Monograph

L02BX02 - Degarelix

Propably not porphyrinogenic

Rationale

Degarelix is a synthetic peptide derivative that has no effects on CYP enzymes, nor is it suspected of having any portentially porphyrinogenic pharmacodynamic effects.

Chemical description

Peptide and hormone antagonist interacting with sex hormone production.

Therapeutic characteristics

Degarelix is a gonadotropin releasing hormone antagonist used in the treatment of prostate cancer. Treatment with degarelix reduces the levels of luteinising hormone and follicle-stimulating hormone which in turn suppress the release of testosterone. It may also be used in women for suppression of female steroid hormones. It is administered monthly as a subcutaneous injection.

Metabolism and pharmacokinetics

Degarelix is not a substrate for the CYP450 system, but it is biotransformed by peptidic degradation and excreted mainly in the faeces as peptide fragments. In Vitro testing has not shown induction or inhibition of CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4/5 to any great extent. Degarelix has a long half life of 29 days as it is slowly released form the depot formed at the injection site (SPC).

References

#	Citation details	PMID
*	Government bodies
1.	European Public Assessment Report, Degarelix Accord (SPC)/ (Scientific discussion). European Medicines Agency (EMA). (Last updated: 20. july.2023).
*	Summary of Product Characteristics
2.	The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Firmagon. (Last edition: 12.0ctober 2022).

Citation details

PMID

Government bodies

European Public Assessment Report, Degarelix Accord (SPC)/ (Scientific discussion). European Medicines Agency (EMA). (Last updated: 20.

july.2023).

Summary of Product Characteristics

The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Firmagon. (Last edition: 12.0ctober 2022).

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Tradenames and packages

From some sources, we get a list of packages (United Kingdom, Ireland, Estonia). Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway). What you see here is the raw data we get from each country, so there will appear to be duplicates. The bold names are the searchable terms. The gray names that follow are all mapped to the bolded term.

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Netherlands

Degarelix · Degarelix Accord 120 mg poeder en oplosmiddel voor oplossing voor injectie · Degarelix Accord 80 mg poeder en oplosmiddel voor oplossing voor injectie · Firmagon · Firmagon, poeder en oplosmiddel voor oplossing voor injectie

Belgium

Degarelix · Degarelix Accord 120 mg sol. perf. (pdr. + solv.) s.c. ser. préremplie flac. · Degarelix Accord 80 mg sol. perf. (pdr. + solv.) s.c. ser. préremplie flac. · Firmagon · Firmagon 120 mg sol. inj. (pdr. + solv.) s.c. ser. préremplie flac. · Firmagon 80 mg sol. inj. (pdr. + solv.) s.c. ser. préremplie flac.

United Kingdom