Fensolvi (leuprolide acetate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Leuprolide, a synthetic nonapeptide analog of naturally occurring porcine or ovine gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin), is used as an antineoplastic agent and for its endocrine effects.
Leuprolide is a gonadotropin-releasing hormone (GnRH) analog that shares the action of the naturally occurring hormone.
Leuprolide differs structurally from naturally occurringGnRH by the presence of the d-isomer of leucine at position 6 and an ethylamide group replacing glycine at position 10. These structural modifications result in increased potency of leuprolide (in terms of luteinizing hormone release) compared with naturalGnRH. The drug does not appear to affect receptor affinity for gonadotropins.
The pharmacology of leuprolide is complex and several mechanisms of action may be involved. Repeated dosing of leuprolide results in suppression of the pituitary-gonadal system and decreased secretion of gonadotropins (e.g., follicle stimulating hormone (FSH) and luteinizing hormone (LH)), which suppresses ovarian and testicular steroidogenesis. This inhibitory effect is reversible upon discontinuance of therapy.
The drug does not appear to affect receptor affinity for gonadotropins.
Leuprolide is a peptide that is primarily metabolized by peptidase into smaller inactive peptides. Because of its polypeptide nature, leuprolide acetate is destroyed in the GI tract and, therefore, usually is administered parenterally. Following subcutaneous administration, leuprolide acetate is rapidly and almost completely absorbed.
In adults, bioavailability of leuprolide acetate following subcutaneous administration is comparable to that following IV+ administration. Bioavailability of the drug reportedly is about 94% in rats following subcutaneous administration. Following IM administration of the long-acting depot suspension (Lupron Depot(R)) or subcutaneous administration of the long-acting injectable suspension (Eligard(R), Fensolvi(R)), or emulsion (Camcevi(R)), the drug is released slowly and gradually from its biodegradable copolymer-containing vehicle (after an initial, rapid absorption of immediately available drug), thus providing a prolonged duration of action.
Plasma protein binding of leuprolide has been reported to range from 43-49%. In healthy male volunteers, the terminal elimination half-life of leuprolide following IV administration was approximately 3 hours (based on a 2-compartment model). The pharmacokinetics of leuprolide in patients with impaired renal or hepatic function have not been determined to date.
USES: Leuprolide is used to stop early puberty (precocious puberty) in children. It helps to delay sexual development (such as growth of the breasts/testicles) and the start of menstrual periods. It also helps slow down early bone growth to increase the likelihood of reaching normal adult height.
Leuprolide works by decreasing the amount of sex hormones that a child's body makes (estrogen in girls, testosterone in boys).
Generic name: leuprolide acetate
Pronunciation: (LOO-proe-lide)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Fensolvi
Indications
The following indications are listed for Fensolvi:
- Precocious Puberty
Also known as: Accelerated Sexual Maturity.
Dosing
No dosing information is available for this tab.
Leuprolide acetate is administered by subcutaneous or IM injection depending on the formulation and indication. Leuprolide acetate depot suspension (e.g., LupronDepot(R), LupronDepot-Ped(R)) is administered by IM injection. Leuprolide acetate injectable suspension (Eligard(R), Fensolvi(R)) and leuprolide acetate injection are administered by subcutaneous injection.
Leuprolide mesylate emulsion (Camcevi(R)) is administered by subcutaneous injection.
Extended-release or depot formulations of leuprolide have different release characteristics. Do not use partial syringes, a combination of syringes, or substitute other extended-release products to achieve a particular dose.
Some formulations of leuprolide are not intended for self-administration and should be administered by a healthcare professional only (e.g., Camcevi(R), Eligard(R), Fensolvi(R), Lupron(R), Lupron Depot-Ped(R)); consult the manufacturer's prescribing information for details.
Store leuprolide acetate injection at a temperature of less than 25degreesC in carton until time of use and protect from light; avoid freezing.
Store leuprolide acetate powder for injectable suspension (Lupron Depot(R), Lupron Depot-Ped(R)) and its diluent at a controlled room temperature of 25degreesC; excursions permitted to temperatures ranging from 15-30degreesC. It is not necessary to store the drug or its diluent under refrigeration;avoid freezing.
Store leuprolide acetate injectable suspension (Eligard(R) and Fensolvi(R)) at 2-8degreesC. Once outside the refrigerator,Eligard(R) and Fensolvi(R) may both be stored at 15-30degreesC in their original packaging for up to 8 weeks prior to reconstitution and administration.
Store leuprolide mesylate injectable emlusion (Camcevi(R)) at 2-8degreesC in carton until time of use and protect from light; do not freeze or shake.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed to date with leuprolide.
Metabolism of leuprolide does not involve cytochrome P-450 (CYP) isoenzymes; pharmacokinetic interactionsassociated with CYP isoenzymesare therefore unlikely to occurwith leuprolide.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to gonadotropin-releasing hormone (GnRH), GnRH analogs, or any ingredient in the respective leuprolide formulation.
*Pregnancy.
*Women with abnormal vaginal bleeding of unknown etiology.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Common adverse reactions occurring in >10% of males receiving leuprolide for the treatment of prostate cancer include hot flashes/sweats, general pain, hypertension, testicular atrophy, injection site reaction, GI disorders, joint disorders, musculoskeletal pain, urinary disorder, and lethargy/fatigue.
Common adverse reactions occurring in >10% of females receiving leuprolide for the treatment of endometriosis and uterine leiomyomata include hot flashes/sweats, headache, vaginitis, depression/emotional lability, general pain, asthenia, weight gain/loss, nausea/vomiting, decreased libido, dizziness, constipation, diarrhea, acne, and skin reactions.
Common adverse reactions occurring in >=10% or more of pediatric patients receiving leuprolide for the treatment of centralprecocious pubertyinclude injection site reactions (includingpain), nasopharyngitis, pyrexia, headache, psychiatric events,and cough.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and effectiveness of leuprolide acetate depot suspension for treatment of central precocious puberty (Lupron Depot-Ped(R)) have been established in pediatric patients >=1 year of age. Safety and effectiveness of leuprolide acetate forinjectable suspension for treatment of central precocious puberty (Fensolvi(R)) have been established in pediatric patients >=2 years of age.
Leuprolide acetate injection may cause fetal harm when administered to a pregnant female based on findings from animal studies and the drug's mechanism of action. Discontinue leuprolide if pregnancy occurs during treatment and inform patients of potential risk to the fetus. Leuprolide is contraindicated in pregnant females.
Based on animal reproduction studies, leuprolide 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 embryofetal 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. Similarstudiesin ratsshowed increased fetal mortality and decreased fetal weights but no increase infetal malformations at doses less than the recommended human dose based on body surface area using an estimated daily dose.
There are no data on the presence of leuprolide in either animal or human milk, the effects on 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 leuprolide and any potential adverse effects on the breastfed infant from the drug or underlying maternal condition.
Safety and efficacy of leuprolide were established in older adult male patients for the treatment of prostate cancer; in clinical trials; 69-80% of patients were >=65 years of age.
Leuprolide is not indicated in postmenopausal women and has not been studied in this population.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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