FENSOLVI KIT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FENSOLVI KIT (FENSOLVI KIT).

How it works

Leuprolide acetate is a GnRH agonist that initially stimulates and then suppresses pituitary gonadotropin release by downregulating GnRH receptors, leading to decreased testosterone and estradiol levels.

What the body does with it

Metabolism	Primarily metabolized by hydrolysis to inactive peptide fragments and excreted in urine; no significant CYP450 involvement.
Excretion	Primarily renal (~80%) and biliary/fecal (~20%) as metabolites and unchanged drug.
Half-life	3-4 hours (terminal); clinical suppression of LH/FSH persists 4 weeks post-injection.
Protein binding	~80% bound to albumin and other plasma proteins.
Volume of Distribution	0.3-0.5 L/kg; moderate distribution indicating limited extravascular penetration.
Bioavailability	SubQ: 85-95% relative to IV; oral: negligible (<5%).
Onset of Action	SubQ: initial LH surge within 2-4 hours; therapeutic suppression by 2-4 weeks.
Duration of Action	Single injection suppresses gonadotropins for 1 month (28-day dosing schedule).

Classification & Brands

Dosing & administration

45 mg subcutaneously every 6 months.

Dosage form	POWDER
Renal impairment	No dose adjustment required for renal impairment.
Liver impairment	No dose adjustment required for hepatic impairment.
Pediatric use	Weight ≥20 kg: 45 mg subcutaneously every 6 months.
Geriatric use	No specific dose adjustment; use standard adult dosing.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for FENSOLVI KIT (FENSOLVI KIT).

Breastfeeding	Not known if leuprolide acetate is excreted in human milk. M/P ratio not available. Due to potential for serious adverse reactions in nursing infants, discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.
Teratogenic Risk	Pregnancy Category X. FENSOLVI (leuprolide acetate) is contraindicated in pregnancy due to risk of fetal harm. First trimester exposure may cause spontaneous abortion or congenital anomalies. Second and third trimester exposure is not applicable as therapy is typically discontinued. No adequate studies in pregnant women; animal studies show embryotoxicity and teratogenicity.

Warnings & precautions

■ FDA Black Box Warning

WARNING: TRANSIENT INCREASE IN TESTOSTERONE LEVELS DURING INITIAL TREATMENT MAY CAUSE WORSENING OF PROSTATE CANCER SYMPTOMS AND SPINAL CORD COMPRESSION.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to leuprolide acetate, GnRH agonists, or any component of the formulation","Pregnancy (may cause fetal harm)","Undiagnosed abnormal vaginal bleeding","Women who are or may become pregnant while using for endometriosis or uterine fibroids"]

Clinical Precautions

Precautions

["Monitor for tumor flare and spinal cord compression in prostate cancer","Risk of QT prolongation","Bone density loss with prolonged use","Hyperglycemia and diabetes","Cardiovascular events (myocardial infarction, sudden cardiac death) with androgen deprivation therapy","Seizures reported","Hypersensitivity reactions including anaphylaxis","Embryo-fetal toxicity; verify pregnancy status before initiating"]

Clinical Tips & Counseling

Drug interactions

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FENSOLVI KIT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FENSOLVI KIT (FENSOLVI KIT).

How it works

What the body does with it

Metabolism	Primarily metabolized by hydrolysis to inactive peptide fragments and excreted in urine; no significant CYP450 involvement.
Excretion	Primarily renal (~80%) and biliary/fecal (~20%) as metabolites and unchanged drug.
Half-life	3-4 hours (terminal); clinical suppression of LH/FSH persists 4 weeks post-injection.
Protein binding	~80% bound to albumin and other plasma proteins.
Volume of Distribution	0.3-0.5 L/kg; moderate distribution indicating limited extravascular penetration.
Bioavailability	SubQ: 85-95% relative to IV; oral: negligible (<5%).
Onset of Action	SubQ: initial LH surge within 2-4 hours; therapeutic suppression by 2-4 weeks.
Duration of Action	Single injection suppresses gonadotropins for 1 month (28-day dosing schedule).

Classification & Brands

Dosing & administration

45 mg subcutaneously every 6 months.

Dosage form	POWDER
Renal impairment	No dose adjustment required for renal impairment.
Liver impairment	No dose adjustment required for hepatic impairment.
Pediatric use	Weight ≥20 kg: 45 mg subcutaneously every 6 months.
Geriatric use	No specific dose adjustment; use standard adult dosing.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for FENSOLVI KIT (FENSOLVI KIT).

Breastfeeding	Not known if leuprolide acetate is excreted in human milk. M/P ratio not available. Due to potential for serious adverse reactions in nursing infants, discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.
Teratogenic Risk	Pregnancy Category X. FENSOLVI (leuprolide acetate) is contraindicated in pregnancy due to risk of fetal harm. First trimester exposure may cause spontaneous abortion or congenital anomalies. Second and third trimester exposure is not applicable as therapy is typically discontinued. No adequate studies in pregnant women; animal studies show embryotoxicity and teratogenicity.

Warnings & precautions

■ FDA Black Box Warning

WARNING: TRANSIENT INCREASE IN TESTOSTERONE LEVELS DURING INITIAL TREATMENT MAY CAUSE WORSENING OF PROSTATE CANCER SYMPTOMS AND SPINAL CORD COMPRESSION.