Firmagon Kit W Diluent Syringe (degarelix acetate)
LHrH(GNrH) Antagonist, Pituitary Suppressant Agents Subcutaneous Vial (EA)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Degarelix acetate, a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone (LHRH), gonadorelin) antagonist, is used as an antineoplastic agent.
Degarelix, a synthetic decapeptide, is a gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin) antagonist. The drug immediately, competitively, and reversibly binds to and blocks GnRH receptors in the pituitary, thereby reducing the release of gonadotropins (i.e., luteinizing hormone (LH), follicle-stimulating hormone (FSH)) and, consequently, testosterone without initial stimulation of the hypothalamic-pituitary-gonadal axis and the associated testosterone surge. Degarelix appears to have low histamine-releasing potential compared with other GnRH antagonists; there have been no signs of immediate- or late-onset systemic allergic reactions with degarelix.
Degarelix forms a depot at the injection site following subcutaneous administration from which the drug is very slowly released into circulation. Peak plasma concentrations of degarelix generally occur within 2 days following subcutaneous administration of a single 240-mg dose at a concentration of 40 mg/mL. The pharmacokinetic behavior of degarelix is strongly influenced by its concentration in the injection solution.
Approximately 90% of the drug is bound to plasma proteins. No quantitatively substantial metabolites have been detected in plasma following subcutaneous administration. Degarelix does not appear to be a substrate, inducer, or inhibitor of the cytochrome P-450 (CYP) enzyme or P-glycoprotein transport systems based on in vitro studies.
Degarelix is eliminated in a biphasic manner, with a median terminal half-life of about 53 days following subcutaneous administration of a 240-mg dose at a concentration of 40 mg/mL in prostate cancer patients. Degarelix is subject to peptide hydrolysis during its passage through the hepatobiliary system and is mainly excreted as peptide fragments in feces. Approximately 20-30% of a given dose of degarelix is excreted unchanged in urine, suggesting that approximately 70-80% is excreted via the hepatobiliary system.
USES: Degarelix is used to treat advanced prostate cancer in men. It is not a cure. Most types of prostate cancer need the hormone testosterone to grow and spread.
Degarelix works by reducing the amount of testosterone that the body makes. This helps slow or stop the growth of cancer cells.
Generic name: degarelix acetate
Pronunciation: (DEG-a-REL-ix)
Drug class: LHrH(GNrH) Antagonist, Pituitary Suppressant Agents
Therapeutic class: Antineoplastics
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Firmagon Kit W Diluent Syringe
Indications
The following indications are listed for Firmagon Kit W Diluent Syringe:
- Advanced Prostatic Carcinoma
Also known as: Advanced Cancer Of Prostate Gland, Advanced Malignant Neoplasm Of Prostate, Advanced Prostate Cancer, Advanced Prostate Malignancy, Advanced Prostatic Cancer.
Dosing
Dosage of degarelix acetate is expressed in terms of degarelix.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Firmagon 80 Mg Kit | Maintenance | Inject 80 mg by subcutaneous route every 28 days in the abdomen rotating injection sites. |
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed with degarelix to date.
Degarelix does not appear to be a substrate, inducer, or inhibitor of the cytochrome P-450 (CYP) isoenzyme or P-glycoprotein transport systems based on in vitro studies.
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 degarelix or any ingredient in the formulation.
Degarelix is not indicated for use in women; the drug is contraindicated in women who are or may become pregnant. (See Fetal/Neonatal Morbidity and Mortality under Cautions: Warnings/Precautions and also see Pregnancy under Warnings/Precautions: Specific Populations, in Cautions.)
There are no contraindication contraindications for this drug.
- Chronic heart failure
- Congenital long QT syndrome
- Hypokalemia
- Hypomagnesemia
- Pregnancy
- Prolonged QT interval
- Disease of liver
- Osteopenia
Adverse reactions
Adverse effects reported in 5% or more of patients receiving degarelix in the open-label clinical study include injection site reactions (e.g., pain, erythema, swelling, induration, nodule), hot flashes, weight gain, increased transaminase and gamma-glutamyltransferase (gamma-glutamyltranspeptidase, GGT, GGTP) concentrations, hypertension, back pain, fatigue, chills, arthralgia, constipation, and urinary tract infection.
Less Frequent
- Hypertension
Rare or Very Rare
- Anaphylaxis
- Angioedema
- Osteopenia
More Frequent
- Abnormal hepatic function tests
- Fatigue
- Flushing
- Injection site sequelae
- Weight gain
Less Frequent
- Arthralgia
- Chills
- Constipation
- Diarrhea
- Dizziness
- Erectile dysfunction
- Fever
- General weakness
- Gynecomastia
- Headache disorder
- Hyperhidrosis
- Induration of skin
- Insomnia
- Nausea
- Night sweats
- Testicular atrophy
- Urinary tract infection
Rare or Very Rare
- Urticaria
Precautions
No enhanced messaging available.
Safety and efficacy have not been established in pediatric patients.
Category X. (See Cautions: Contraindications and also see Fetal/Neonatal Morbidity and Mortality under Cautions: Warnings/Precautions.)
Not known whether degarelix is distributed into milk. Degarelix is not indicated for use in women. (See Cautions: Contraindications.)
In clinical studies of degarelix, approximately 82% of the patients were 65 years of age or older, and 42% were 75 years of age or older. No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out. (See Dosage and Administration: Special Populations.)
ICD codes
| Code | Type | Description |
|---|---|---|
| Advanced prostatic carcinoma | ||
| C61 | ICD10CM | Malignant neoplasm of prostate |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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