Abarelix

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Abarelix
Abarelix
Structural formula
Mass / length primary structure 10 amino acids, 1416 Da
Identifier
External IDs
Drug information
ATC code L02 BX01
DrugBank DB00106
Drug class Cytostatic

Abarelix (trade name: Plenaxis ® ) is a drug from the GnRH antagonist group that is used to treat advanced or metastatic hormone-dependent prostate cancer .

Pharmacological properties

Abarelix is ​​administered by intramuscular injection and, through the active principle of competitive receptor inhibition , leads to a rapid but reversible interruption of testosterone production. In contrast to treatment with an LHRH analogue , abarelix does not lead to a testosterone surge (increase in testosterone level), which under certain circumstances can worsen the clinical picture. A combination with antiandrogens to prevent the effect of a testosterone surge is therefore not necessary.

Clinical studies have shown that under a Abarelix treatment both in comparison with an LHRH analog-treatment (eg. As leuprorelin , goserelin , buserelin ), and in comparison with a maximum androgen blockade (LHRH analogue + antiandrogen) testosterone and PPE can be lowered faster. After discontinuing treatment with abarelix, the active ingredient is washed out and testosterone can be produced again by the organism, after which the side effects of testosterone withdrawal subside. If necessary, the treatment can be restarted.

Side effects

Abarelix can cause anaphylactoid reactions (in clinical studies in 1.1% of all treated patients, but in 3.7% of patients with advanced prostate cancer). Because of this, it is necessary to observe the patient for at least 30 minutes after the injection. Another critical side effect is a prolongation of the QT interval with the risk of QT syndrome . Degarelix is said to be an active ingredient with less allergic effects .

Other Information

Plenaxis was approved by the FDA in the USA in 2003 ; the manufacturer at the time, Praecis Pharmaceuticals , refrained from further marketing in 2005. In 2005, the BfArM granted approval for Germany without the product being brought onto the market. In 2007 the company Specialty European Pharma , founded in 2006, acquired the rights to the drug, and it has been marketed in Germany since February 2008. Approval in other EU member states or Switzerland has not yet been granted.

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