Cetrotide® (cetrorelix acetate for injection) should be prescribed by physicians who are experienced in fertility treatment. Before starting treatment with Cetrotide®, pregnancy must be excluded (see CONTRAINDICATIONS and PRECAUTIONS).

General

Cases of hypersensitivity reactions, including anaphylactoid reactions with the first dose, have been reported during post-marketing surveillance (see ADVERSE REACTIONS). A severe anaphylactic reaction associated with cough, rash, and hypotension, was observed in one patient after seven months of treatment with Cetrotide® (10 mg/day) in a study for an indication unrelated to infertility.

Special care should be taken in women with signs and symptoms of active allergic conditions or known history of allergic predisposition. Treatment with Cetrotide® is not advised in women with severe allergic conditions.

Laboratory Tests

After the exclusion of preexisting conditions, enzyme elevations (ALT, AST, GGT, alkaline phosphatase) were found in 1-2% of patients receiving Cetrotide® during controlled ovarian stimulation. The elevations ranged up to three times the upper limit of normal. The clinical significance of these findings was not determined.

During stimulation with human menopausal gonadotropin, Cetrotide® had no notable effects on hormone levels aside from inhibition of LH surges.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term carcinogenicity studies in animals have not been performed with cetrorelix acetate. Cetrorelix acetate was not genotoxic in vitro (Ames test, HPRT test, chromosome aberration test) or in vivo (chromosome aberration test, mouse micronucleus test). Cetrorelix acetate induced polyploidy in CHL-Chinese hamster lung fibroblasts, but not in V79-Chinese hamster lung fibroblasts, cultured peripheral human lymphocytes or in an in vitro micronucleus test in the CHL-cell line. Treatment with 0.46 mg/kg cetrorelix acetate for 4 weeks resulted in complete infertility in female rats which was reversed 8 weeks after cessation of treatment.

Pregnancy Category X

(see CONTRAINDICATIONS)

Cetrotide® is contraindicated in pregnant women.

When administered to rats for the first seven days of pregnancy, cetrorelix acetate did not affect the development of the implanted conceptus at doses up to 38 µg/kg(approximately 1 times the recommended human therapeutic dose based on body surface area). However, a dose of 139 µg/kg (approximately 4 times the human dose) resulted in a resorption rate and a post-implantation loss of 100%.

When administered from day 6 to near term to pregnant rats and rabbits, very early resorptions and total implantation losses were seen in rats at doses from 4.6 µg/kg (0.2 times the human dose) and in rabbits at doses from 6.8 µg/kg (0.4 times the human dose). In animals that maintained their pregnancy, there was no increase in the incidence of fetal abnormalities.

The fetal resorption observed in animals is a logical consequence of the alteration in hormonal levels affected by the antigonadotrophic properties of Cetrotide®, which could result in fetal loss in humans as well. Therefore, this drug should not be used in pregnant women.

Nursing Mothers

It is not known whether Cetrotide® is excreted in human milk. Because many drugs are excreted in human milk, and because the effects of Cetrotide® on lactation and/or the breast-fed child have not been determined, Cetrotide® should not be used by nursing mothers.

Geriatric Use

Cetrotide® is not intended to be used in subjects aged 65 and over.

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