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Degarelix Brand Names- Degarelix | Firmagon
What is Degarelix
Degarelix acetate is a gonadotropin-releasing hormone (GnRH) receptor antagonist with weak histamine-releasing potential and profound testosterone suppression.
It is indicated for the treatment of patients with advanced prostate cancer.
The only other GnRH receptor antagonist that has been approved for the treatment of prostate cancer, abarelix, had restricted use due to its increased risk of serious, potentially life-threatening, allergic reactions; it was eventually discontinued due to limited use.
After administration, degarelix reversibly binds to the pituitary GnRH receptor resulting in a reduction of gonadotropin and a subsequent drop in testosterone concentration, without an initial increase in serum testosterone or estrogen concentration.
No testosterone surge occurred in any of 409 patients that received degarelix whereas 161 of 201 men that received a GnRH agonist alone or in combination with a nonsteroidal antiandrogen had a testosterone surge with treatment initiation.
Of 409 men, greater than 95% achieved the target serum testosterone concentration by the third day after degarelix 240 mg subcutaneous as compared with none of the 201 men that received leuprolide 7.5 mg IM.
Degarelix offers a treatment option to patients with prostate cancer without the risk of serious histamine-related side effects or the symptoms of clinical flare seen following the administration of GnRH analogs.
Indications
- prostate cancer
For the treatment of advanced prostate cancer
Side Effects
- anaphylactoid reactions
- angioedema
- antibody formation
- arthralgia
- asthenia
- back pain
- chills
- constipation
- diarrhea
- dizziness
- elevated hepatic enzymes
- elevated hepatic enzymes
- erythema
- fatigue
- fever
- gynecomastia
- headache
- hot flashes
- hyperhidrosis
- hypertension
- impotence (erectile dysfunction)
- infection
- injection site reaction
- injection site reaction
- insomnia
- nausea
- night sweats
- osteopenia
- osteoporosis
- QT prolongation
- testicular atrophy
- urticaria
- weight gain
Monitoring Parameters
- prostate-specific antigen (PSA)
Contraindications
- alcoholism
- angioedema
- bradycardia
- breast-feeding
- cardiac arrhythmias
- cardiac disease
- coronary artery disease
- diabetes mellitus
- females
- geriatric
- heart failure
- hepatic disease
- hypertension
- hypocalcemia
- hypokalemia
- hypomagnesemia
- infertility
- laboratory test interference
- long QT syndrome
- malnutrition
- myocardial infarction
- pregnancy
- QT prolongation
- thyroid disease
- urticaria
Interactions
- Alfuzosin
- Amiodarone
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Anagrelide
- Androgens
- Apomorphine
- Aripiprazole
- Arsenic Trioxide
- Artemether; Lumefantrine
- Asenapine
- Atomoxetine
- Azithromycin
- Bedaquiline
- Bismuth Subcitrate Potassium; Metronidazole; Tetracycline
- Bismuth Subsalicylate; Metronidazole; Tetracycline
- Buprenorphine
- Buprenorphine; Naloxone
- Ceritinib
- Chloroquine
- Chlorpromazine
- Cimetidine
- Ciprofloxacin
- Cisapride
- Citalopram
- Clarithromycin
- Class IA Antiarrhythmics
- Clofazimine
- Clozapine
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- Crizotinib
- Danazol
- Dasatinib
- Desflurane
- Deutetrabenazine
- Dextromethorphan; Promethazine
- Dextromethorphan; Quinidine
- Disopyramide
- Dofetilide
- Dolasetron
- Dolutegravir; Rilpivirine
- Donepezil
- Donepezil; Memantine
- Dronedarone
- Droperidol
- Efavirenz
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Eliglustat
- Emtricitabine; Rilpivirine; Tenofovir alafenamide
- Emtricitabine; Rilpivirine; Tenofovir disoproxil fumarate
- Encorafenib
- Enflurane
- Entrectinib
- Eribulin
- Erythromycin
- Erythromycin; Sulfisoxazole
- Escitalopram
- Esterified Estrogens; Methyltestosterone
- Ezogabine
- Fingolimod
- Flecainide
- Fluconazole
- Fluoxetine
- Fluoxetine; Olanzapine
- Fluoxymesterone
- Fluphenazine
- Fluvoxamine
- Foscarnet
- Gemifloxacin
- Gemtuzumab Ozogamicin
- Gilteritinib
- Glasdegib
- Granisetron
- Halofantrine
- Halogenated Anesthetics
- Haloperidol
- Halothane
- Hydroxychloroquine
- Hydroxyzine
- Ibutilide
- Iloperidone
- Inotuzumab Ozogamicin
- Isoflurane
- Itraconazole
- Ivosidenib
- Ketoconazole
- Lapatinib
- Lefamulin
- Lenvatinib
- Levofloxacin
- Lithium
- Lofexidine
- Long-acting beta-agonists
- Loperamide
- Loperamide; Simethicone
- Lopinavir; Ritonavir
- Loxapine
- Macimorelin
- Maprotiline
- Mefloquine
- Meperidine; Promethazine
- Mesoridazine
- Methadone
- Methyltestosterone
- Metronidazole
- Midostaurin
- Mifepristone
- Mirtazapine
- Moxifloxacin
- Nandrolone Decanoate
- Nilotinib
- Norfloxacin
- Octreotide
- Ofloxacin
- Olanzapine
- Ondansetron
- Osilodrostat
- Osimertinib
- Oxaliplatin
- Oxandrolone
- Oxymetholone
- Paliperidone
- Panobinostat
- Pasireotide
- Pazopanib
- Pentamidine
- Perphenazine
- Perphenazine; Amitriptyline
- Phenylephrine; Promethazine
- Pimavanserin
- Pimozide
- Pitolisant
- Posaconazole
- Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
- Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
- Primaquine
- Procainamide
- Prochlorperazine
- Promethazine
- Propafenone
- Quetiapine
- Quinidine
- Quinine
- Ranolazine
- Ribociclib
- Ribociclib; Letrozole
- Rilpivirine
- Risperidone
- Romidepsin
- Saquinavir
- Sertraline
- Sevoflurane
- Short-acting beta-agonists
- Siponimod
- Solifenacin
- Sorafenib
- Sotalol
- Sunitinib
- Tacrolimus
- Tamoxifen
- Telavancin
- Telithromycin
- Testolactone
- Testosterone
- Tetrabenazine
- Thioridazine
- Tolterodine
- Toremifene
- Trazodone
- Trifluoperazine
- Vandetanib
- Vardenafil
- Vemurafenib
- Venlafaxine
- Voriconazole
- Vorinostat
- Ziprasidone
