HomeNDC LookupIngredientsLeuprolide Acetate › 70710-1769-03
LEUPROLIDE ACETATE Kit — NDC 70710-1769-03 package photo

LEUPROLIDE ACETATE Kit

by Zydus Pharmaceuticals USA Inc. · 1 KIT in 1 CARTON (70710-1769-3) * 1 VIAL, MULTI-DOSE in 1 CARTON (70710-1768-1) / 2.8 mL in 1 VIAL, MULTI-DOSE * 1 mL in 1 PACKET (70710-1897-8)
NDC 70710-1769-03
🏷️ FDA NDC (as labeled) 70710-1769-3 billing pads the package segment with a zero
Rx only Generic On market Non-controlled
🗂️ Data synced Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

🆔 Identity & classification

FDA NDC (as labeled) 70710-1769-3
Product NDC 70710-1769
11-digit billing NDC 70710176903
NCPDP billing unit EA — each (per item)
RxCUI 545835, 797544
Application # ANDA215826
SPL Set ID 35634415-000f-47db-9bd7-9e16eef3f02e
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2026-01-08
Dosage form KIT
GPI-14 21405010106407
GCN Seq No 044967
GCN 84597
HICL code 021102
Ingredient (HICL) Leuprolide Acetate
HIC1 code V
Therapeutic class — broad (HIC1) Neoplasms
HIC2 code V1
Therapeutic class — intermediate (HIC2) Antineoplastic Drugs
HIC3 code V1O
Therapeutic class — specific (HIC3) Antineoplastic Lhrh(Gnrh) Agonist,Pituitary Suppr.
AHFS code 10:00.00.00
AHFS class Antineoplastic Agents
FDB label name LEUPROLIDE 2WK 14 MG/2.8 ML KT
FDB brand name Leuprolide Acetate
Legend status F — Federal legend — prescription drug or device
TE code (Orange Book) AP · RLD · RS
Why two NDCs? The FDA registers this code as 70710-1769-3 — a 5-4-1 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 package segment → 70710-1769-03. 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 Agonist class.

Pharmacologic class Gonadotropin Releasing Hormone Receptor Agonist
Drug family (ATC) Gonadotropin releasing hormone analogues
How it works Gonadotropin Releasing Hormone Receptor Agonists
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

LabelerZydus Pharmaceuticals USA Inc.
Application holderZYDUS PHARMACEUTICALS USA INC
FDA applicationANDA215826 (ANDA)
Labeler code70710
First marketedJan 2026
Product typeHuman Prescription Drug
Portfolio451 products on file
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 LEUPROLIDE 2WK 14 MG/2.8 ML KT Ingredient Leuprolide Acetate
📖 What it is MedlinePlus · NLM

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 ↗
📗 Our plain-language guide HelloPharmacist
  • 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.
📖 Read our full Leuprolide guide →
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.

🧪 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.

A current SPL was checked, but it does not contain a structured or narrative inactive-ingredient list for this product. This does not mean the product has no inactive ingredients.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

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 eaPer package
Retail pharmacies payNADAC · weekly $197.606
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 $407.34
NADAC price history (per ea) — tap or hover for the price & month
Jun 2026 $197.606 $197.606
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
leuprolide acetate 00121-2106-02 PAI 1 kit $197.606 AP Availability likely
Leuprolide Acetate 00781-4003-32 Sandoz 1 kit $197.606 AP Availability likely
leuprolide acetate 47335-0936-40 Sun 1 kit $197.606 AP Availability likely
Leuprolide Acetate 55150-0478-01 Eugia 1 kit $197.606 AP Availability likely
leuprolide acetate 70121-2537-06 Amneal 1 kit $197.606 AP Availability likely
Leuprolide Acetatethis 70710-1769-03 Zydus 1 kit $197.606 AP Availability likely
Leuprolide Acetate 71288-0569-90 Meitheal 1 kit $197.606 AP Availability likely
Leuprolide Acetate 83634-0454-61 Avenacy, 1 kit $197.606 AP Discontinued
Leuprolide Acetate 72603-0344-01 NorthStar 1 kit $205.708 AP Availability likely +4%
Leuprolide Acetate 72664-0611-28 VGYAAN 1 kit $261.318 AP FDA listed +32%
Lupron Depot 00074-3641-03 AbbVie 1 kit $1,821.130 Availability likely +822%
Lupron Depot 00074-3642-03 AbbVie 1 kit $2,174.170 Availability likely +1000%
Lupron Depot 00074-3663-03 AbbVie 1 kit $5,430.930 Availability likely +2648%
Lupron Depot 00074-3346-03 AbbVie 1 kit $6,516.300 Availability likely +3198%
Leuprolide Acetate 70771-1687-03 Zydus 1 kit AP FDA listed
leuprolide acetate 72843-0591-99 UBI 1 kit AP FDA listed
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
Lupron Depot-PED 00074-2282-03 AbbVie 1 kit FDA listed
Lupron Depot-PED 00074-3779-03 AbbVie 1 kit FDA listed
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
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

🏛️
2026
On the market since
Jan 2026
📍
2026
Currently FDA-listed
listed with the FDA
🔓
·
Generic on the market
this product is a generic
This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

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.

📊 Medicare Part D spend CMS · PART D · 2025 (Q1-Q4)

Medicare Part D (outpatient prescription) spending for Leuprolide Acetate — the program that covers self-administered drugs. 2 manufacturers.
⚠️ 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 Leuprolide Acetate. 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.
Total Part D spend
$40.9K
Claims incl. refills
31
Beneficiaries
15
Spend / beneficiary
$2,724.07
Spend / claim
$1,318.10
💵 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 Leuprolide Acetate — the ingredient across all brands.

Top reported reactions

Hot Flush9,564
Intercepted Product Preparation Error9,222
Death8,528
Syringe Issue7,900
Device Leakage6,230
Fatigue5,098
Injection Site Pain4,870

Age at onset

Neonate21
Infant3
Child247
Adolescent40
Adult1,262
Elderly3,751

Reporter sex

77,113 reports

Serious outcomes

Death12,049
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 7,373 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 Marketing startStatus
70710-1769-03 You're viewing this 1 KIT in 1 CARTON (70710-1769-3) * 1 VIAL, MULTI-DOSE in 1 CARTON (70710-1768-1) / 2.8 mL in 1 VIAL, MULTI-DOSE * 1 mL in 1 PACKET (70710-1897-8) 2026-01-08 Active

🧭 About this NDC listing & data coverage

Finished prescription product Kit / multi-component package

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 ✓ 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

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 70710-1769-3, 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: 70710-1769-03, written without dashes as 70710176903. 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 70710-1769-03, the first segment (70710) is the labeler code FDA assigned to Zydus Pharmaceuticals USA Inc.; the middle segment (1769) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (03) 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 Zydus Pharmaceuticals USA Inc.. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Zydus Pharmaceuticals USA 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.
🎯 Indications and Usage 16 words

INDICATIONS AND USAGE Leuprolide acetate injection is indicated in the palliative treatment of advanced prostatic cancer.

⏱️ Dosage and Administration 113 words

DOSAGE AND ADMINISTRATION The recommended dose is 1 mg (0.2 mL or 20 unit mark) administered as a single daily subcutaneous injection. As with other drugs administered chronically by subcutaneous injection, the injection site should be varied periodically. Each 0.2 mL contains 1 mg of leuprolide acetate, USP, sodium chloride, USP for tonicity adjustment, 1.8 mg of benzyl alcohol, NF as preservative and water for injection, USP.

The pH may have been adjusted with sodium hydroxide, NF and/or Glacial acetic acid, USP. Follow the pictorial directions on the reverse side of this package insert for administration. NOTE: As with all parenteral products, inspect the solution for discoloration and particulate matter before each use.

Contraindications 41 words

CONTRAINDICATIONS Leuprolide acetate injection is contraindicated in patients known to be hypersensitive to GnRH, GnRH agonist analogs or any of the excipients in leuprolide acetate injection: Reports of anaphylactic reactions to GnRH agonist analogs have been reported in the medical literature.

⚠️ Warnings ~1 min read

WARNINGS Initially, leuprolide acetate injection, like other LH-RH agonists, causes increases in serum levels of testosterone. Transient worsening of symptoms, or the occurrence of additional signs and symptoms of prostate cancer, may develop during the first few weeks of leuprolide acetate injection treatment. Patients may experience a temporary increase in bone pain, which can be managed symptomatically.

As with other LH-RH agonists, ureteral obstruction and spinal cord compression have been observed, which may contribute to paralysis with or without fatal complications. Safe use of leuprolide acetate in pregnancy has not been established clinically. Leuprolide acetate injection may cause fetal harm.

Periodic monitoring of serum testosterone and prostate-specific antigen (PSA) levels is recommended, especially if the anticipated clinical or biochemical response to treatment has not been achieved. It should be noted that results of testosterone determinations are dependent on assay methodology. It is advisable to be aware of the type and precision of the assay methodology to make appropriate clinical and therapeutic decisions.

Severe Cutaneous Adverse Reactions Leuprolide acetate can cause severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN), drug reaction with eosinophilia and systemic symptoms (DRESS) and acute generalized exanthematous pustulosis (AGEP). SCARs, including SJS/TEN, DRESS, and AGEP, occurred in patients receiving leuprolide acetate; including cases with visceral involvement and/or requiring skin grafts [see Adverse Reactions]. Monitor patients for the development of SCARs.

If a SCAR is suspected, interrupt leuprolide acetate until the etiology of the reaction has been determined. Consultation with a dermatologist is recommended. If a SCAR is confirmed or for other grade 4 skin reactions, permanently discontinue leuprolide acetate.

🤒 Adverse Reactions ~2 min read

ADVERSE REACTIONS Clinical Trials In the majority of patients testosterone levels increased above baseline during the first week, declining thereafter to baseline levels or below by the end of the second week of treatment. This transient increase was occasionally associated with a temporary worsening of signs and symptoms, usually manifested by an increase in bone pain (see WARNINGS section). Cases of temporary worsening of existing hematuria and urinary tract obstruction have occurred during the first week.

Temporary weakness and paresthesia of the lower limbs have been reported. Potential exacerbations of signs and symptoms during the first few weeks of treatment is a concern in patients with vertebral metastases and/or urinary obstruction which, if aggravated, may lead to neurological problems or increase the obstruction. In a comparative trial of leuprolide acetate injection versus DES, in 5% or more of the patients receiving either drug, the following adverse reactions were reported to have a possible or probable relationship to drug as ascribed by the treating physician.

Often, causality is difficult to assess in patients with metastatic prostate cancer. Reactions considered not drug related are excluded. Leuprolide Acetate Injection (N=98) DES (N=101) Number of Reports Cardiovascular System Congestive heart failure 1 5 ECG changes/ischemia 19 22 High blood pressure 8 5 Murmur 3 8 Peripheral edema 12 30 Phlebitis/thrombosis 2 10 Gastrointestinal System Anorexia 6 5 Constipation 7 9 Nausea/vomiting 5 17 Endocrine System *Decreased testicular size 7 11 *Gynecomastia/breast tenderness or pain 7 63 *Hot flashes 55 12 *Impotence 4 12 Hemic and Lymphatic System Anemia 5 5 Musculoskeletal System Bone pain 5 2 Myalgia 3 9 Central/Peripheral Nervous System Dizziness/lightheadedness 5 7 General pain 13 13 Headache 7 4 Insomnia/sleep disorders 7 5 Respiratory System Dyspnea 2 8 Sinus congestion 5 6 Integumentary System Dermatitis 5 8 Urogenital System Frequency/urgency 6 8 Hematuria 6 4 Urinary tract infection 3 7 Miscellaneous Asthenia 10 10 * Physiologic effect of decreased testosterone.

In this same study, the following adverse reactions were reported in less than 5% of the patients on leuprolide acetate injection. Cardiovascular System - Angina, Cardiac arrhythmias, Myocardial infarction, Pulmonary emboli Gastrointestinal System - Diarrhea, Dysphagia, Gastrointestinal bleeding, Gastrointestinal disturbance, Peptic ulcer, Rectal polyps Endocrine System - Libido decrease, Thyroid enlargement Musculoskeletal System - Joint pain Central/Peripheral Nervous System - Anxiety, Blurred vision, Lethargy, Memory disorder, Mood swings, Nervousness, Numbness, Paresthesia, Peripheral neuropathy, Syncope/blackouts, Taste disorders Respiratory System - Cough, Pleural rub, Pneumonia, Pulmonary fibrosis Integumentary System - Carcinoma of skin/ear, Dry skin, Ecchymosis, Hair loss, Itching, Local skin reactions, Pigmentation, Skin lesions Urogenital System - Bladder spasms, Dysuria, Incontinence, Testicular pain, Urinary obstruction Miscellaneous - Depression, Diabetes, Fatigue, Fever/chills, Hypoglycemia, Increased BUN, Increased calcium, Increased creatinine, Infection/inflammation, Ophthalmologic disorders, Swelling (temporal bone).

In an additional clinical trial and from long-term observation of both studies, the following additional adverse reactions were reported for patients receiving leuprolide acetate injection. Cardiovascular System - Bradycardia, Carotid bruit, Extrasystole, Palpitations, Perivascular cuffing (eyes), Ruptured aortic aneurysm, Stroke, Tachycardia, Transient ischemic attack Gastrointestinal System - Flatus, Dryness of mouth and throat, Hepatitis, Hepatomegaly, Occult blood (rectal exam), Rectal fistula/erythema Endocrine System - Libido increase, Thyroid nodule Musculoskeletal System - Ankylosing spondylosis, Arthritis, Blurred disc margins, Bone fracture, Muscle stiffness, Muscle tenderness, Pelvic fibrosis, Spasms/cra…

🔄 Drug Interactions ~1 min read

Drug Interactions See CLINICAL PHARMACOLOGY , Pharmacokinetics section. Drug/Laboratory Test Interactions Administration of leuprolide acetate in therapeutic doses results in suppression of the pituitary-gonadal system. Normal function is usually restored within 4 to 12 weeks after treatment is discontinued.

Carcinogenesis, Mutagenesis, Impairment of Fertility Two-year carcinogenicity studies were conducted with leuprolide acetate in rats and mice. In rats, a dose-related increase of benign pituitary hyperplasia and benign pituitary adenomas was noted at 24 months when the drug was administered subcutaneously at high daily doses (0.6 to 4 mg/kg). There was a significant but not dose-related increase of pancreatic islet-cell adenomas in females and of testicular interstitial cell adenomas in males (highest incidence in the low dose group).

In mice, no pituitary abnormalities were observed at a dose as high as 60 mg/kg for two years. Patients have been treated with leuprolide acetate for up to three years with doses as high as 10 mg/day and for two years with doses as high as 20 mg/day without demonstrable pituitary abnormalities. Mutagenicity studies have been performed with leuprolide acetate using bacterial and mammalian systems.

These studies provided no evidence of a mutagenic potential. Leuprolide injection may reduce male and female fertility. Administration of leuprolide acetate to male and female rats at dose of 0.024, 0.24, and 2.4 mg/kg as monthly depot formulation for up to 3 months (approximately as low as 1/30 of the human dose based on body surface area using an estimated daily dose in animals and humans) caused atrophy of the reproductive organs, and suppression of reproductive function.

These changes were reversible upon cessation of treatment.

🤰 Pregnancy ~1 min read

Pregnancy Risk Summary Based on findings in animal studies and mechanism of action, leuprolide acetate injection may cause fetal harm when administered to a pregnant woman. There are no available data in pregnant women to inform the drug-associated risk. In animal developmental and reproductive toxicology studies, administration of a monthly formulation of leuprolide acetate on day 6 of pregnancy (sustained exposure was expected throughout the period of organogenesis) caused adverse embryo-fetal toxicity in animals at doses less than the human dose based on body surface area using an estimated daily dose (see data) .

Advise pregnant patients and females of reproductive potential of the potential risk to the fetus. Data Animal Data Major fetal malformations were observed in developmental and reproductive toxicology studies in rabbits after a single administration of the monthly formulation of leuprolide acetate administered on day 6 of pregnancy at test dosages of 0.00024, 0.0024, and 0.024 mg/kg (approximately 1/600 to 1/6 the human dose based on body surface area using an estimated daily dose in animals and humans). Since a depot formulation was utilized in the study, a sustained exposure to leuprolide was expected throughout the period of organogenesis and to the end of gestation.

Similar studies in rats did not demonstrate an increase in fetal malformations, however, there was increased fetal mortality and decreased fetal weights with the two higher doses of the monthly formulation of leuprolide acetate in rabbits and with the highest dose in rats.

🧓 Geriatric Use 39 words

Geriatric Use In the clinical trials for leuprolide acetate injection, the majority (69%) of subjects studied were at least 65 years of age. Therefore, the labeling reflects the pharmacokinetics, efficacy and safety of leuprolide acetate injection in this population.

🆘 Overdosage 79 words

OVERDOSAGE In rats subcutaneous administration of 250 to 500 times the recommended human dose, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a clinical counterpart of this phenomenon. In early clinical trials with leuprolide acetate doses as high as 20 mg/day for up to two years caused no adverse effects differing from those observed with the 1 mg/day dose.

🧬 Clinical Pharmacology ~2 min read

CLINICAL PHARMACOLOGY Leuprolide acetate, a GnRH agonist, acts as an inhibitor of gonadotropin secretion. Animal studies indicate that following an initial stimulation, continuous administration of leuprolide acetate results in suppression of ovarian and testicular steroidogenesis. This effect was reversible upon discontinuation of drug therapy.

Administration of leuprolide acetate has resulted in inhibition of the growth of certain hormone dependent tumors (prostatic tumors in Noble and Dunning male rats and DMBA-induced mammary tumors in female rats) as well as atrophy of the reproductive organs. In humans, subcutaneous administration of single daily doses of leuprolide acetate results in an initial increase in circulating levels of luteinizing hormone (LH) and follicle stimulating hormone (FSH), leading to a transient increase in levels of the gonadal steroids (testosterone and dihydrotestosterone in males, and estrone and estradiol in pre-menopausal females).

However, continuous daily administration of leuprolide acetate results in decreased levels of LH and FSH. In males, testosterone is reduced to castrate levels. In pre-menopausal females, estrogens are reduced to post-menopausal levels.

These decreases occur within two to four weeks after initiation of treatment, and castrate levels of testosterone in prostatic cancer patients have been demonstrated for periods of up to five years. Leuprolide acetate is not active when given orally. Pharmacokinetics Absorption Bioavailability by subcutaneous administration is comparable to that by intravenous administration.

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 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. In rats and dogs, administration of 14 C-labeled leuprolide was shown to be metabolized to smaller inactive peptides, a pentapeptide (Metabolite I), tripeptides (Metabolites II and III) and a dipeptide (Metabolite IV). These fragments may be further catabolized.

The major metabolite (M-I) 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 of LUPRON DEPOT ® 3.75 mg to 3 patients, less than 5% of the dose was recovered as parent and M-I metabolite in the urine.

Special Populations The pharmacokinetics of the drug in hepatically and renally impaired patients has not been determined. Drug Interactions No pharmacokinetic-based drug-drug interaction studies have been conducted with leuprolide acetate. However, because leuprolide acetate is a peptide that is primarily degraded by peptidase and not by cytochrome P-450 enzymes as noted in specific studies, and the drug is only about 46% bound to plasma proteins, drug interactions would not be expected to occur.

📦 How Supplied / Storage and Handling 53 words

HOW SUPPLIED Leuprolide Acetate Injection is a sterile solution supplied in a 2.8 mL multiple-dose vial. The vial is packaged as follows: 14 Day Patient Administration Kit with 14 disposable syringes and 28 alcohol swabs, NDC 70710-1769-3. Store below 77°F (25°C). Do not freeze. Protect from light; store vial in carton until use.

📋 Description 103 words

DESCRIPTION Leuprolide acetate, USP is a synthetic nonapeptide analog of naturally occurring gonadotropin releasing hormone (GnRH or LH-RH). The analog possesses greater potency than the natural hormone. 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: Leuprolide Acetate Injection is a sterile, aqueous solution intended for subcutaneous injection.

It is available in a 2.8 mL multiple-dose vial containing leuprolide acetate, USP (5 mg/mL), sodium chloride, USP (6.3 mg/mL) for tonicity adjustment, benzyl alcohol, NF as a preservative (9 mg/mL), and water for injection, USP. The pH may have been adjusted with sodium hydroxide, NF and/or Glacial acetic acid, USP. Image

💬 Information for Patients ~3 min read

Information for Patients See INFORMATION FOR PATIENTS which appears after the REFERENCE section. Laboratory Tests Response to leuprolide acetate should be monitored by measuring serum levels of testosterone and prostate-specific antigen (PSA). In the majority of patients, testosterone levels increased above baseline during the first week, declining thereafter to baseline levels or below by the end of the second week of treatment.

Castrate levels were reached within two to four weeks and once attained were maintained for as long as drug administration continued.

INFORMATION FOR PATIENTS Be sure to consult your physician with any questions you may have or for information about leuprolide acetate injection and its use. WHAT IS LEUPROLIDE ACETATE INJECTION ? Leuprolide acetate injection is chemically similar to gonadotropin releasing hormone (GnRH or LH-RH) a hormone which occurs naturally in your body.

Normally, your body releases small amounts of LH-RH and this leads to events which stimulate the production of sex hormones. However, when you inject leuprolide acetate injection, the normal events that lead to sex hormone production are interrupted and testosterone is no longer produced by the testes. Leuprolide acetate injection must be injected because, like insulin which is injected by diabetics, leuprolide acetate is inactive when taken by mouth.

If you were to discontinue the drug for any reason, your body would begin making testosterone again. DIRECTIONS FOR USING LEUPROLIDE ACETATE INJECTION Wash hands thoroughly with soap and water. When using a new vial of leuprolide acetate injection, flip off the plastic cover to expose the grey rubber stopper.

Wipe metal ring and rubber stopper with an alcohol wipe each time you use leuprolide acetate injection. Check the liquid in the vial for particulate matter and discoloration prior to use. DO NOT USE if the liquid is not clear or has particles and replace with a new vial.

Remove needle cap and inject the needle in the center of the rubber stopper on the leuprolide acetate injection vial. Take cover off needle. Push the needle through the center of the rubber stopper on the leuprolide acetate injection vial.

Push the plunger all the way in to inject air into the vial. Keep the needle in the vial and turn the vial upside down. Check to make sure the tip of the needle is in the liquid.

Slowly pull back on the plunger, until the syringe fills to the 0.2 mL or 20 unit mark. Toward the end of a two-week period, the amount of leuprolide acetate injection left in the vial will be small. Take special care to hold the vial straight and to keep the needle tip in liquid while pulling back on the plunger.

Keeping the needle in the vial and the vial upside down, check for air bubbles in the syringe. If you see any, push the plunger slowly in to push the air bubble back into the vial. Keep the tip of the needle in the liquid and pull the plunger back again to fill to the 0.2 mL or 20 unit mark.

Do this again if necessary to eliminate air bubbles. To protect your skin, inject each daily dose at a different injection site. Choose an injection site.

Cleanse the injection site with another alcohol wipe. Hold the syringe in one hand. Hold the skin taut, or pull up a little flesh with the other hand, as you were instructed.

Holding the syringe as you would a pencil, inject the needle all the way into the skin at a 90° angle. Push the plunger to administer the injection. Hold an alcohol wipe down on your skin where the needle is inserted and withdraw the needle at the same angle it was inserted.

Use the disposable syringe only once and dispose of it properly as you were instructed. Needles thrown into a garbage bag could accidentally stick someone. NEVER LEAVE SYRINGES OR DRUGS WHERE CHILDREN CAN REACH THEM.

SOME SPECIAL ADVICE You may experience hot flashes when using leuprolide acetate injection. During the first few weeks of treatment you may experience increased bone pain, increased difficulty in…

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
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.