prone to oxidation darkening during storage. In this study, a dopamine-copolymerized hydrogel with high catechol content was developed. The catechol groups are partially protected by phenylboronic acid-modified dextran, resulting in durable transparency and good adhesiveness of the hydrogel. The hydrogel exhibits desirable antioxidant performance and can effectively promote chronic diabetic wound healing by relieving oxidative stress and regulating immune function. This highly transparent hydrogel with intrinsic antioxidation and self-adhesiveness properties represents a potential and effective strategy for chronic wound management.

01 May 2025·Small

Inhibition of Insulin Amyloid Fibrillogenesis Using Antioxidant Copolymers with Dopamine Pendants

Article

Author: Das, Shubham ; Mondal, Anushree ; Mallick, Tamanna ; De, Priyadarsi

Abstract:

Amyloid aggregation, intricately related to various neurodegenerative and metabolic diseases, presents a significant growing health challenge. Dopamine, a potent antioxidant, plays a pivotal role in modulating protein misfolding by leveraging its potent anti‐amyloidogenic and neuroprotective properties. However, its biological applications are limited by poor aqueous solubility and suboptimal biocompatibility. To address these challenges, water‐soluble copolymers (DP1‐DP3) featuring dopamine and glucose side‐chain pendants are fabricated and investigated for their efficacy in inhibiting amyloid fibril formation from insulin and amyloid beta (Aβ42) peptide. The effects of DP1‐DP3 copolymers on amyloid fibrillation are assessed using several biophysical techniques, which demonstrate excellent radical scavenging properties and the remarkable efficacy of DP3 copolymer in suppressing insulin amyloid fibrillation, achieving ≈97% inhibition. Isothermal titration calorimetry (ITC) and fluorescence binding experiments are carried out to quantify the insulin‐DP3 complex formation. Molecular dynamics simulations validate the ability of DP3 to prevent amyloid fibrillogenesis of both insulin and Aβ42. These studies demonstrate beneficial interactions between DP3 and amyloidogenic protein/peptide, facilitating the stability of the resulting complexes. Overall, the present findings suggest that dopamine‐based antioxidant polymers hold significant potential as advanced therapeutic agents for preventing amyloidogenic disorders.

71

News (Medical) associated with Ethinylestradiol/Levonorgestrel

07 Aug 2025

·www.pharmamanufacturing.com

WuXi XDC boosts sterile drug product capacity with new China facility

WuXi XDC Cayman, a global contract research, development and manufacturing organization focused on bioconjugates, has completed GMP release of its new DP3 facility in Wuxi, China, the company announced . The site is expected to add seven million vials per year to the company's sterile drug product manufacturing capacity. Headquartered in China, WuXi XDC said the DP3 facility was completed in just 18 months, encompassing design, construction, equipment qualification, media fill and GMP readiness. With DP3 now operational, WuXi XDC’s total bioconjugate drug product capacity at the Wuxi site reaches approximately 15 million vials annually across three facilities (DP1, DP2 and DP3). The company said the DP3 facility was built to meet FDA, EMA and NMPA GMP requirements and integrates several advanced manufacturing features. These include automated disinfection, high-speed filling up to 300 vials per minute, non-vacuum stoppering, 100% online weight checks, robotic packaging and traceability functions. According to the company, DP3 offers both liquid and lyophilized sterile drug product manufacturing services. It is equipped to support clinical and commercial production through single-use technology and integrated environmental monitoring. WuXi XDC said it plans to add one new sterile drug product facility each year as part of its ongoing global expansion strategy. One of these projects is a 25,000-square-meter bioconjugates manufacturing site in Singapore, which the company said reached mechanical completion in July . The site is expected to begin operations by the end of 2025 and GMP manufacturing in early 2026.

05 Aug 2025

·www.mobihealthnews.com

Afaxys garners $8M to develop novel contraceptive product

Afaxys, a sexual and reproductive healthcare-focused company, secured $8 million in funding, including a $3 million program-related investment from the David and Lucile Packard Foundation and a $5 million grant from an anonymous foundation. The funding round is the third investment from the Packard Foundation since Afaxys' inception in 2008. WHAT IT DOES Afaxyx is a public benefit corporation (PBC) operating in the reproductive health space that delivers a range of contraceptive options and services. Afaxys Group Services is an outsourcing operation that negotiates pricing via its group purchasing organization. In addition, emapp is a cloud-based emarketplace and purchasing portal that connects healthcare centers to their preferred suppliers. Afaxys Pharma provides a portfolio of branded and generic contraceptives to the public healthcare market, including oral contraceptives, emergency contraceptives, contraceptive patches and adjacent products. The company said it will use the funds to complete the development of a novel contraceptive product that is specially tailored to address the needs of "marginalized communities and women living in contraceptive deserts." MARKET SNAPSHOT In 2024, Afaxys announced it acquired Agile Therapeutics by Insud Pharma, the parent company of Exeltis USA, with whom Afaxys has partnered since 2022. In June, Afaxys announced the renewal of its alliance to support access to Twirla (levonorgestrel and ethinyl estradiol) transdermal system and additional Exeltis products in the public health market. The renewal follows the August 2024 acquisition of Agile Therapeutics by Insud Pharma. In 2024, Afaxys became legally recognized as a PBC. Other companies in the reproductive and contraceptive healthcare space include Wisp , which in 2024 announced a strategic partnership with the food as medicine platform Nourish to allow Wisp patients access to nutrition counseling services via their health insurance or an exclusive self-pay rate. The aim is to make it easier for women looking for a more holistic approach to weight management to access nutrition support. In addition, patients enrolled in Wisp's weight care program can merge medical weight loss treatments with personalized nutrition counseling from Nourish. That same year, femtech company Clue partnered with Headspace to provide Clue Plus Members with a 50% discount on a Headspace subscription. Clue offers reproductive health services from period tracking to pregnancy tracking. Through the partnership, Clue Plus Members have access to Headspace's mental health and mindfulness offerings, enabling them to understand better at which points of their cycle they experience the most stress. The partnership also offered Clue Plus Members targeted support for cycle tracking, pregnancy, fertility and perimenopause/menopause to help individuals navigate the different stages of their cycle.

Acquisition

14 Jan 2025

·pharma.economictimes.indiatimes.com

Lupin launches contraceptive pill Balcoltra generic version in US

Mumbai: After a year of receiving marketing approval from the US drug regulator, generics developer Lupin Limited (Lupin) has launched its generic birth control pill, MinzoyaTM in the United States drug market. MinzoyaTM ( Levonorgestrel and Ethinyl Estradiol Tablets, and Ferrous Bisglycinate Tablets) is a generic equivalent of Balcoltra (Levonorgestrel and Ethinyl Estradiol Tablets, and Ferrous Bisglycinate Tablets) of Avion Pharmaceuticals LLC . The launched generic medication is indicated for use by females of reproductive potential to prevent pregnancy and the ANDA application of the drug was approved by the US FDA in February 2024. In the last twelve month period ending November 2024, the original branded version Balcoltra generated gross sales of $24 million in the US drug market whereas in the previous sequential phase (ending December 2023) the drug had reported an estimated annual sales of $42 million. By Online Bureau ,

Drug Approval

100 Deals associated with Ethinylestradiol/Levonorgestrel

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	G03AB03 G03AA07	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Dysmenorrhea	Japan	Nobelpharma Co., Ltd.	02 Jul 2018
Contraception	United States	Teva Branded Pharmaceutical Products R&D LLC	10 May 1982

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Migraine Without Aura	Phase 2	United States	Teva Branded Pharmaceutical Products R&D LLC	01 Jan 2009
Hemorrhage	Phase 2	United States	Teva Branded Pharmaceutical Products R&D LLC	01 Oct 2006
Metrorrhagia	Phase 2	United States	Teva Branded Pharmaceutical Products R&D LLC	01 Oct 2006
Hepatitis C	Phase 1	Belgium	Pfizer Inc.	01 Jun 2010

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02158572 (Pubmed \| Contraception) Manual	Phase 2	Contraception	2,032	Ethinylestradiol/Levonorgestrel	tsiskmkzyc(fovmoczcjo) = whlxdbdshq hjvcsujenx (qouufnnghm ) View more	Positive	01 Mar 2021
NCT02493712 (CTgov)	Phase 2	Colitis, Ulcerative	51	IBD98-M (High Dose Group)	frkqztfljk = ookoiacigr kidstlsbgu (qdyypjtyjm, tfctdzgsvn - kvrknxjctp) View more	-	14 Aug 2020
				IBD98-M (Low Dose Group)	frkqztfljk = oddegbjsbs kidstlsbgu (qdyypjtyjm, vjwndwpwvq - qtniegtfqb) View more
NCT02531321 (CTgov)	Phase 4	HIV Infections \| Contraception	17	Levonorgestrel and Ethinyl Estradiol (Ritonavir)	uwbhcgcxps(xkjuwxxufr) = qphprmudwo syaiviitqt (icstrddmjx, 61) View more	-	31 May 2019
				Levonorgestrel and Ethinyl Estradiol (Control)	uwbhcgcxps(xkjuwxxufr) = pjfuarixcx syaiviitqt (icstrddmjx, 83) View more
NCT01422135 (CTgov)	Phase 1	-	24	EE+LNG (AG200-15)	xkniiqwawb(ujoguwfmoi) = nppzdoncem yvpelaqlgo (vxslprbumi, 998) View more	-	31 Dec 2018
				EE+LNG (AG200-15 on Lower Abdomen)	plmbxzrcdx(dwuvcgzjbb) = pfsvebaefd mosuqnrwjp (clbuyfebpt, coexlqrahw - scpjzjfnin) View more
NCT01250210 (CTgov)	Phase 2	-	123	levonorgestrel (AG200LE)	uvklurlvie = tzjnwwmrmy qydjlhpnit (cybgjetusn, vyaecnjvdw - xtutfttirz) View more	-	05 Jul 2018
				levonorgestrel and ethinyl estradiol (AG200)	uvklurlvie = xunubbmhgn qydjlhpnit (cybgjetusn, mpkjidwlcj - niupyxdesx) View more
NCT01181479 (CTgov)	Phase 3	Contraception	1,504	AG200-15 (AG200-15 for Cycle 7-13)	drviykufus = ocdbhrlhrv njiajbkeyn (rtpqzonpjs, bbhvtdcmlz - pcgobcbyxf)	-	03 Jul 2018
				Lessina (Lessina)	drviykufus = brxclegxdq njiajbkeyn (rtpqzonpjs, kwbjophyij - lnfatvcqoj) View more
NCT01243580 (AG200-15, CTgov)	Phase 1	-	36	Ortho-Cyclen (Ortho-Cyclen®)	jrmriwtrhg(kbrakgwjog) = nzskvolhba uditzewrqf (pmxnjtpxnh, 50.7) View more	-	19 Dec 2017
				AG200-15 (AG200-15)	jrmriwtrhg(kbrakgwjog) = folyditoyt uditzewrqf (pmxnjtpxnh, 24.0) View more
NCT02158572 (CTgov)	Phase 3	-	2,032	AG200-15	fnjbcyfuio = izujglmcgf rskrovdrfv (bawmymkrvt, xsjslbmzjb - ienxusqodn) View more	-	25 Sep 2017
NCT01236768 (ATI-CL13, CTgov)	Phase 3	Contraception	407	AG200-15 (AG200-15)	yntrwyfthk = kxgbwrovkz cnyxlcfqkx (onvgduuema, cwxpnetbjn - lrnjleaxgh) View more	-	15 Sep 2017
				Levora (Levora)	yntrwyfthk = wcgnecwfyt cnyxlcfqkx (onvgduuema, pqyoaxroau - gxyobfyxnt) View more
NCT01165307 (iTOM, CTgov)	Phase 4	Menorrhagia	77	Naproxen sodium pills+Estradiol 30mcg / Levonorgestrel 150mcg monophasic oral contraceptive pills (Medical Therapy)	rgsulaggzj(vnhktlobos) = xbtwpnnofr vqywedmnrj (rmzzptbmuo, hdvikhtoib - bqmmmeksww) View more	-	15 Nov 2016
				NovaSure® Radiofrequency Endometrial Ablation (Radiofrequency Endometrial Ablation)	rgsulaggzj(vnhktlobos) = jlisunfvxx vqywedmnrj (rmzzptbmuo, wmpenlhbaq - syzqfftvao) View more