Lupron Depot leuprolide acetate Kit
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Gonadotropin Releasing Hormone Receptor Agonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Leuprolide injection is used to treat certain types of prostate cancer central precocious puberty (CPP; a condition causing children to enter puberty too soon, resulting in faster than normal bone growth and development of sexual characteristics) endometriosis (a condition in which the type of tissue that lines the uterus [womb] grows in other areas of the body and causes infertility, pain before and during menstrual periods, pain during and after sexual activity, and heavy, irregular bleeding) anemia (a lower-than-normal number of red blood cells) caused by uterine fibroids (growths i...
Read the full MedlinePlus article ↗- That's a really common concern, and it's smart to ask. When you first start leuprolide, your testosterone levels actually spike for a week or two before the drug kicks in and bring...
- Why does my doctor say my symptoms might get worse right after starting leuprolide?
- Hot flashes are actually one of the most common side effects in men taking leuprolide — over half of men in clinical studies experienced them. Because leuprolide drops testosterone...
- Will I get hot flashes? I thought that was just a women's issue.
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Supplement & herbal interactions
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🧪 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.
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IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
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💲 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 system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $5,430.930 | — |
| Medicaid paysCMS SDUD · 12 mo | $4,606.12 | — |
| Medicare drug plans payPart D · Q2 2026 | $5,560.07 | — |
| Medicare Part B allowsASP · J1950 | $1,841.261 / J1950 unit | — |
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🧾 Billing & reimbursement
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Leuprolide Acetate 00781-4003-32 | Sandoz | 1 kit | $197.606 | AP | Availability likely | save 96% |
| Leuprolide Acetate 55150-0478-01 | Eugia | 1 kit | $197.606 | AP | Availability likely | save 96% |
| leuprolide acetate 47335-0936-40 | Sun | 1 kit | $197.606 | AP | Availability likely | save 96% |
| Leuprolide Acetate 70710-1769-03 | Zydus | 1 kit | $197.606 | AP | Availability likely | save 96% |
| Leuprolide Acetate 72664-0611-28 | VGYAAN | 1 kit | $261.318 | AP | FDA listed | save 95% |
| Lupron Depot 00074-3641-03 | AbbVie | 1 kit | $1,821.130 | — | Availability likely | save 66% |
| Lupron Depot 00074-3642-03 | AbbVie | 1 kit | $2,174.170 | — | Availability likely | save 60% |
| Lupron Depotthis 00074-3663-03 | AbbVie | 1 kit | $5,430.930 | — | Availability likely | — |
| Lupron Depot 00074-3346-03 | AbbVie | 1 kit | $6,516.300 | — | Availability likely | +20% |
| Fensolvi 62935-0153-50 | TOLMAR | 1 kit | — | — | FDA listed | — |
| Lupron Depot 00074-3473-03 | AbbVie | 1 kit | — | — | FDA listed | — |
| Lupron Depot-PED 00074-9694-03 | AbbVie | 1 kit | — | — | FDA listed | — |
| Lupron Depot-PED 00074-2108-03 | AbbVie | 1 kit | — | — | FDA listed | — |
| Lupron Depot-PED 00074-2440-03 | AbbVie | 1 kit | — | — | FDA listed | — |
| Lupron Depot 00074-3683-03 | AbbVie | 1 kit | — | — | FDA listed | — |
| Leuprolide Acetate Depot 69097-0909-50 | CIPLA | 1 kit | — | — | FDA listed | — |
| Lutrate Depot 83831-0134-01 | Avyxa | 1 kit | — | — | FDA listed | — |
| Lupron Depot-PED 00074-3575-01 | AbbVie | 1 kit | — | — | FDA listed | — |
| Leuprolide Acetate 70771-1687-03 | Zydus | 1 kit | — | AP | FDA listed | — |
| Lupron Depot-PED 00074-2282-03 | AbbVie | 1 kit | — | — | FDA listed | — |
| Lupron Depot-PED 00074-3779-03 | AbbVie | 1 kit | — | — | FDA listed | — |
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⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
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🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 00074-3663-03 You're viewing this | 1 KIT in 1 CARTON (0074-3663-03) * 1.5 mL in 1 SYRINGE * 1 mL in 1 PACKET | 2010-11-08 | Active |
🧭 About this NDC listing & data coverage
Kit / multi-component package
This NDC identifies a kit — a package containing more than one component. Structured data (pricing, ingredients, equivalents) is often reported per component rather than for the kit NDC itself, which can make this page look thinner than the components' own pages.
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 | ✓ Available |
| Inactive ingredients (structured) | — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available. |
| NADAC pharmacy acquisition price (CMS) | ✓ Available |
| Orange Book / therapeutic-equivalence data | — Not published for this NDC Applies only to products approved under an NDA/ANDA; many listings are out of scope. |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
Is the NDC printed on the package the same as the 11-digit billing NDC?
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE LUPRON DEPOT 11.25 mg is a gonadotropin-releasing hormone (GnRH) agonist indicated for: Endometriosis Management of endometriosis, including pain relief and reduction of endometriotic lesions. ( 1.1 ) In combination with a norethindrone acetate for initial management of the painful symptoms of endometriosis and for management of recurrence of symptoms. ( 1.1 ) Limitations of Use: The total duration of therapy with LUPRON DEPOT 11.25 mg plus add-back therapy should not exceed 12 months due to concerns about adverse impact on bone mineral density.
( 1.1 , 2.1 , 5.1 ) Uterine Leiomyomata (Fibroids) Concomitant use with iron therapy for preoperative hematologic improvement of women with anemia caused by fibroids for whom three months of hormonal suppression is deemed necessary. ( 1.2 ) Limitations of Use: LUPRON DEPOT 11.25 mg is not indicated for combination use with norethindrone acetate add-back therapy for the preoperative hematologic improvement of women with anemia caused by heavy menstrual bleeding due to fibroids. ( 1.2 )
1.1Endometriosis Monotherapy LUPRON DEPOT 11.25 mg is indicated for management of endometriosis, including pain relief and reduction of endometriotic lesions. In Combination with Norethindrone Acetate LUPRON DEPOT 11.25 mg in combination with norethindrone acetate is indicated for initial management of the painful symptoms of endometriosis and for management of recurrence of symptoms. Use of norethindrone acetate in combination with LUPRON DEPOT 11.25 mg is referred to as add-back therapy, and is intended to reduce the loss of bone mineral density (BMD) and reduce vasomotor symptoms associated with use of LUPRON DEPOT 11.25 mg.
Limitations of Use : The total duration of therapy with LUPRON DEPOT 11.25 mg plus add-back therapy should not exceed 12 months due to concerns about adverse impact on bone mineral density [see Dosage and Administration ( 2.1 ) and Warnings and Precautions ( 5.1 ) ] .
1.2Uterine Leiomyomata (Fibroids) LUPRON DEPOT 11.25 mg, used concomitantly with iron therapy, is indicated for the preoperative hematologic improvement of women with anemia caused by fibroids for whom three months of hormonal suppression is deemed necessary. Consider a one-month trial period on iron alone, as some women will respond to iron alone [see Clinical Studies ( 14.2 )]. LUPRON DEPOT 11.25 mg may be added if the response to iron alone is considered inadequate.
Limitations of Use : LUPRON DEPOT 11.25 mg is not indicated for combination use with norethindrone acetate add-back therapy for the preoperative hematologic improvement of women with anemia caused by heavy menstrual bleeding due to fibroids [see Dosage and Administration ( 2.1 )].
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION LUPRON DEPOT 11.25mg for 3-month administration, given by a healthcare provider as a single intramuscular injection. LUPRON DEPOT 11.25 mg has different release characteristics than LUPRON 3.75 mg and is dosed differently. ( 2.1 ) Do not substitute LUPRON DEPOT 11.25 mg for LUPRON DEPOT 3.75 mg.
Do not administer LUPRON DEPOT 11.25 mg more frequently than every 3 months. Do not give a fractional dose of the LUPRON DEPOT 11.25 mg, as it is not equivalent to the same dose of the LUPRON DEPOT 3.75 mg monthly formulation. Reconstitute LUPRON DEPOT 11.25 mg prior to use.
( 2.2 ) Endometriosis: LUPRON DEPOT 11.25 mg administered as a single intramuscular (IM) injection once every three months for up to two injections (6 months of therapy). LUPRON DEPOT may be administered alone or in combination with daily 5 mg tablet of norethindrone acetate (add-back). ( 2.1 ) If endometriosis symptoms recur after initial course of therapy, retreatment for no more than six months may be considered but only with the addition of norethindrone acetate add-back therapy.
Do not re-treat with LUPRON DEPOT 11.25 mg alone. ( 2.1 ) Fibroids: Recommended dose of LUPRON DEPOT 11.25 mg is one IM injection. ( 2.1 ) Figure A img-128 plunger img-129 blue line img-0184 shake Injection site Figure F Figure G
2.1Important Use Information LUPRON DEPOT 11.25 mg must be administered by a healthcare professional. LUPRON DEPOT 11.25 mg for 3-month administration has different release characteristics than LUPRON 3.75 mg for 1-month administration and is dosed differently. Do not substitute LUPRON DEPOT 11.25 mg for LUPRON DEPOT 3.75 mg.
Do not administer LUPRON DEPOT 11.25 mg more frequently than every 3 months. Do not give a fractional dose of the LUPRON DEPOT 11.25 mg, as it is not equivalent to the same dose of the LUPRON DEPOT 3.75 mg monthly formulation. Endometriosis The initial and retreatment dosage regimens for LUPRON DEPOT 11.25 mg for the management of women with endometriosis are outlined in Table 1 .
Table 1. LUPRON DEPOT 11.25 mg, Management of Endometriosis Treatment Phase LUPRON DEPOT 11.25 mg Dosing Maximum Treatment Duration Initial Treatment 1 11.25 mg IM every 3 months for 1 to 2 doses 6 months Retreatment 2 11.25 mg IM every 3 months for 1 to 2 doses 6 months 12 MONTHS 3 TOTAL TREATMENT DURATION 1 May use LUPRON DEPOT 11.25 mg with or without norethindrone acetate 5 mg tablet taken daily. 2 Use LUPRON DEPOT 11.25 mg with norethindrone acetate for retreatment 5 mg tablet taken daily [see Warnings and Precautions ( 5.1 ) ] and assess bone mineral density (BMD) prior to retreatment.
3 Treatment should not exceed 12 months due to concerns about adverse impact on bone mineral density. Fibroids The recommended dosage of LUPRON DEPOT 11.25 mg is one IM injection of 11.25 mg which provides a three-month treatment course.
2.2Reconstitution and Administration for Injection of LUPRON DEPOT Reconstitute and administer the lyophilized microsphere as a single IM injection as directed below. Visually inspect the drug product for particulate matter and discoloration prior to administration, whenever solution and container permit. Inject the LUPRON DEPOT 11.25 mg suspension immediately or discard if not used within two hours as the suspension does not contain a preservative.
1. Visually inspect the LUPRON DEPOT 11.25 mg powder. Do not use the syringe if clumping or caking is evident.
A thin layer of powder on the wall of the syringe is considered normal prior to mixing with the diluent. The diluent should appear clear. 2.
To prepare for injection, screw the white plunger into the end stopper until the stopper begins to turn (see Figure A and Figure B ). Figure A: Figure B: 3. Hold the syringe UPRIGHT.
Release the diluent by SLOWLY PUSHING the plunger for 6 to 8 seconds until the first middle stopper is at the blue line in the middle of the barrel (see Figure C ). Figure C: 4. Keep the syringe upright .
Mix the microsphere powder thorough…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS For Injection: 11.25 mg of leuprolide acetate as a white lyophilized microsphere powder for reconstitution in a single dose prefilled dual chamber syringe; with one chamber containing the lyophilized powder and the other chamber containing the clear diluent. Depot suspension for injection: 11.25 mg lyophilized powder for reconstitution in a dual-chamber syringe. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS LUPRON DEPOT 11.25 mg is contraindicated in women with the following: Hypersensitivity to gonadotropin-releasing hormone (GnRH), GnRH agonist analogs, including leuprolide acetate, or any of the excipients in LUPRON DEPOT 11.25 mg [see Warnings and Precautions ( 5.4 ) and Adverse Reactions ( 6.2 ) ] Undiagnosed abnormal uterine bleeding Pregnancy [see Warnings and Precautions ( 5.2 ) and Use in Specific Populations ( 8.1 ) ] When norethindrone acetate is administered with LUPRON DEPOT 11.25 mg, the contraindications to the use of norethindrone acetate also apply to this combination regimen.
Refer to the norethindrone acetate prescribing information for a list of contraindications for norethindrone acetate. Hypersensitivity to GnRH, GnRH agonist analogs, including leuprolide acetate, or any of the excipients in LUPRON DEPOT 11.25 mg. ( 4 , 5.4 ) Undiagnosed abnormal uterine bleeding.
( 4 ) Pregnancy. ( 4 , 8.1 ) If LUPRON DEPOT 11.25 mg is administered with norethindrone acetate, the contraindications for norethindrone acetate also apply. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Loss of bone mineral density (BMD): Duration of treatment is limited by risk of bone mineral density. When using for management of endometriosis: combination use with norethindrone acetate is effective in reducing loss of BMD; do not retreat without combination norethindrone acetate. Assess BMD before retreatment.
( 1.1 , 1.2 , 5.1 ) Embryo-Fetal Toxicity: May cause fetal harm. Exclude pregnancy before initiating treatment if clinically indicated and discontinue use if pregnancy occurs. Use non-hormonal methods of contraception only.
( 5.2 ) Severe Cutaneous Adverse Reactions (SCARs), including Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN), occurred in patients treated with LUPRON DEPOT. Discontinue LUPRON DEPOT 11.25 mg if signs or symptoms of SCARs develop. Permanently discontinue if SCARs are confirmed.
( 5.3 ) Hypersensitivity reactions including anaphylaxis, have been reported with LUPRON DEPOT 11.25 mg. ( 5.4 ) If LUPRON is administered with norethindrone acetate, the warnings and precautions for norethindrone acetate apply to the combination regimen. ( 5.8 )
5.1Loss of Bone Mineral Density LUPRON DEPOT 11.25 mg induces a hypoestrogenic state that results in loss of bone mineral density (BMD), some of which may not be reversible after stopping treatment. In women with major risk factors for decreased BMD such as chronic alcohol use (> 3 units per day), tobacco use, strong family history of osteoporosis, or chronic use of drugs that can decrease BMD, such as anticonvulsants or corticosteroids, use of LUPRON DEPOT 11.25 mg may pose an additional risk. Carefully weigh the risks and benefits of LUPRON DEPOT 11.25 mg use in these populations.
The duration of LUPRON DEPOT 11.25 mg treatment is limited by the risk of loss of bone mineral density [see Dosage and Administration ( 2.1 )] . When using LUPRON DEPOT 11.25 mg for the management of endometriosis, combination use of norethindrone acetate (add-back therapy) is effective in reducing the loss of BMD that occurs with leuprolide acetate [see Clinical Studies ( 14.2 )] . Do not retreat with LUPRON DEPOT 11.25 mg without combination norethindrone acetate.
Assess BMD before retreatment.
5.2Embryo-Fetal Toxicity Based on animal reproduction studies and the drug’s mechanism of action, LUPRON DEPOT 11.25 mg may cause fetal harm if administered to a pregnant woman and is contraindicated in pregnant women. Exclude pregnancy prior to initiating treatment with LUPRON DEPOT 11.25 mg if clinically indicated. Discontinue LUPRON DEPOT 11.25 mg if the woman becomes pregnant during treatment and inform the woman of potential risk to the fetus [see Contraindications ( 4 ) and Use in Specific Populations ( 8.1 ) ] .
Advise women to notify their healthcare provider if they believe they may be pregnant. When used at the recommended dose and dosing interval, LUPRON DEPOT 11.25 mg usually inhibits ovulation and stops menstruation. Contraception, however, is not ensured by taking LUPRON DEPOT 11.25 mg.
If contraception is indicated, advise women to use non-hormonal methods of contraception while on treatment with LUPRON DEPOT 11.25 mg.
5.3Severe Cutaneous Adverse Reactions Severe cutaneous adverse reactions (SCARs) have been reported in patients receiving GnRH agonists, including LUPRON DEPOT. These reactions include Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP), including cases with visceral involvement and/or requiring skin grafts [see Adverse Reactions ( 6.2 )]. Monitor patients for the signs and symptoms of SCARs such as fever, flu-like symptoms, mucosal lesions, progressive skin rash, or lymphadenopathy.
Advise patients of the signs and symptoms of SCARs. If a SCAR is suspected, discontinue LUPRON DEPOT 11.25 mg. Consult with a healthcare provider with expertise in the diagnosis and management of SCARs.
If a diagnos…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Loss of Bone Mineral Density [see Warnings and Precautions ( 5.1 )] Severe Cutaneous Adverse Reactions [see Warnings and Precautions ( 5.3 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.4 )] Initial Flare of Symptoms with Management of Endometriosis [see Warnings and Precautions ( 5.5 )] Convulsions [see Warnings and Precautions ( 5.6 )] Clinical Depression [see Warnings and Precautions ( 5.7 )] Most common adverse reactions (>10%) in clinical trials were hot flashes/sweats, headache/migraine, vaginitis, depression/emotional lability, general pain, weight gain/loss, nausea/vomiting, decreased libido, and dizziness.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact AbbVie Inc. at 1-800-633-9110 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. LUPRON DEPOT 11.25 mg (Monotherapy) The safety of LUPRON DEPOT 11.25 mg for the endometriosis and fibroids indications was established based on adequate and well-controlled adult studies of LUPRON DEPOT 3.75 mg for 1-month administration and on a single trial of LUPRON DEPOT 11.25 mg.
The safety of LUPRON DEPOT 3.75 mg was evaluated in six clinical studies in which a total of 332 women were treated for up to six months. Women were treated with monthly IM injections of LUPRON DEPOT 3.75 mg. The population age range was 18 to 53 years old.
Adverse Reactions (>1%) Leading to Study Discontinuation In the six studies 1.8% of women treated with LUPRON DEPOT 3.75 mg discontinued prematurely due to hot flashes. Common Adverse Reactions The safety of LUPRON DEPOT 3.75 mg was evaluated in controlled clinical trials in 166 women with endometriosis and 166 women with uterine fibroids. Adverse reactions reported in ≥ 5% of women in either of these populations are noted in Tables 2 and 3 , below.
Table 2. Adverse Reactions Reported in ≥ 5% of Women with Endometriosis Taking LUPRON DEPOT 3.75 mg - 2 Studies LUPRON DEPOT 3.75 mg N=166 Danazol N=136 Placebo N=31 % % % Hot flashes/sweats* 84 57 29 Headache* 32 22 6 Vaginitis* 28 17 0 Depression/emotional lability* 22 20 3 General pain 19 16 3 Weight gain/loss 13 26 0 Nausea/vomiting 13 13 3 Decreased libido* 11 4 0 Dizziness 11 3 0 Acne 10 20 0 Skin reactions 10 15 3 Joint disorder* 8 8 0 Edema 7 13 3 Paresthesias 7 8 0 GI disturbances* 7 6 3 Neuromuscular disorders* 7 13 0 Breast changes/tenderness/pain* 6 9 0 Nervousness* 5 8 0 In these same studies, symptoms reported in < 5% of women included: Body as a Whole - Injection site reactions Cardiovascular System - Palpitations, syncope, tachycardia Digestive System - Appetite changes, dry mouth, thirst Endocrine System - Androgen-like effects, lactation Blood and Lymphatic System - Ecchymosis Nervous/Psychiatric System - Anxiety*, insomnia/sleep disorders*, delusions, memory disorder, personality disorder Dermal System - Alopecia, hair disorder Ocular system - Ophthalmologic disorders* Urogenital System - Dysuria*. * = Possible effect of decreased estrogen.
Table 3. Adverse Reactions Reported in ≥ 5% of Women with Uterine Fibroids (4 Studies) Taking LUPRON DEPOT 3.75 mg LUPRON DEPOT 3.75 mg N=166 Placebo N=163 % % Hot flashes/sweats* 73 18 Headache* 26 18 Vaginitis* 11 2 Depression/emotional lability* 11 4 Asthenia 8 5 General pain 8 6 Joint disorder* 8 3 Edema 5 1 Nausea/vomiting 5 4 Nervousness* 5 1 In these same studies, symptoms reported in < 5% of women included: Body as a Whole - Body odor, flu syndrome, injection site reactions Cardiovascular System - Tachycardia Digestive System - Appetite changes, dry mouth, taste perversion Endocrine System - Androgen-like effects,…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS No drug-drug interaction studies have been conducted with LUPRON DEPOT 11.25 mg.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary LUPRON DEPOT 11.25 mg is contraindicated in pregnancy [see Contraindications ( 4 ) ] . LUPRON DEPOT 11.25 mg may cause fetal harm based on findings from animal studies and the drug’s mechanism of action [see Clinical Pharmacology ( 12.1 ) ] . There are limited human data on the use of LUPRON DEPOT in pregnant women.
Based on animal reproduction studies, LUPRON DEPOT 11.25 mg may be associated with an increased risk of pregnancy complications, including early pregnancy loss and fetal harm. In animal reproduction studies, subcutaneous administration of leuprolide acetate to rabbits during the period of organogenesis caused embryo-fetal toxicity, decreased fetal weights and a dose-dependent increase in major fetal abnormalities in animals at doses less than the recommended human dose based on body surface area using an estimated daily dose.
A similar rat study also showed increased fetal mortality and decreased fetal weights but no major fetal abnormalities at doses less than the recommended human dose based on body surface area using an estimated daily dose [see Data ] . Data Animal Data When administered on day 6 of pregnancy at test dosages of 0.00024 mg/kg, 0.0024 mg/kg, and 0.024 mg/kg (1/300 to 1/3 of the human dose) to rabbits, leuprolide acetate produced a dose-related increase in major fetal abnormalities. Similar studies in rats failed to demonstrate an increase in fetal malformations.
There was increased fetal mortality and decreased fetal weights with the two higher doses of LUPRON DEPOT in rabbits and with the highest dose (0.024 mg/kg) in rats.
8.2Lactation Risk Summary There are no data on the presence of leuprolide acetate in either animal or human milk, the effects on the breastfed infants, or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for LUPRON DEPOT 11.25 mg and any potential adverse effects on the breastfed infant from LUPRON DEPOT 11.25 mg or from the underlying maternal condition.
8.3Females and Males of Reproductive Potential Pregnancy Testing Exclude pregnancy in women of reproductive potential prior to initiating LUPRON DEPOT 11.25 mg if clinically indicated [see Warnings and Precautions ( 5.2 ) ] . Contraception Females LUPRON DEPOT 11.25 mg may cause embryo-fetal harm when administered during pregnancy. LUPRON DEPOT 11.25 mg is not a contraceptive.
If contraception is indicated, advise females of reproductive potential to use a non-hormonal method of contraception during treatment with LUPRON DEPOT 11.25 mg [see Warnings and Precautions ( 5.2 ) ] . Infertility Based on its pharmacodynamic effects of decreasing secretion of gonadal steroids, fertility is expected to be decreased while on treatment with LUPRON DEPOT 11.25 mg. Clinical and pharmacologic studies in adults (>18 years) with leuprolide acetate and similar analogs have shown reversibility of fertility suppression when the drug is discontinued after continuous administration for periods of up to 24 weeks [see Clinical Pharmacology ( 12.1 ) ] .
There is no evidence that pregnancy rates are affected following discontinuation of LUPRON DEPOT 11.25 mg. Animal studies (prepubertal and adult rats and monkeys) with leuprolide acetate and other GnRH analogs have shown functional recovery of fertility suppression.
8.4Pediatric Use Safety and effectiveness of LUPRON DEPOT 11.25 mg for management of endometriosis and the preoperative hematologic improvement of women with anemia caused by fibroids have been established in females of reproductive age. Efficacy is expected to be the same for postpubertal adolescents under the age of 18 as for users 18 years and older. The safety and effectiveness of LUPRON DEPOT 11.25 mg for these indications have not been established in premenarcheal pediatric patients.
8.5Geriatric Use LUPRON DEPOT 11.25 mg is not indicated in postmenopausal women and has not be…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary LUPRON DEPOT 11.25 mg is contraindicated in pregnancy [see Contraindications ( 4 ) ] . LUPRON DEPOT 11.25 mg may cause fetal harm based on findings from animal studies and the drug’s mechanism of action [see Clinical Pharmacology ( 12.1 ) ] . There are limited human data on the use of LUPRON DEPOT in pregnant women.
Based on animal reproduction studies, LUPRON DEPOT 11.25 mg may be associated with an increased risk of pregnancy complications, including early pregnancy loss and fetal harm. In animal reproduction studies, subcutaneous administration of leuprolide acetate to rabbits during the period of organogenesis caused embryo-fetal toxicity, decreased fetal weights and a dose-dependent increase in major fetal abnormalities in animals at doses less than the recommended human dose based on body surface area using an estimated daily dose.
A similar rat study also showed increased fetal mortality and decreased fetal weights but no major fetal abnormalities at doses less than the recommended human dose based on body surface area using an estimated daily dose [see Data ] . Data Animal Data When administered on day 6 of pregnancy at test dosages of 0.00024 mg/kg, 0.0024 mg/kg, and 0.024 mg/kg (1/300 to 1/3 of the human dose) to rabbits, leuprolide acetate produced a dose-related increase in major fetal abnormalities. Similar studies in rats failed to demonstrate an increase in fetal malformations.
There was increased fetal mortality and decreased fetal weights with the two higher doses of LUPRON DEPOT in rabbits and with the highest dose (0.024 mg/kg) in rats.
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness of LUPRON DEPOT 11.25 mg for management of endometriosis and the preoperative hematologic improvement of women with anemia caused by fibroids have been established in females of reproductive age. Efficacy is expected to be the same for postpubertal adolescents under the age of 18 as for users 18 years and older. The safety and effectiveness of LUPRON DEPOT 11.25 mg for these indications have not been established in premenarcheal pediatric patients.
🧓 Geriatric Use ▾
8.5Geriatric Use LUPRON DEPOT 11.25 mg is not indicated in postmenopausal women and has not been studied in this population.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Leuprolide acetate is a long-acting GnRH analog. A single injection of LUPRON DEPOT 11.25 mg results in an initial stimulation followed by a prolonged suppression of pituitary gonadotropins. Repeated dosing of LUPRON DEPOT 11.25 mg at quarterly intervals results in decreased secretion of gonadal steroids.
Consequently, tissues and functions that depend on gonadal steroids for their maintenance become quiescent. This effect is reversible on discontinuation of drug therapy. Leuprolide acetate is not active when given orally.
12.2Pharmacodynamics In a pharmacokinetic/pharmacodynamic study of LUPRON DEPOT 11.25 mg in healthy female subjects (N=20), the onset of estradiol suppression was observed for individual subjects between day 4 and week 4 after dosing. By the third week following the injection, the mean estradiol concentration (8 pg/mL) was in the menopausal range. Throughout the remainder of the dosing period, mean serum estradiol levels ranged from the menopausal to the early follicular range.
Serum estradiol was suppressed to ≤20 pg/mL in all subjects within four weeks and remained suppressed (≤40 pg/mL) in 80% of subjects until the end of the 12-week dosing interval, at which time two of these subjects had a value between 40 and 50 pg/mL. Four additional subjects had at least two consecutive elevations of estradiol (range 43-240 pg/mL) levels during the 12-week dosing interval, but there was no indication of luteal function for any of the subjects during this period. Administration of LUPRON DEPOT 11.25 mg in therapeutic doses results in suppression of the pituitary-gonadal system.
Normal function is usually restored within three months after treatment is discontinued. Therefore, diagnostic tests of pituitary gonadotropic and gonadal functions conducted during treatment and for up to three months after discontinuation of LUPRON DEPOT 11.25 mg may be affected.
12.3Pharmacokinetics Absorption Following a single injection of the 3-month formulation of LUPRON DEPOT 11.25 mg in female subjects, a mean plasma leuprolide concentration of 36.3 ng/mL was observed at 4 hours. Leuprolide appeared to be released at a constant rate following the onset of steady-state levels during the third week after dosing and mean levels then declined gradually to near the lower limit of detection by 12 weeks. The mean (± standard deviation) leuprolide concentration from 3 to 12 weeks was 0.23 ± 0.09 ng/mL.
However, intact leuprolide and an inactive major metabolite could not be distinguished by the assay which was employed in the study. The initial burst, followed by the rapid decline to a steady-state level, was similar to the release pattern seen with the monthly formulation. In a pharmacokinetic/pharmacodynamic study of endometriosis patients, IM LUPRON DEPOT 11.25 mg (n=19) every 12 weeks or IM LUPRON DEPOT 3.75 mg (n=15) every 4 weeks was administered for 24 weeks.
There was no statistically significant difference in changes of serum estradiol concentration from baseline between the 2 treatment groups. Distribution The mean steady-state volume of distribution of leuprolide following intravenous bolus administration to healthy male volunteers was 27 L. In vitro binding to human plasma proteins ranged from 43% to 49%.
Metabolism Leuprolide acetate is a peptide that is primarily degraded by peptidase. In healthy male volunteers, a 1 mg bolus of leuprolide administered intravenously revealed that the mean systemic clearance was
7.6L/h, with a terminal elimination half-life of approximately 3 hours based on a two-compartment model. Metabolite I, a smaller inactive peptide, plasma concentrations measured in 5 prostate cancer patients reached maximum concentration 2 to 6 hours after dosing and were approximately 6% of the peak parent drug concentration. One week after dosing, mean plasma M-I concentrations were approximately 20% of mean leuprolide concentrations.
Excretion Following administration…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Leuprolide acetate is a long-acting GnRH analog. A single injection of LUPRON DEPOT 11.25 mg results in an initial stimulation followed by a prolonged suppression of pituitary gonadotropins. Repeated dosing of LUPRON DEPOT 11.25 mg at quarterly intervals results in decreased secretion of gonadal steroids.
Consequently, tissues and functions that depend on gonadal steroids for their maintenance become quiescent. This effect is reversible on discontinuation of drug therapy. Leuprolide acetate is not active when given orally.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Each LUPRON DEPOT 11.25 mg kit (NDC 0074-3663-03) contains: one prefilled dual-chamber syringe one plunger two alcohol swabs Each single-dose dual chamber syringe contains sterile white lyophilized microsphere powder of 11.25 mg of leuprolide acetate incorporated in a biodegradable polymer in one chamber and a colorless diluent (1.5 mL) in the other chamber. When mixed with the diluent, LUPRON DEPOT 11.25 mg for injection, is administered as a single IM injection. Store between 20° to 25°C (68° to 77°F).
Excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature] .
📋 Description ▾
11 DESCRIPTION Leuprolide acetate is a synthetic nonapeptide analog of gonadotropin-releasing hormone [GnRH or luteinizing hormone releasing hormone (LH-RH)], a GnRH agonist. The chemical name is 5- oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate (salt) with the following structural formula: LUPRON DEPOT 11.25 mg (leuprolide acetate for depot suspension for injection) is available in a prefilled dual-chamber syringe containing sterile lyophilized microspheres powder which, when mixed with diluent, become a suspension intended as an IM injection.
The front chamber of LUPRON DEPOT 11.25 mg prefilled dual-chamber syringe contains leuprolide acetate for depot suspension (11.25 mg), polylactic acid (99.3 mg) and D-mannitol (19.45 mg). The second chamber of diluent contains carboxymethylcellulose sodium (7.5 mg), D-mannitol (75.0 mg), polysorbate 80 (1.5 mg), water for injection, USP, and glacial acetic acid, USP to control pH. During the manufacture of LUPRON DEPOT 11.25 mg, acetic acid is lost, leaving the peptide.
Lupron Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Loss of Bone Density Advise patients about the risk of loss of bone mineral density and that treatment is limited [see Dosage and Administration ( 2.1 ) ] . Advise patients about other factors that can increase and decrease their risk of bone mineral density loss [see Warnings and Precautions ( 5.1 ) ] . Embryo-Fetal Toxicity Advise females of reproductive potential of the possible risk to a fetus.
Advise patients to inform healthcare provider of a known or suspected pregnancy [see Warnings and Precautions ( 5.2 ) and Use in Special Populations ( 8.1 ) ] . If contraception is indicated, advise females of reproductive potential to use non-hormonal contraception during treatment with LUPRON DEPOT 11.25 mg [see Use in Special Populations ( 8.3 ) ] . Severe Cutaneous Adverse Reactions Inform patients that severe cutaneous adverse reactions (SCARs), may occur during treatment with LUPRON DEPOT 11.25 mg.
Advise patients to discontinue LUPRON DEPOT 11.25 mg and to immediately contact their healthcare provider if they experience signs or symptoms of SCARs [see Warnings and Precautions ( 5.3 ) ]. Hypersensitivity Reactions Inform patients that hypersensitivity reactions, including anaphylaxis, have been reported with LUPRON DEPOT. Advise patients to seek appropriate medical care if symptoms of hypersensitivity reactions occur [see Warnings and Precautions ( 5.4 ) and Adverse Reactions ( 6.2 ) ].
Initial Flare of Symptoms Advise patients that they may experience an increase in symptoms during the initial days of therapy. Advise patients that these symptoms should dissipate with continued therapy [see Warnings and Precautions ( 5.5 ) ]. Convulsions Inform patients that convulsions have been reported in patients who have received LUPRON DEPOT.
Advise patients to seek medical attention in the event of a convulsion [see Warnings and Precautions ( 5.6 ) ] . Clinical Depression Inform patients that depression may occur or worsen during treatment with GnRH agonists, including LUPRON DEPOT 11.25 mg, especially in patients with a history of depression. Advise patients to immediately report thoughts and behaviors of concern to healthcare providers [see Warnings and Precautions ( 5.7 ) ] .
Manufactured for AbbVie Inc. North Chicago, IL 60064 by Takeda Pharmaceutical Company Limited Osaka, Japan 540-8645 Revised 09/2025 20085415