Estradiol; norethindrone acetate; relugolix - Generic Drug Details

What are the generic sources for estradiol; norethindrone acetate; relugolix and what is the scope of freedom to operate?

Estradiol; norethindrone acetate; relugolix is the generic ingredient in one branded drug marketed by Sumitomo Pharma Am and is included in one NDA. There are seven patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Estradiol; norethindrone acetate; relugolix has one hundred and fifty-six patent family members in thirty-six countries.

One supplier is listed for this compound.

Summary for estradiol; norethindrone acetate; relugolix

International Patents:	156
US Patents:	7
Tradenames:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Clinical Trials:	12
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for estradiol; norethindrone acetate; relugolix
DailyMed Link:	estradiol; norethindrone acetate; relugolix at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for estradiol; norethindrone acetate; relugolix

Dosage:

TABLET;ORAL

^*The generic entry opportunity date is the latter of the last compound-claiming patent and the last regulatory exclusivity protection. Many factors can influence early or later generic entry. This date is provided as a rough estimate of generic entry potential and should not be used as an independent source.

Recent Clinical Trials for estradiol; norethindrone acetate; relugolix

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
Myovant Sciences GmbH	Phase 4
University of Chicago	Phase 4
Myovant Sciences GmbH	Phase 1

See all estradiol; norethindrone acetate; relugolix clinical trials

Pharmacology for estradiol; norethindrone acetate; relugolix

Drug Class	Estrogen Gonadotropin Releasing Hormone Receptor Antagonist Progestin
Mechanism of Action	Breast Cancer Resistance Protein Inhibitors Cytochrome P450 2B6 Inducers Cytochrome P450 3A Inducers Estrogen Receptor Agonists Gonadotropin Releasing Hormone Receptor Antagonists P-Glycoprotein Inhibitors
Physiological Effect	Decreased GnRH Secretion

Anatomical Therapeutic Chemical (ATC) Classes for estradiol; norethindrone acetate; relugolix

G03CA	Natural and semisynthetic estrogens, plain
G03C	ESTROGENS
G03	SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
G	Genito-urinary system and sex hormones

L02BX	Other hormone antagonists and related agents
L02B	HORMONE ANTAGONISTS AND RELATED AGENTS
L02	ENDOCRINE THERAPY
L	Antineoplastic and immunomodulating agents

Paragraph IV (Patent) Challenges for ESTRADIOL; NORETHINDRONE ACETATE; RELUGOLIX

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
MYFEMBREE	Tablets	estradiol; norethindrone acetate; relugolix	1 mg/0.5 mg/40 mg	214846	1	2024-12-18

US Patents and Regulatory Information for estradiol; norethindrone acetate; relugolix

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes			Y	Y
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes

Expired US Patents for estradiol; norethindrone acetate; relugolix

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Sumitomo Pharma Am	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021

International Patents for estradiol; norethindrone acetate; relugolix

Country	Patent Number	Title	Estimated Expiration
Israel	300071
Israel	265700
Spain	2913753
Hungary	E044048
Taiwan	201418262	Production method of thienopyrimidine derivative

Supplementary Protection Certificates for estradiol; norethindrone acetate; relugolix

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1453521	C 2015 029	Romania		PRODUCT NAME: LEVONORGESTREL SI ETINILESTRADIOL; NATIONAL AUTHORISATION NUMBER: RO 7793/2015/001; DATE OF NATIONAL AUTHORISATION: 20150612; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): SK. 17/0017/15-S; DATE OF FIRST AUTHORISATION IN EEA: 20150129
1591446	PA2021529	Lithuania		PRODUCT NAME: RELUGOLIKSAS ARBA JO DRUSKA ; REGISTRATION NO/DATE: EU/1/21/1565 20210716
1591446	C 2021 047	Romania		PRODUCT NAME: RELUGOLIX SAU O SARE A ACESTUIA; NATIONAL AUTHORISATION NUMBER: EU/1/21/1565; DATE OF NATIONAL AUTHORISATION: 20210716; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/21/1565; DATE OF FIRST AUTHORISATION IN EEA: 20210716
1453521	15C0050	France		PRODUCT NAME: ETHINYLESTRADIOL ET MELANGE DE LEVONORGESTREL ET ETHINYLESTRADIOL; NAT. REGISTRATION NO/DATE: NL 42237 20150320; FIRST REGISTRATION: SK - 17/0017/15-S 20150129
1591446	21C1056	France		PRODUCT NAME: RELUGOLIX OU UN SEL DE CELUI-CI; REGISTRATION NO/DATE: EU/1/21/1565 20210720

Market Dynamics and Financial Trajectory for the Pharmaceutical Drug: Estradiol, Norethindrone Acetate, and Relugolix

Last updated: July 28, 2025

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Introduction

The pharmaceutical landscape for hormonal therapies, including estradiol, norethindrone acetate, and relugolix, has experienced significant shifts driven by evolving clinical needs, regulatory changes, and market dynamics. Understanding the current trends and predicted financial trajectories for these compounds provides crucial insights for stakeholders ranging from investors to healthcare providers. This analysis dissects the factors influencing market growth, competitive positioning, and future revenue potential for these drugs.

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Market Overview and Key Drivers

1. Estradiol and Norethindrone Acetate: Established Hormonal Therapies

Estradiol, a biologically active estrogen, and norethindrone acetate, a progestin, form the backbone of hormone replacement therapy (HRT). These agents have a well-established market, primarily addressing menopausal symptoms, osteoporosis prevention, and hormone deficiency conditions.

• Market Size and Growth: In 2022, the global HRT market was valued at approximately USD 14 billion, projected to grow at a CAGR of 4-5% through 2030 (Market Research Future). This steady expansion underscores ongoing demand driven by aging populations, especially in North America and Europe.

• Regulatory Landscape: Recent regulatory restrictions around bioidentical hormones and the scrutiny of compounded hormone therapies have reaffirmed the importance of approved formulations like estradiol and norethindrone acetate, bolstering their market stability.

• Patent and Formulation Opportunities: While many formulations are off-patent, novel delivery systems (transdermal patches, bioavailability-enhanced tablets) are under development, creating opportunities for branded versions and incremental revenue.

2. Relugolix: A Novel Oral Gonadotropin-Releasing Hormone (GnRH) Antagonist

Relugolix, marketed as Orgovyx (for prostate cancer) and relugolix in women’s health indications, is a recently approved GnRH antagonist offering oral administration—an advantage over injectable counterparts.

• Market Entry and Growth Potential: Since its approval by the FDA in 2020 for prostate cancer and in 2022 for uterine fibroids, relugolix has gained traction due to its convenience, safety profile, and reduced cardiovascular risks compared to GnRH agonists.

• Pipeline and Indications: The drug is undergoing trials for endometriosis, breast cancer, and other hormone-driven conditions, promising diversified revenue streams.

• Market Size and Forecast: The global GnRH antagonist market is projected to reach USD 3.5 billion by 2028, growing at a CAGR of over 7% (Grand View Research). Relugolix is positioned to capture significant share within this niche, especially with expanding indications.

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Market Challenges and Competitive Dynamics

1. Patent Expirations and Generic Competition

Many formulations of estradiol and norethindrone acetate are facing patent expirations, leading to commoditization and pricing pressure. Generic manufacturers have eroded branded market share, emphasizing the importance of innovation and new delivery methods to maintain profitability.

2. Regulatory and Safety Concerns

Claims linking estrogen therapy to cancer risks (e.g., breast cancer) have constrained market growth. Conversely, newer formulations with improved safety profiles, like transdermal patches, mitigate these concerns, offering a competitive edge.

3. Competitive Landscape for Relugolix

Relugolix faces competition from injectable GnRH agonists (e.g., leuprolide, goserelin) and other oral antagonists like relugolix's main competitor, linzagolix. Navigating regulatory approvals, pricing, and physician acceptance remain critical success factors.

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Financial Trajectory and Revenue Projections

1. Estradiol and Norethindrone Acetate

While mature, these drugs’ revenues are expected to stabilize or decline mildly due to patent expiries, unless companies innovate with new formulations or expand indications.

• Revenue Estimates: The global HRT market maintains a steady overall value (~USD 14 billion), with branded formulations generating between USD 0.5 to 1 billion annually for leading companies such as AbbVie, Pfizer, and Teva.

• Growth Strategies: Companies investing in transdermal systems, combination therapies, and biosimilar development aim to sustain revenue streams, especially in emerging markets where hormone therapies are gaining acceptance.

2. Relugolix

Relugolix’s novel mechanism and oral route afford higher growth potential. Sales forecasts, according to EvaluatePharma, project revenues surpassing USD 1.2 billion by 2027.

• Market Penetration: The drug’s uptake in prostate cancer management is strong, with additional market expansion in females with adenomyosis, endometriosis, and fibroids projected to contribute significantly.

• Pricing and Market Share: Premium pricing strategies are likely given its innovative status, with potential for value-based agreements emphasizing its safety benefits and convenience.

• Pipeline Impact: Upcoming indications such as uterine fibroids and endometriosis could add US$ 500 million+ annually per indication within five years.

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Regulatory and Market Access Considerations

The successful commercialization of relugolix hinges on obtenir reimbursement, physician adoption, and adherence to evolving clinical guidelines. Regulatory agencies’ ongoing scrutiny regarding hormone-related malignancies and cardiovascular risks will influence product positioning and market acceptance.

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Future Trends and Strategic Implications

• Personalized Medicine: Advances in pharmacogenomics may tailor hormone therapies, affecting market segmentation and pricing strategies.
• Digital Health Integration: Digital monitoring and adherence programs can enhance patient outcomes and differentiate products in competitive markets.
• Emerging Markets: Rising awareness and increasing healthcare investments in Asia-Pacific and Latin America present expansion opportunities for established and new entrants.

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Key Takeaways

• The market for estradiol and norethindrone acetate remains sizable but faces saturation and patent expiration risks, necessitating innovation in formulations and indications.
• Relugolix offers a promising growth trajectory, driven by its oral administration, expanding indications, and favorable safety profile.
• Competitive pressures, including generics and emerging therapies, push companies towards developing novel delivery systems, biosimilars, and combination therapies to sustain revenue streams.
• Regulatory landscape and market access strategies will critically influence financial outcomes, especially for newer agents like relugolix.
• Emerging markets and personalized medicine trends will shape future growth, creating opportunities for differentiated products and targeted therapies.

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FAQs

1. What factors influence the market growth of estradiol and norethindrone acetate?
Market growth is driven by aging populations, increasing prevalence of menopause-related conditions, and innovations in drug delivery systems. Regulatory stability and expanding indications further support demand.

2. How does relugolix compare to existing GnRH therapies?
Relugolix’s oral formulation and favorable safety profile give it advantages over injectable GnRH agonists, facilitating patient adherence and expanding its market potential.

3. What are the main challenges facing these drugs' market expansion?
Patent expiries, generic competition, safety concerns, and regulatory scrutiny pose significant challenges. Successful innovation and market positioning are essential to navigate these hurdles.

4. What emerging indications could boost relugolix’s revenue?
Uterine fibroids, endometriosis, and certain cancers represent significant opportunities, potentially adding billions in annual sales if clinical trials demonstrate efficacy.

5. How might personalized medicine impact the future of hormonal therapies?
Genomic insights could tailor treatments to individual patient profiles, improving efficacy and safety, thus influencing pricing strategies and market segmentation.

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References

1. Market Research Future. "Hormone Replacement Therapy Market," 2022.
2. Grand View Research. "GnRH Antagonists Market Size & Growth Analysis," 2022.
3. EvaluatePharma. "Global Oncology and Hormone Therapy Market Forecast," 2022.
4. FDA Approvals and Regulatory Data, 2022.
5. Company Reports and Press Releases on Relugolix, 2022–2023.