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Myfembree relugolix, estradiol hemihydrate, and norethindrone acetate 40 mg; 1 mg; .5 mg Tablet, Film Coated, 7-count

by Sumitomo Pharma America, Inc · 7 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72974-415-99)
NDC 72974-0415-99
🏷️ FDA NDC (as labeled) 72974-415-99 billing pads the product segment with a zero
This package
Contains7-count Pack sizes2 compare ↓
Also priced by: Part D plans $45.35/unit — full pricing hub ↓
Also comes in: 28 tablets 72974-0415-01
Rx only Brand On market Non-controlled
🗂️ Data synced Sep 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

🆔 Identity & classification

FDA NDC (as labeled) 72974-415-99
Product NDC 72974-415
11-digit billing NDC 72974041599
RxCUI 2556799, 2556800
UNII P76B05O5V6, CXY7B3Q98Z, 9S44LIC7OJ
UPC 0372974415013
Application # NDA214846
SPL Set ID fc3feb73-cc84-43a8-aa32-b262460495e8
Established class (EPC) Gonadotropin Releasing Hormone Receptor Antagonist
Mechanism of action Gonadotropin Releasing Hormone Receptor Antagonists; Cytochrome P450 3A Inducers; Cytochrome P450 2B6 Inducers; Breast Cancer Resistance Protein Inhibitors; P-Glycoprotein Inhibitors
Physiologic effect Decreased GnRH Secretion
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2021-05-26
Route ORAL
Dosage form TABLET, FILM COATED
Substance RELUGOLIX; ESTRADIOL HEMIHYDRATE; NORETHINDRONE ACETATE
GPI-14 24993503800320
GPI class Myfembree
GCN Seq No 082317
GCN 49699
HICL code 047392
Ingredient (HICL) Relugolix/Estradiol/Norethindr
HIC1 code P
Therapeutic class — broad (HIC1) Endocrine System
HIC2 code P1
Therapeutic class — intermediate (HIC2) Anteriorpituitary Hormones
HIC3 code P1R
Therapeutic class — specific (HIC3) Lhrh (Gnrh) Antagonist,Estrogen And Progestin Comb
AHFS code 68:16.04.00
AHFS class Estrogens
FDB label name MYFEMBREE 40 MG-1 MG-0.5 MG TB
FDB brand name Myfembree
Legend status F — Federal legend — prescription drug or device
Why two NDCs? The FDA registers this code as 72974-415-99 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 72974-0415-99. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

🏷️ RxNorm drug class

This medicine belongs to the Gonadotropin Releasing Hormone Receptor Antagonist class.

Pharmacologic class Gonadotropin Releasing Hormone Receptor Antagonist
Drug family (ATC) Other hormone antagonists and related agents
How it works Gonadotropin Releasing Hormone Receptor Antagonists, P-Glycoprotein Inhibitors, Cytochrome P450 2B6 Inducers, Breast Cancer Resistance Protein Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

🏭 Manufacturer & labeler

LabelerSumitomo Pharma America, Inc
Application holderSUMITOMO PHARMA AMERICA INC
FDA applicationNDA214846 (NDA)
Labeler code72974
First marketedMay 2021
Product typeHuman Prescription Drug
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

🩺 Clinical

Label name MYFEMBREE 40 MG-1 MG-0.5 MG TB Ingredient Relugolix/Estradiol/Norethindr
📗 Our plain-language guide HelloPharmacist
  • Great question. The main ingredient, relugolix, works by turning down the hormonal signals your pituitary gland sends to your ovaries. This lowers estrogen and progesterone, which...
  • What is Myfembree actually doing in my body, and why does it have three ingredients?
  • You take one tablet once a day by mouth, ideally at the same time each day. You can take it with or without food — a high-fat meal may slightly reduce relugolix absorption, but not...
  • How do I take it, and does it matter if I take it with food?
📖 Read our full Relugolix, Estradiol, and Norethindrone guide →

Supplement & herbal interactions

🌿 Drug–supplement interaction checker →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

💊 What it looks like

Color Yellow
ShapeRound
ImprintMVT;415
Size8 mm
ScoringNot scored
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

🧪 Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII EX438O2MRT
    Ferric oxide yellow is a naturally occurring iron compound used as a colorant in medications. It gives tablets, capsules, and other forms a yellow or golden hue for identification and appearance.
  • UNII 9XZ8H6N6OH
    A plant-based cellulose derivative used as a binder to hold tablet ingredients together, a thickener in liquids, and a coating agent to control how fast the medicine dissolves.
  • UNII 0WZ8WG20P6
    Hypromellose 2910 is a plant-based cellulose derivative that acts as a thickener, binder, and film-coating agent. It helps control how quickly the medicine dissolves and protects the tablet or capsule from moisture and light.
  • UNII EWQ57Q8I5X
    Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
  • UNII 70097M6I30
    Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
  • UNII 3OWL53L36A
    A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
  • UNII H8AV0SQX4D
    A modified starch derived from potato or corn starch. It absorbs water quickly and helps tablets or capsules break apart and dissolve in the stomach, acting as a disintegrant to ensure the medicine releases its active ingredients properly.
  • UNII 15FIX9V2JP
    Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
  • UNII XHX3C3X673
    Triacetin is a clear, oily liquid made from glycerin and acetic acid. It works as a plasticizer and solvent in medicines, helping soften coatings and improve how liquids mix together in formulations.

9 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

💲 Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $45.35 $317.48 / 7 tablets
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Myfembree 40 mg/1; 1 mg/1; .5 mgthis 72974-0415-99 Sumitomo 7 tablets — — FDA listed —
About this product: this is the brand-name version. We did not find an FDA-approved generic match for this exact strength, form and route.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

⏳ Availability & generic status

🏛️
2021
First FDA approval
May 2021
📍
2026
Currently FDA-listed
5 years listed
🛡️
2042
Latest patent/protection listed
not a guaranteed launch date
🔒No FDA-approved generic found

We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.

🛡️ Latest patent/protection date listed: FDA patent/protection data lists protections through Nov 2042. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved May 26, 2021 RLD RS ⏳ ~16.1 yr to latest listed protection

Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.

Patents & exclusivity — FDA Orange Book
US 11793812 — method of use (U-2360)
US 11033551 — method of use (U-3129)
US 11957684 — method of use (U-3129)
US 12325714 — drug substance
US 11795178 — drug substance
US 7300935 — drug substance
US 12551447 — drug product
US 8058280 — drug substance
Exclusivity M-289
2021 2023 2025 2027 2029 2031 2033 2035 2037 2039 2041 2043
Today
LOE
Substance patent Formulation patent Method-of-use patent Exclusivity Pediatric +6mo
🏛️FDA exclusivity
FDA-granted marketing protection. It’s separate from patents and may be shorter than patent protection.
🧪Product / substance patents
Patents covering the active ingredient, product, formulation, or related drug features.
🎯Method-of-use patents
Patents covering specific approved uses. These can sometimes be carved out with a “skinny label,” but not always.
🛈 What do these terms mean?
Patent
Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
Substance patent
Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
Formulation (product) patent
Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
Method-of-use patent
A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
Skinny label
A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
Exclusivity
FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
Paragraph IV
A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
RLD / RS
Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
TE / AB rating
FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
LOE (loss of exclusivity)
The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.

Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.

Listed patents (8)
PatentTypeUse codeExpires
US 11793812 ↗ Method of use U-2360 May 3, 2038
US 11033551 ↗ Method of use U-3129 Sep 29, 2037
US 11957684 ↗ Method of use U-3129 Sep 29, 2037
US 12325714 ↗ Drug substance — Sep 27, 2033
US 11795178 ↗ Drug substance — Sep 27, 2033
US 7300935 ↗ Drug substance — Jan 28, 2029
US 12551447 ↗ Drug product — Nov 5, 2042
US 8058280 ↗ Drug substance — Jan 28, 2026
FDA exclusivity
CodeWhat it grantsExpires
M-289New indication / labeling change (3-year)Jan 27, 2026
Common questions
Is there a generic version of MYFEMBREE 40 MG-1 MG-0.5 MG TB?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for MYFEMBREE 40 MG-1 MG-0.5 MG TB. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Nov 2042 — an estimate, not a guaranteed launch date.
The FDA approved a generic — why can’t I get it at my pharmacy yet?
FDA approval and pharmacy availability are two different things. The FDA can approve a generic years before it actually reaches pharmacies, because the brand company may still hold patents or have a settlement that delays the launch. A manufacturer also has to choose to make and sell it, and have supply ready. So a drug can be “FDA-approved generic exists” and still be brand-only at the counter today.
Why do different websites show different generic release dates?
Generic availability is not based on one single date. Some sources use the first exclusivity expiration, some use the last product patent, and others use the latest method-of-use patent. Patent challenges, settlements, licenses, and label carve-outs can also change the real-world launch date. This page shows the underlying Orange Book dates so you can see why estimates may differ.
What does “FDA listed” mean?
It means the product appears in the FDA’s official NDC directory. That’s a good sign a product exists and is intended for the U.S. market, but on its own it does not confirm a pharmacy can fill it today. Where we have recent retail pricing data (NADAC) for a product, we label it “Availability likely” instead.
What does a patent or protection date mean here?
It’s the latest date currently listed in the FDA Orange Book for a patent or exclusivity on the brand product. It can affect when a full generic version becomes widely available — but it is not a guaranteed generic launch date. Generics sometimes arrive earlier (through a settlement or patent challenge) or later (a manufacturer still has to make and sell one).
What does “current Orange Book estimate” mean?
It means we are using the latest patent and exclusivity dates currently listed in the FDA Orange Book. It is not a guaranteed launch date.
Can a generic come out before the last patent expires?
Sometimes. A generic company may challenge a patent, settle with the brand manufacturer, receive a license, or obtain approval with a narrower label that avoids a patented use. In other cases, the last listed protection may delay full-label generic competition.
Can a generic come out after the listed dates?
Yes. Even after patents or exclusivity expire, a generic still needs FDA approval and a manufacturer must choose to market it. Supply, litigation, business decisions, or regulatory issues can delay actual availability.
What is the difference between patents and exclusivity?
Patents are legal protections usually issued by the U.S. Patent and Trademark Office. FDA exclusivity is marketing protection granted by the FDA. They are separate, and either one can affect generic timing.
Why are there multiple patent dates?
One drug can have several patents covering different things: the active ingredient, a formulation, a manufacturing process, or a specific approved use. That is why a page may show several expiration dates instead of one simple generic date.
Built from FDA Orange Book patent and exclusivity data. Dates are refreshed from public FDA data when available; the marker is max(latest patent expiry, latest exclusivity expiry). Paragraph-IV settlements and first-filer 180-day exclusivity can shift the real date; a method-of-use patent may allow an earlier skinny-label generic for non-protected indications. Generic launch timing is an estimate, not a guarantee.
Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

💊 Medicaid utilization by pack size

Medicaid (SDUD) totals over the four most recent reported quarters for every package size of this drug — handy when a specific package (e.g. a starter/titration pack) carries little or no Medicaid volume on its own.
28 tablets72974-0415-01 18,905 Rx · $28,324,030
7 tablets this page72974-0415-99 No Medicaid data
Drug total (last 4 qtrs): 18,905 Rx · 652,900 units · $28,324,030 gross reimbursed
Tap a pack size to open its page. Source: CMS State Drug Utilization Data, last 4 quarters.

📊 Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Myfembree — the program that covers self-administered drugs. 1 manufacturer.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Myfembree. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$593.3K
Claims incl. refills
358
Beneficiaries
188
Spend / beneficiary
$3,155.89
Spend / claim
$1,657.28
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Myfembree (this brand).

Top reported reactions

Therapy Interrupted470
Heavy Menstrual Bleeding233
Intermenstrual Bleeding118
Headache73
Alopecia68
Hot Flush68
Menstruation Irregular62

Age at onset

Adult48

Reporter sex

1,495 reports
Female · 100%
Unknown · 0%

Serious outcomes

Hospitalization35
Life-threatening4
Disabling2
Death1
Reports over time (by year) — tap or hover for the count & year
2021 2022 2024 2026 542 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Per unit Per pack Marketing startStatus
72974-0415-01 28 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72974-415-01) $45.25 / ea $1,267.04 2021-05-26 Active
72974-0415-99 You're viewing this 7 TABLET, FILM COATED in 1 BOTTLE, PLASTIC (72974-415-99) — — 2021-07-07 Active

You're viewing the smallest of 2 pack sizes for this product.

This pack shows little to no recent Medicaid volume — the 28 tablets pack carries most fills. See all packs ↓

Pack size FAQ

What quantity is in NDC 72974-0415-99?
NDC 72974-0415-99 is a 7-count package — 7 tablet, film coated in 1 bottle, plastic.
What is the difference between NDC 72974-0415-99 and NDC 72974-0415-01?
Both are Myfembree relugolix, estradiol hemihydrate, and norethindrone acetate 40 mg; 1 mg; .5 mg Tablet, Film Coated — the drug itself is identical. NDC 72974-0415-99 is the 7-count package, while NDC 72974-0415-01 is the 28 tablets package.
What NDC number is used to bill for this package of Myfembree relugolix, estradiol hemihydrate, and norethindrone acetate 40 mg; 1 mg; .5 mg Tablet, Film Coated?
Bill NDC 72974-0415-99 — the 11-digit billing format is 72974041599. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.

🧭 About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The FDA registers it as 72974-415-99, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 72974-0415-99, written without dashes as 72974041599. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 72974-0415-99, the first segment (72974) is the labeler code FDA assigned to Sumitomo Pharma America, Inc; the middle segment (0415) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (99) identifies this exact package size and type. Together they name one specific package of one specific product.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Sumitomo Pharma America, Inc. Listing status can change — the directory data on this page refreshes weekly.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 28 tablets (72974-0415-01). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
Sumitomo Pharma America, Inc is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🚨 Boxed Warning 🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📦 Storage and Handling 📋 Description 💬 Information for Patients
🚨 Boxed Warning 173 words ▾

WARNING: THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS Estrogen and progestin combinations, including MYFEMBREE, increase the risk of thrombotic or thromboembolic disorders including pulmonary embolism (PE), deep vein thrombosis (DVT), stroke and myocardial infarction (MI), especially in women at increased risk for these events [see Warnings and Precautions ( 5.1 )]. MYFEMBREE is contraindicated in women with current or a history of thrombotic or thromboembolic disorders and in women at increased risk for these events, including women over 35 years of age who smoke or women with uncontrolled hypertension [see Contraindications ( 4 )].

WARNING: THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS See full prescribing information for complete boxed warning Estrogen and progestin combinations, including MYFEMBREE, increase the risk of thrombotic or thromboembolic disorders, especially in women at increased risk for these events. ( 5.1 ) MYFEMBREE is contraindicated in women with current or a history of thrombotic or thromboembolic disorders and in women at increased risk for these events, including women over 35 years of age who smoke or women with uncontrolled hypertension.

( 4 )

🎯 Indications and Usage 197 words ▾

1 INDICATIONS AND USAGE MYFEMBREE is a combination of relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, estradiol, an estrogen, and norethindrone acetate, a progestin, indicated in premenopausal women for the: management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids). ( 1.1 , 14.1 ) management of moderate to severe pain associated with endometriosis. ( 1.2 , 14.2 ) Limitations of Use Use of MYFEMBREE should be limited to 24 months due to the risk of continued bone loss which may not be reversible.

( 1.3 , 5.2 , 6 )

1.1Heavy Menstrual Bleeding Associated with Uterine Leiomyomas MYFEMBREE is indicated for the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women [ see Clinical Studies ( 14 ) ].

1.2Moderate to Severe Pain Associated with Endometriosis MYFEMBREE is indicated for the management of moderate to severe pain associated with endometriosis in premenopausal women [ see Clinical Studies ( 14 ) ].

1.3Limitations of Use Use of MYFEMBREE should be limited to 24 months due to the risk of continued bone loss that may not be reversible [see Warnings and Precautions ( 5.2 ) and Adverse Reactions ( 6 )].

⏱️ Dosage and Administration ~1 min read ▾

2 DOSAGE AND ADMINISTRATION Exclude pregnancy and discontinue hormonal contraceptives prior to MYFEMBREE initiation. ( 2.1 ) Take one tablet orally once daily. ( 2.2 ) Take the missed dose of MYFEMBREE as soon as possible the same day and then resume regular dosing the next day at the usual time. ( 2.3 ) If concomitant use of oral P-gp inhibitors is unavoidable, take MYFEMBREE at least 6 hours before taking the P-gp inhibitor ( 2.4 )

2.1Prior to Initiation of MYFEMBREE Exclude pregnancy [see Contraindications ( 4 )] . Discontinue hormonal contraceptives [see Warnings and Precautions ( 5.8 )] .

2.2Recommended Dosage Take one tablet of MYFEMBREE orally once daily at approximately the same time, with or without food [see Clinical Pharmacology ( 12.3 )]. Start MYFEMBREE as early as possible after the onset of menses but no later than seven days after menses has started [ see Clinical Studies ( 14 ) ]. The recommended total duration of treatment with MYFEMBREE is 24 months [see Indications and Usage ( 1.3 ), Warnings and Precautions ( 5.2 ), and Adverse Reactions ( 6 )] .

2.3Missed Dose Take the missed dose of MYFEMBREE as soon as possible the same day and then resume regular dosing the next day at the usual time.

2.4Dosage Modification for Concomitant Use with P-gp Inhibitors Avoid concomitant use of MYFEMBREE with oral P-gp inhibitors. If concomitant use is unavoidable, take MYFEMBREE first and separate dosing by at least 6 hours [see Drug Interactions ( 7.1 ) and Clinical Pharmacology ( 12.3 )] .

💊 Dosage Forms and Strengths 68 words ▾

3 DOSAGE FORMS AND STRENGTHS Tablets: Each tablet of MYFEMBREE contains a fixed-dose combination of relugolix 40 mg, estradiol (E2) 1 mg, and norethindrone acetate (NETA) 0.5 mg. The tablets are light yellow to yellow, round, film-coated, and debossed with “MVT” on one side and “415” on the other side. Tablets: fixed-dose combination containing relugolix 40 mg, estradiol 1 mg and norethindrone acetate 0.5 mg. ( 3 )

⛔ Contraindications ~1 min read ▾

4 CONTRAINDICATIONS MYFEMBREE is contraindicated in women: With a high risk of arterial, venous thrombotic, or thromboembolic disorders [see Boxed Warning and Warnings and Precautions ( 5.1 )] . Examples include women over 35 years of age who smoke and women who are known to have: current or history of deep vein thrombosis or pulmonary embolism vascular disease (e.g., cerebrovascular disease, coronary artery disease, peripheral vascular disease) thrombogenic valvular or thrombogenic rhythm diseases of the heart (e.g., subacute bacterial endocarditis with valvular disease, or atrial fibrillation) inherited or acquired hypercoagulopathies uncontrolled hypertension headaches with focal neurological symptoms or migraine headaches with aura if over 35 years of age Who are pregnant.

Exposure to MYFEMBREE early in pregnancy may increase the risk of early pregnancy loss [see Warnings and Precautions ( 5.9 ) and Use in Specific Populations ( 8.1 )] . With known osteoporosis, because of the risk of further bone loss [see Warnings and Precautions ( 5.2 )]. With current or history of breast cancer or other hormone-sensitive malignancies, and with increased risk for hormone-sensitive malignancies [see Warnings and Precautions ( 5.3 )] .

With known hepatic impairment or disease [see Warnings and Precautions ( 5.5 )] . With undiagnosed abnormal uterine bleeding. With known anaphylactic reaction, angioedema, or hypersensitivity to MYFEMBREE or any of its components.

Anaphylactoid reactions, urticaria, and angioedema have been reported [see Warnings and Precautions ( 5.14 ), Adverse Reactions ( 6.2 )]. High risk of arterial, venous thrombotic, or thromboembolic disorder. ( 4 ) Pregnancy.

( 4 ) Known osteoporosis. ( 4 ) Current or history of breast cancer or other hormone-sensitive malignancies. ( 4 ) Known hepatic impairment or disease.

( 4 ) Undiagnosed abnormal uterine bleeding. ( 4 ) Known hypersensitivity to components of MYFEMBREE. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Thromboembolic Disorders and Vascular Events : Discontinue MYFEMBREE if an arterial or venous thrombotic, cardiovascular, or cerebrovascular event occurs. Discontinue MYFEMBREE if there is sudden unexplained partial or complete loss of vision, proptosis, diplopia, papilledema, or retinal vascular lesions and evaluate for retinal vein thrombosis immediately. ( 5.1 ) Bone Loss : Decreases in bone mineral density (BMD) may not be completely reversible.

Baseline BMD assessment is recommended in all women. In women with heavy menstrual bleeding associated with uterine fibroids, periodic BMD assessments are recommended. In women with moderate to severe pain associated with endometriosis, annual BMD assessments are recommended.

Assess risk-benefit for women with additional risk factors for bone loss. ( 5.2 ) Suicidal Ideation and Mood Disorders (Including Depression) : Advise patients to seek medical attention for new onset or worsening depression, anxiety, or other mood changes. ( 5.4 ) Hepatic Impairment and Transaminase Elevations : Counsel patients on signs and symptoms of liver injury.

( 5.5 ) Elevated Blood Pressure : Do not use in women with uncontrolled hypertension. For women with well-controlled hypertension, continue to monitor blood pressure and stop MYFEMBREE if blood pressure rises significantly. ( 5.7 ) Change in Menstrual Bleeding Pattern and Reduced Ability to Recognize Pregnancy : Advise women to use non-hormonal contraception during treatment and for one week after discontinuing MYFEMBREE.

MYFEMBREE may delay the ability to recognize pregnancy because it alters menstrual bleeding. Perform testing if pregnancy is suspected and discontinue MYFEMBREE if pregnancy is confirmed. ( 5.8 ) Risk of Early Pregnancy Loss : Can cause early pregnancy loss.

Advise women to use effective non-hormonal contraception. ( 5.9 ) Uterine Fibroid Prolapse or Expulsion : Advise patients to seek medical attention for severe uterine bleeding. ( 5.10 ) Hypersensitivity Reactions : Immediately discontinue MYFEMBREE if a hypersensitivity reaction occurs.

( 5.14 )

5.1Thromboembolic Disorders and Vascular Events MYFEMBREE is contraindicated in women with current or history of thrombotic or thromboembolic disorders and in women at increased risk for these events [see Contraindications ( 4 )] . Discontinue MYFEMBREE immediately if an arterial or venous thrombotic, cardiovascular, or cerebrovascular event occurs or is suspected. Discontinue MYFEMBREE at least 4 to 6 weeks before surgery of the type associated with an increased risk of thromboembolism, or during periods of prolonged immobilization, if feasible.

Discontinue MYFEMBREE immediately if there is sudden unexplained partial or complete loss of vision, proptosis, diplopia, papilledema, or retinal vascular lesions and evaluate for retinal vein thrombosis as these have been reported in patients receiving estrogens and progestins. Estrogen and progestin combinations, including the estradiol/norethindrone acetate component of MYFEMBREE, increase the risk of thrombotic or thromboembolic disorders, including pulmonary embolism, deep vein thrombosis, stroke, and myocardial infarction, especially in women at high risk for these events.

In general, the risk is greatest among women over 35 years of age who smoke and women with uncontrolled hypertension, dyslipidemia, vascular disease, or obesity. Two thromboembolic events (DVT and PE) occurred in one woman treated for 38 days with MYFEMBREE for moderate to severe pain associated with endometriosis.

5.2Bone Loss MYFEMBREE is contraindicated in women with known osteoporosis [see Contraindications ( 4 )]. Consider the benefits and risks of MYFEMBREE treatment in patients with a history of a low trauma fracture or risk factors for osteoporosis or bone loss, including taking medications that may decrease bone mineral density (BMD) (e.g., systemic or chronic inhaled corticosteroids, anticonvulsants, or chronic use of proton pump…

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed elsewhere in the labeling: Thromboembolic Disorders and Vascular Events [see Warnings and Precautions ( 5.1 )] Bone Loss [see Warnings and Precautions ( 5.2 )] Suicidal Ideation and Mood Disorders (Including Depression) [see Warnings and Precautions ( 5.4 )] Hepatic Impairment and Transaminase Elevations [see Warnings and Precautions ( 5.5 )] Elevated Blood Pressure [see Warnings and Precautions ( 5.7 )] Change in Menstrual Bleeding Pattern and Reduced Ability to Recognize Pregnancy [see Warnings and Precautions ( 5.8 )] Uterine Fibroid Prolapse or Expulsion [see Warnings and Precautions ( 5.10 )] Alopecia [see Warnings and Precautions ( 5.11 )] Effects on Carbohydrate and Lipid Metabolism [see Warnings and Precautions ( 5.12 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.14 )] In women with heavy menstrual bleeding associated with uterine fibroids, most common adverse reactions (incidence ≥ 3%) are vasomotor symptoms, uterine bleeding, alopecia, and decreased libido.

In women with moderate to severe pain associated with endometriosis, most common adverse reactions (incidence ≥ 3%) are headache, vasomotor symptoms, mood disorders, abnormal uterine bleeding, nausea, toothache, back pain, decreased sexual desire and arousal, arthralgia, fatigue, and dizziness. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sumitomo Pharma America, Inc. at 1-833-696-8268 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Heavy Menstrual Bleeding Associated with Uterine Leiomyomas The safety of MYFEMBREE was evaluated in two placebo-controlled clinical trials, Study L1 (LIBERTY 1) and Study L2 (LIBERTY 2), in women with heavy menstrual bleeding associated with uterine fibroids.

In these trials, women received a once daily relugolix 40-mg tablet and an over-encapsulated tablet of E2 1 mg and NETA 0.5 mg (relugolix + E2/NETA), which is equivalent to 1 tablet of MYFEMBREE. Across the two trials, 254 women received MYFEMBREE once daily for 24 weeks. Additionally, 256 women received placebo for 24 weeks, and 258 women received relugolix 40-mg monotherapy once daily for 12 weeks followed by MYFEMBREE for 12 weeks [see Clinical Studies ( 14.1 )] .

Of these, 476 women were treated with MYFEMBREE in a 28-week extension trial, Study L3 (LIBERTY Extension), for a total treatment duration of up to 12 months. Demographics were similar across the studies; approximately 43% were White, 51% were Black, and approximately 23% were of Hispanic or Latino ethnicity. The mean age at study entry was approximately 42 years (range 19 to 51 years).

Of women who completed Study L3, 229 were rerandomized to continue MYFEMBREE or withdraw from therapy (placebo) for an additional 52 weeks (Study L4). Serious Adverse Reactions In Studies L1 and L2, serious adverse reactions were reported in 3.1% of MYFEMBREE-treated women as compared to 2.3% of placebo-treated women. In MYFEMBREE-treated women, serious adverse drug reactions included uterine myoma expulsion and menorrhagia experienced by one woman and uterine leiomyoma (prolapse), cholecystitis, and pelvic pain reported for one woman each.

Adverse Reactions Leading to Study Drug Discontinuation In Studies L1 and L2, 3.9% of women treated with MYFEMBREE discontinued therapy due to adverse reactions, as compared to 4.3% receiving placebo. The most common adverse reaction leading to discontinuation of MYFEMBREE was uterine bleeding (1.2%) with an onset usually reported within the first 3 months of therapy. Common Adverse Reactions The most common adverse reactions reported in at least 3% of women treated with MYFEMBREE fo…

🔄 Drug Interactions 168 words ▾

7 DRUG INTERACTIONS Avoid use of MYFEMBREE with oral P-gp inhibitors. ( 7.1 ) Avoid use with combined P-gp and strong CYP3A inducers, as the exposure of the components of MYFEMBREE may be decreased. ( 7.1 )

7.1Effect of Other Drugs on MYFEMBREE P-gp Inhibitors Co-administration of MYFEMBREE with P-gp inhibitors increases the AUC and maximum concentration (C max ) of relugolix [see Clinical Pharmacology ( 12.3 )] and may increase the risk of adverse reactions associated with MYFEMBREE. Avoid use of MYFEMBREE with oral P-gp inhibitors. If use is unavoidable, take MYFEMBREE first, separate dosing by at least 6 hours, and monitor patients for adverse reactions [see Dosage and Administration ( 2.4 )] .

Combined P-gp and Strong CYP3A Inducers Use of MYFEMBREE with combined P-gp and strong CYP3A inducers decreases the AUC and C max of relugolix, estradiol, and/or norethindrone [see Clinical Pharmacology ( 12.3 )] and may decrease the therapeutic effects of MYFEMBREE. Avoid use of MYFEMBREE with combined P-gp and strong CYP3A inducers.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to MYFEMBREE during pregnancy. Pregnant females exposed to MYFEMBREE and healthcare providers are encouraged to call the MYFEMBREE Pregnancy Exposure Registry at 1-855-428-0707. Risk Summary MYFEMBREE is contraindicated in pregnancy [see Contraindications ( 4 ) and Warnings and Precautions ( 5.9 )].

Based on findings from animal studies and its mechanism of action, MYFEMBREE may cause early pregnancy loss. Discontinue MYFEMBREE if pregnancy occurs during treatment [see Warnings and Precautions ( 5.9 ) and Clinical Pharmacology ( 12.1 )] . The limited human data with the use of MYFEMBREE in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes [see Data ].

In animal reproduction studies, oral administration of relugolix in pregnant rabbits during organogenesis resulted in spontaneous abortion and total litter loss at relugolix exposures about half those at the maximum recommended human dose (MRHD) of 40 mg. In both rabbits and rats, no fetal malformations were present at any dose level tested which were associated with relugolix exposures about half and approximately 300 times exposures in women at the MRHD, respectively [see Data ]. Epidemiologic studies and meta-analyses have not found an increased risk of genital or non-genital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to estrogens and progestins before conception or during early pregnancy.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. There are insufficient data to conclude whether the presence of uterine fibroids or endometriosis reduces the likelihood of achieving pregnancy or increases the risk of adverse pregnancy outcomes. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

In the United States general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies are 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study, oral administration of relugolix to pregnant rabbits during the period of organogenesis (Days 6 to 18 of gestation) resulted in abortion, total litter loss, or decreased number of live fetuses at a dose of 9 mg/kg/day (about half the human exposure at the maximum recommended human dose [MRHD] of 40 mg daily, based on AUC).

No treatment related malformations were observed in surviving fetuses. No treatment related effects were observed at 3 mg/kg/day (about 0.1-fold the MRHD) or lower. The binding affinity of relugolix for rabbit GnRH receptors is unknown.

In a similar embryo-fetal development study, oral administration of relugolix to pregnant rats during the period of organogenesis (Days 6 to 17 of gestation) did not affect pregnancy status or fetal endpoints at doses up to 1000 mg/kg/day (300 times the MRHD), a dose at which maternal toxicity (decreased body weight gain and food consumption) was observed. A no observed adverse effect level (NOAEL) for maternal toxicity was 200 mg/kg/day (86 times the MRHD). In rats, the binding affinity of relugolix for GnRH receptors is more than 1000-fold lower than that in humans, and this study represents an assessment of non-pharmacological targets of relugolix during pregnancy.

No treatment related malformations were observed up to 1000 mg/kg/day. In a pre- and postnatal developmental study in pregnant and lactating rats, oral administration of relugolix to rats during late pregnancy and lactation (Day 6 of gestation to Day 20 of lactation) had no effects on pre- and postnatal development at doses up to 1000 mg/kg/day (300 times the MRHD), a dose in which maternal toxicity was observed (effects on body weight gain). A NOAE…

🤰 Pregnancy ~3 min read ▾

8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to MYFEMBREE during pregnancy. Pregnant females exposed to MYFEMBREE and healthcare providers are encouraged to call the MYFEMBREE Pregnancy Exposure Registry at 1-855-428-0707. Risk Summary MYFEMBREE is contraindicated in pregnancy [see Contraindications ( 4 ) and Warnings and Precautions ( 5.9 )].

Based on findings from animal studies and its mechanism of action, MYFEMBREE may cause early pregnancy loss. Discontinue MYFEMBREE if pregnancy occurs during treatment [see Warnings and Precautions ( 5.9 ) and Clinical Pharmacology ( 12.1 )] . The limited human data with the use of MYFEMBREE in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes [see Data ].

In animal reproduction studies, oral administration of relugolix in pregnant rabbits during organogenesis resulted in spontaneous abortion and total litter loss at relugolix exposures about half those at the maximum recommended human dose (MRHD) of 40 mg. In both rabbits and rats, no fetal malformations were present at any dose level tested which were associated with relugolix exposures about half and approximately 300 times exposures in women at the MRHD, respectively [see Data ]. Epidemiologic studies and meta-analyses have not found an increased risk of genital or non-genital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to estrogens and progestins before conception or during early pregnancy.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. There are insufficient data to conclude whether the presence of uterine fibroids or endometriosis reduces the likelihood of achieving pregnancy or increases the risk of adverse pregnancy outcomes. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes.

In the United States general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies are 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study, oral administration of relugolix to pregnant rabbits during the period of organogenesis (Days 6 to 18 of gestation) resulted in abortion, total litter loss, or decreased number of live fetuses at a dose of 9 mg/kg/day (about half the human exposure at the maximum recommended human dose [MRHD] of 40 mg daily, based on AUC).

No treatment related malformations were observed in surviving fetuses. No treatment related effects were observed at 3 mg/kg/day (about 0.1-fold the MRHD) or lower. The binding affinity of relugolix for rabbit GnRH receptors is unknown.

In a similar embryo-fetal development study, oral administration of relugolix to pregnant rats during the period of organogenesis (Days 6 to 17 of gestation) did not affect pregnancy status or fetal endpoints at doses up to 1000 mg/kg/day (300 times the MRHD), a dose at which maternal toxicity (decreased body weight gain and food consumption) was observed. A no observed adverse effect level (NOAEL) for maternal toxicity was 200 mg/kg/day (86 times the MRHD). In rats, the binding affinity of relugolix for GnRH receptors is more than 1000-fold lower than that in humans, and this study represents an assessment of non-pharmacological targets of relugolix during pregnancy.

No treatment related malformations were observed up to 1000 mg/kg/day. In a pre- and postnatal developmental study in pregnant and lactating rats, oral administration of relugolix to rats during late pregnancy and lactation (Day 6 of gestation to Day 20 of lactation) had no effects on pre- and postnatal development at doses up to 1000 mg/kg/day (300 times the MRHD), a dose in which maternal toxicity was observed (effects on body weight gain). A NOAEL for maternal toxicity was 10…

🧒 Pediatric Use 15 words ▾

8.4Pediatric Use Safety and effectiveness of MYFEMBREE in pediatric patients have not been established.

🆘 Overdosage 40 words ▾

10 OVERDOSAGE Overdosage of estrogen plus progestin may cause nausea, vomiting, breast tenderness, abdominal pain, drowsiness, fatigue, and withdrawal bleeding. Supportive care is recommended if an overdose occurs. The amount of relugolix, estradiol, or norethindrone removed by hemodialysis is unknown.

🧬 Clinical Pharmacology ~2 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action MYFEMBREE is a combination of relugolix, estradiol (E2), and norethindrone acetate (NETA). Relugolix is a non-peptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased serum concentrations of the ovarian sex hormones estradiol and progesterone and reduced bleeding associated with uterine fibroids and pain associated with endometriosis. Estradiol acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues.

As a component of MYFEMBREE, the addition of exogenous estradiol may reduce the increase in bone resorption and resultant bone loss that can occur due to a decrease in circulating estrogen concentrations from relugolix alone. Progestins such as norethindrone act by binding to nuclear receptors that are expressed in progesterone-responsive tissues. As a component of MYFEMBREE, norethindrone may protect the uterus from the potential adverse endometrial effects of unopposed estrogen.

12.2Pharmacodynamics Estradiol and norethindrone acetate (components of MYFEMBREE) may have the following effects: Increased thyroxin-binding globulin levels leading to [see Warnings and Precautions ( 5.13 )]: Increased circulating total thyroid hormone concentrations as measured by protein-bound iodine (PBI), thyroxine (T4) levels (by column or by radioimmunoassay), or triiodothyronine (T3) concentrations by radioimmunoassay Decreased T3 resin uptake Unaltered free T4 and free T3 concentrations in women with normal thyroid function [see Warnings and Precautions ( 5.13 )].

Elevated corticosteroid-binding globulin (CBG) and sex hormone-binding globulin (SHBG) concentrations leading to increases in total circulating corticosteroid and sex hormone concentrations, respectively [see Warnings and Precautions ( 5.13 )] . Possible decreased free testosterone concentrations. Possible increased other plasma proteins concentrations (angiotensinogen/renin substrate, alpha-1 antitrypsin, ceruloplasmin).

Increased plasma high-density lipoprotein (HDL) and HDL2 cholesterol subfraction concentration, reduced low-density lipoprotein concentration, increased triglyceride concentrations. Accelerated prothrombin time, partial thromboplastin time, and platelet aggregation time; increased platelet count; increased factors II, VII antigen, VIII coagulant activity, IX, X, XII, VII-X complex, and beta-thromboglobulin; decreased concentrations of anti-factor Xa and antithrombin III, decreased antithrombin III activity, increased concentrations of fibrinogen and fibrinogen activity; increased plasminogen antigen and activity.

Cardiac Electrophysiology At a dose 9 times the maximum approved recommended dose of relugolix, the QT interval was not prolonged to a clinically relevant extent. The effect of estradiol and norethindrone acetate (two of the components of MYFEMBREE) on the QTc interval has not been studied.

12.3Pharmacokinetics The pharmacokinetic parameters of relugolix, unconjugated estradiol, and norethindrone after administration of a single dose of MYFEMBREE to healthy postmenopausal women under fasted conditions are summarized in Table 7 . Table 7: Pharmacokinetic Parameters of Relugolix, Unconjugated Estradiol, and Norethindrone After Single Dose Administration of MYFEMBREE Abbreviations: AUC = area under the concentration-time curve; AUC 0-inf = AUC from time 0 extrapolated to infinity; C max = maximum observed concentration; E2 = estradiol; NET = norethindrone; T max = time to maximum observed concentration.

Notes: AUC 0-inf is presented in ng·hr/mL for relugolix, NET and in pg·hr/mL for unconjugated E2. C max is presented in ng/mL for relugolix, NET and in pg/mL for unconjugated E2. Relugolix Unconjugated Estradiol Norethindrone AUC 0-inf (ng·hr/mL or pg·hr/mL), mean (SD) 198.1 (111.6) 818.7 (334.4) 17.5 (8.5) C max (ng/mL or pg/mL), mean…

🧬 Mechanism of Action 150 words ▾

12.1Mechanism of Action MYFEMBREE is a combination of relugolix, estradiol (E2), and norethindrone acetate (NETA). Relugolix is a non-peptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased serum concentrations of the ovarian sex hormones estradiol and progesterone and reduced bleeding associated with uterine fibroids and pain associated with endometriosis. Estradiol acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues.

As a component of MYFEMBREE, the addition of exogenous estradiol may reduce the increase in bone resorption and resultant bone loss that can occur due to a decrease in circulating estrogen concentrations from relugolix alone. Progestins such as norethindrone act by binding to nuclear receptors that are expressed in progesterone-responsive tissues. As a component of MYFEMBREE, norethindrone may protect the uterus from the potential adverse endometrial effects of unopposed estrogen.

📦 How Supplied / Storage and Handling 176 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING

16.1How Supplied MYFEMBREE film-coated tablets contain relugolix 40 mg, estradiol (E2) 1 mg, and norethindrone acetate (NETA) 0.5 mg. The tablets are light yellow to yellow, round film-coated tablet with “MVT” on one side and “415” on the other side. MYFEMBREE is supplied in a white, opaque, high-density polyethylene bottle containing 28 tablets with desiccant and closed with an induction-sealed child-resistant cap (NDC Code 72974-415-01).

16.2Storage and Handling Store at 15ºC to 30ºC (59ºF to 86ºF). Dispose unused medication via a take-back option if available. Otherwise, follow FDA instructions for disposing medication in the household trash, www.fda.gov/drugdisposal. Do NOT flush down the toilet.

16.1How Supplied MYFEMBREE film-coated tablets contain relugolix 40 mg, estradiol (E2) 1 mg, and norethindrone acetate (NETA) 0.5 mg. The tablets are light yellow to yellow, round film-coated tablet with “MVT” on one side and “415” on the other side. MYFEMBREE is supplied in a white, opaque, high-density polyethylene bottle containing 28 tablets with desiccant and closed with an induction-sealed child-resistant cap (NDC Code 72974-415-01).

📦 Storage and Handling 39 words ▾

16.2Storage and Handling Store at 15ºC to 30ºC (59ºF to 86ºF). Dispose unused medication via a take-back option if available. Otherwise, follow FDA instructions for disposing medication in the household trash, www.fda.gov/drugdisposal. Do NOT flush down the toilet.

📋 Description ~1 min read ▾

11 DESCRIPTION MYFEMBREE tablets for oral administration contain a fixed-dose combination of relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg as active ingredients. Relugolix is a non-peptide small molecule, GnRH receptor antagonist. It is a white to off white to slightly yellow solid and is sparingly soluble in water.

The chemical name is N-(4-{1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl}phenyl)-N-methoxyurea with the empirical formula of C 29 H 27 F 2 N 7 O 5 S and a molecular weight of 623.63. The structural formula is: Estradiol (E2), an estrogen, is present as the hemihydrate (C 18 H 24 O 2 •½H 2 O) which is a white or almost white crystalline powder. Its chemical name is estra-1, 3, 5 ( 10 )-triene-3, 17β-diol with the empirical formula of C 18 H 24 O 2 and a molecular weight of 272.4.

The structural formula is: Norethindrone acetate (NETA), a progestin, is a white or yellowish-white crystalline powder. Its chemical name is 17-Hydroxy-19-nor-17α-pregn-4-en-20-yn-3-one acetate with the empirical formula of C 22 H 28 O 3 and a molecular weight of 340.5. The structural formula is: Each MYFEMBREE (relugolix, estradiol, and norethindrone acetate) film-coated tablet contains the following inactive ingredients: hydroxypropyl cellulose, hypromellose, iron oxide yellow, lactose monohydrate, mannitol, magnesium stearate, sodium starch glycolate, titanium dioxide, and triacetin.

Relugolix Structural Formula Estradiol Structural Formula Norethindrone Acetate Structural Formula

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling ( Patient Information ). Thromboembolic Disorders and Vascular Events Advise patients that use of estrogen and progestin combinations may increase the risk of venous and arterial thrombotic/thromboembolic events, especially in women at high risk for these events [see Boxed Warning , Contraindications ( 4 ) and Warnings and Precautions ( 5.1 )] . Bone Loss Advise patients about the risk of bone loss.

Advise patients that supplementary calcium and vitamin D may be beneficial if dietary intake of calcium and vitamin D is not adequate. Advise women that oral iron supplementation should not be taken at the same time as calcium and vitamin D [see Warnings and Precautions ( 5.2 ) and Adverse Reactions ( 6.1 )]. Suicidal Ideation and Mood Disorders (Including Depression) Advise patients that depression, mood disorders, and suicidal ideation may occur with MYFEMBREE use.

Instruct women with new onset or worsening depression, anxiety, or other mood changes to promptly seek medical attention [see Warnings and Precautions ( 5.4 ) and Adverse Reactions ( 6.1 )]. Hepatic Impairment and Transaminase Elevations Advise women to promptly seek medical attention in case of signs or symptoms that may reflect liver injury, such as jaundice [see Warnings and Precautions ( 5.5 )] . Change in Menstrual Bleeding Pattern and Reduced Ability to Recognize Pregnancy Advise patients that MYFEMBREE may delay the recognition of pregnancy because it may reduce the duration and amount of menstrual bleeding.

Advise patients to use effective non-hormonal contraception while taking MYFEMBREE and to discontinue MYFEMBREE if pregnancy is diagnosed [see Warnings and Precautions ( 5.8 )] . Advise pregnant patients that there is a pregnancy registry that monitors pregnancy outcomes in women exposed to MYFEMBREE during pregnancy [see Use in Specific Populations ( 8.1 , 8.3 )]. Alopecia Advise women with uterine fibroids that alopecia, hair loss, and hair thinning in no specific pattern may occur with MYFEMBREE.

Advise these women that hair loss and hair thinning may not resolve completely after stopping MYFEMBREE. Advise these women to contact their healthcare provider if they have concerns about changes to their hair [see Warnings and Precautions ( 5.11 ) and Adverse Reactions ( 6.1 )] . Females of Reproductive Potential Advise women to use effective non-hormonal contraception while taking MYFEMBREE and for one week after discontinuing treatment and to discontinue MYFEMBREE if pregnancy is confirmed.

Advise pregnant patients that there is a pregnancy registry that monitors pregnancy outcomes in women exposed to MYFEMBREE during pregnancy [see Use in Specific Populations ( 8.1 , 8.3 )]. Drug Interactions Advise women to report their use of any other prescription or nonprescription medications or dietary supplements. Co-administration with certain drugs may decrease the therapeutic effects of MYFEMBREE [see Drug Interactions ( 7.1 )].

Administration Instructions Advise women to begin taking MYFEMBREE as soon as possible after the start of menses but no later than 7 days after menses has started [see Dosage and Administration ( 2.2 )]. Advise women to take any missed dose of MYFEMBREE as soon as possible the same day and then resume regular dosing the next day at the usual time [see Dosage and Administration ( 2.3 )]. Advise women taking oral P-gp inhibitors to take MYFEMBREE first and separate dosing by at least 6 hours [see Dosage and Administration ( 2.4 )].

Manufactured by Patheon Inc., 2100 Syntex Court, Mississauga, Ontario L5N 7K9, Canada Distributed by: Sumitomo Pharma America, Inc., 84 Waterford Drive, Marlborough, MA 01752 214846 MS 007

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
← 72974-0120-01 · Sumitomo 72975-0277-00 · FITGLOW →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.