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 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 thirty-four patent family members in thirty-four countries.

One supplier is listed for this compound.

Summary for ESTRADIOL; NORETHINDRONE ACETATE; RELUGOLIX

International Patents:	134
US Patents:	7
Tradenames:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Clinical Trials:	12
DailyMed Link:	ESTRADIOL; NORETHINDRONE ACETATE; RELUGOLIX at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for ESTRADIOL; NORETHINDRONE ACETATE; RELUGOLIX

Constraining patent/regulatory exclusivity:

INFORMATION ADDED TO THE LABELING TO DESCRIBE THE RESULTS OF MVT-601-035

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
University of Chicago	Phase 4
Myovant Sciences GmbH	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

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	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes
Sumitomo Pharma	MYFEMBREE	estradiol; norethindrone acetate; relugolix	TABLET;ORAL	214846-001	May 26, 2021		RX	Yes	Yes			Y	Y
Sumitomo Pharma	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	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
Hungary	S2100052
Japan	6250564
Canada	3038865	METHODES DE TRAITEMENT DE L'INFERTILITE FEMININE (METHODS OF TREATING FEMALE INFERTILITY)

Supplementary Protection Certificates for ESTRADIOL; NORETHINDRONE ACETATE; RELUGOLIX

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1591446	PA2021529	Lithuania		PRODUCT NAME: RELUGOLIKSAS ARBA JO DRUSKA ; REGISTRATION NO/DATE: EU/1/21/1565 20210716
1591446	CA 2021 00048	Denmark		PRODUCT NAME: RELUGOLIX OR A SALT THEREOF; REG. NO/DATE: EU/1/21/1565 20210720
1453521	122015000093	Germany		PRODUCT NAME: LEVONORGESTREL UND ETHINYLESTRADIOL; NAT. REGISTRATION NO/DATE: 87675.00.00 20150720; FIRST REGISTRATION: SLOWAKEI 17/0017/15-S 20150129

ESTRADIOL; NORETHINDRONE ACETATE; RELUGOLIX Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Myfembree (Relugolix, Estradiol, Norethindrone Acetate)

Introduction

Myfembree, a combination drug containing relugolix, estradiol, and norethindrone acetate, has recently gained significant attention in the pharmaceutical market for its efficacy in managing heavy menstrual bleeding associated with uterine fibroids and moderate to severe pain associated with endometriosis in premenopausal women. Here, we delve into the market dynamics and financial trajectory of this drug.

Regulatory Approvals and Market Availability

Myfembree has received regulatory approvals in several key markets. In the United States, it was approved by the FDA in May 2021 for the management of heavy menstrual bleeding associated with uterine fibroids and in August 2022 for the management of moderate to severe pain associated with endometriosis[2][4].

In Canada, Myfembree was approved by Health Canada and became available by prescription in January 2024 for both indications[4].

Therapeutic Indications

Myfembree is indicated for two primary therapeutic areas:

• Heavy Menstrual Bleeding (HMB) Associated with Uterine Fibroids: Clinical trials, such as the LIBERTY-1 and LIBERTY-2 studies, have shown that Myfembree significantly reduces menstrual blood loss and improves other symptoms associated with uterine fibroids[2][3][5].
• Moderate to Severe Pain Associated with Endometriosis: Myfembree has also been approved for managing pain associated with endometriosis, with clinical trials demonstrating its efficacy in reducing pain and improving quality of life for patients[2][4].

Mechanism of Action

Relugolix, the active GnRH receptor antagonist in Myfembree, works by reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby decreasing estrogen and progesterone production. This reduction in hormone levels helps in managing symptoms of uterine fibroids and endometriosis. The addition of estradiol and norethindrone acetate mitigates the adverse effects of relugolix, such as bone loss and vasomotor symptoms[1][2][3].

Clinical Evidence and Efficacy

The efficacy of Myfembree has been established through several clinical trials. The LIBERTY-1 and LIBERTY-2 trials showed that Myfembree significantly reduced menstrual blood loss and improved other symptoms in women with uterine fibroids. The SPIRIT-1 and SPIRIT-2 trials demonstrated its effectiveness in managing pain associated with endometriosis[2][3][5].

Safety Profile

While Myfembree has a generally favorable safety profile, it is associated with some adverse effects. Common adverse reactions include headache, vasomotor symptoms, mood disorders, and abnormal uterine bleeding. There is also a risk of bone mineral density loss, although the addition of estradiol and norethindrone acetate helps mitigate this risk. Serious adverse events such as suicidal ideation and mood disorders have been reported, necessitating careful patient monitoring[2][3].

Market Demand and Competition

The market demand for treatments targeting uterine fibroids and endometriosis is significant due to the prevalence of these conditions among premenopausal women. Myfembree enters a market where current treatments often involve surgical interventions or less effective medical therapies. Its convenience as a once-daily oral tablet and its comprehensive symptom management make it an attractive option for patients and healthcare providers alike[3][4].

Financial Trajectory

The financial trajectory of Myfembree is expected to be positive given its unique positioning and efficacy. Here are some key financial considerations:

Revenue Projections

With approvals in major markets and a strong clinical evidence base, Myfembree is poised to generate substantial revenue. The drug's ability to address two significant therapeutic areas will likely drive high adoption rates among healthcare providers and patients.

Market Share

Myfembree is expected to capture a significant market share in the treatment of uterine fibroids and endometriosis due to its efficacy and convenience. It will compete with existing treatments, including other GnRH agonists and antagonists, but its unique combination and oral administration are likely to differentiate it in the market.

Pricing Strategy

The pricing strategy for Myfembree will be critical in determining its financial success. Given its innovative nature and the lack of effective oral treatments for these conditions, the drug is likely to be priced competitively with other GnRH therapies but may command a premium due to its convenience and comprehensive symptom management.

Partnership and Distribution

The partnership between Sumitomo Pharma and Pfizer Canada for the distribution of Myfembree in Canada highlights the strategic collaborations that can enhance the drug's market reach and financial performance. Similar partnerships in other regions can further bolster its financial trajectory[4].

Key Takeaways

• Regulatory Approvals: Myfembree has received approvals in the U.S. and Canada for managing heavy menstrual bleeding associated with uterine fibroids and moderate to severe pain associated with endometriosis.
• Therapeutic Efficacy: Clinical trials have demonstrated the drug's efficacy in reducing menstrual blood loss and managing pain associated with endometriosis.
• Safety Profile: While generally well-tolerated, Myfembree is associated with some adverse effects, including bone mineral density loss and mood disorders.
• Market Demand: High demand is anticipated due to the prevalence of uterine fibroids and endometriosis and the lack of effective oral treatments.
• Financial Projections: Strong revenue projections are expected due to its unique positioning, efficacy, and convenience.

FAQs

Q: What are the primary indications for Myfembree?

Myfembree is indicated for the management of heavy menstrual bleeding associated with uterine fibroids and moderate to severe pain associated with endometriosis in premenopausal women.

Q: How does Myfembree work?

Myfembree works by using relugolix to reduce LH and FSH secretion, thereby decreasing estrogen and progesterone production. Estradiol and norethindrone acetate are added to mitigate adverse effects such as bone loss and vasomotor symptoms.

Q: What are the common adverse reactions associated with Myfembree?

Common adverse reactions include headache, vasomotor symptoms, mood disorders, and abnormal uterine bleeding.

Q: Is Myfembree available in Canada?

Yes, Myfembree was approved by Health Canada and became available by prescription in January 2024.

Q: What is the recommended treatment duration for Myfembree?

The treatment duration should be limited to 24 months due to the risk of bone loss that may not be reversible.

Sources

1. Health Canada: Summary Basis of Decision (SBD) for Myfembree.
2. VA Formulary Advisor: Relugolix, Estradiol, Norethindrone (MYFEMBREE) National Drug Monograph.
3. PubMed: Relugolix/Estradiol/Norethisterone (Norethindrone) Acetate.
4. Sumitomo Pharma and Pfizer Canada: Availability of MYFEMBREE in Canada.
5. FDA: 214846Orig1s000 - MYFEMBREE NDA.