Zoladex - Drug Information | Physicians Office Resource

Overview

Goserelin acetate, a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin), may be used as an antineoplastic agent and for its endocrine effects.

Goserelin acetate is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin) that is structurally related to leuprolide, nafarelin, and triptorelin.

Goserelin is a potent inhibitor of gonadotropin secretion when given continuously in therapeutic doses and has greater activity than naturally occurring GnRH. After initial administration of goserelin, there is a transient surge in circulating levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone, and estradiol. Following chronic and continuous administration of goserelin (generally, 2-4 weeks after initiation of therapy), a sustained decrease in LH and FSH secretion and a marked reduction of testicular and ovarian steroidogenesis are observed.

Reductions in serum testosterone concentrations in males receiving goserelin are comparable to those achieved after surgical castration (i.e., less than 50 ng/dL). Consequently, physiologic functions and tissues dependent on testosterone for maintenance become quiescent. In clinical trials, with follow-up of more than 2 years, such suppression of testosterone concentrations has been maintained for the duration of therapy.

Serum testosterone concentrations usually return to baseline after cessation of therapy.

In most premenopausal women receiving goserelin, serum estradiol concentrations are reduced to levels comparable to those observed after menopause within 3 weeks of initiating therapy. Consequently, physiologic functions and tissues dependent on gonadal steroids (estrogen) for maintenance become quiescent. Serum estradiol, FSH, and LH concentrations usually return to pretreatment levels within about 12 weeks after subcutaneous implantation of the last 3.6-mg dose of goserelin.

In clinical trials, isolated elevations of estradiol have been observed in about 10% of women. In addition, sustained decreases in LH and FSH secretion may not occur in some women receiving goserelin.

In vitro and animal studies suggest that goserelin may produce regression or inhibition of growth of hormonally sensitive dimethylbenzanthracene (DMBA)-induced mammary tumors in female rats and Dunning R3327H prostate tumors in male rats.

The drug is commercially available as a biodegradable copolymer implant in which goserelin acetate is dispersed in a matrix of lactic and glycolic acids. Following subcutaneous implantation of an implant containing 3.6 or 10.8 mg of goserelin, therapeutic plasma concentrations of goserelin persist for 4 or 12 weeks, respectively.

USES: Goserelin is used to treat certain types of cancer (prostate and breast). It is also used to thin the lining of the uterus (endometrium) in preparation for a procedure to treat abnormal uterine bleeding. Goserelin is also used to treat a condition in which the tissue that normally lines the inside of the uterus also grows outside the uterus (endometriosis).

Talk to your doctor about the risks and benefits of treatment. Goserelin is similar to a natural hormone made by the body (luteinizing hormone releasing hormone-LHRH). It works by decreasing testosterone hormones and estrogen hormones.

This effect helps to slow or stop the growth of certain cancer cells and uterine tissue that need these hormones to grow and spread.

Generic name: goserelin acetate
Pronunciation: (GOE-se-REL-in)

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Zoladex:

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

No dosing information is available for this tab.

Drug interactions

No formal drug interaction studies have been performed.

Contraindications

Known hypersensitivity to goserelin or any ingredient in the formulation, other gonadotropin-releasing hormone (GnRH) agonists, or GnRH. The implant containing 10.8 mg of goserelin should not be used in women, since there are insufficient data available to date to determine whether this preparation is associated with reliable suppression of serum estradiol. Known or suspected pregnancy unless being used for palliative treatment of advanced breast cancer. Abnormal vaginal bleeding of unknown etiology.

Adverse reactions

Initial (usually during the first weeks of therapy) transient increases in serum testosterone occur in most men receiving goserelin and may be associated with temporary worsening in manifestation of prostate cancer. Similarly, initial increases in serum estrogen concentrations occur in most women receiving goserelin and may be associated with transient worsening in the manifestations of breast cancer. Transient changes in blood pressure (hypotension or hypertension) have occurred in patients receiving goserelin.

Adverse effects occurring in 5% or more of men include hot flushes (flashes), sexual dysfunction, decreased erections, lower urinary tract symptoms, lethargy, pain (worsened in the first month), edema, upper respiratory tract infection, rash, sweating, anorexia, chronic obstructive pulmonary disease, congestive heart failure, dizziness, insomnia, and nausea. Decreases in bone mineral density, osteoporosis, and bone fracture have been reported in men receiving goserelin for prostate cancer. Concurrent use of bisphosphonates may minimize bone mineral loss in men receiving GnRH agonists.

Adverse effects occurring in 5% or more of women include hot flushes (flashes), vaginitis, headache, emotional lability, decreased/increased libido, sweating, depression, acne, breast atrophy, seborrhea, edema (may be peripheral), breast enlargement, pelvic symptoms, pain (e.g., abdominal, breast, back), dyspareunia, infection, asthenia, nausea, hirsutism, insomnia, flu-like syndrome, dizziness, application site reaction, and pharyngitis. Decreases in bone mineral density have occurred in women receiving goserelin; concurrent use of hormone replacement therapy or bisphosphonates (e.g., alendronate) may minimize bone mineral loss associated with GnRH agonist therapy without compromising efficacy of these drugs in the management of endometriosis. (See Cautions: Endocrine Effects andsee Precautions and Contraindications, in Leuprolide Acetate 68:18.08.) Currently available data suggest that recovery of bone loss occurs following cessation of GnRH agonist therapy in most patients.

Precautions

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ICD codes

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Formulary status

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Zoladex (goserelin acetate)