Abarelix
- CAS Number: 183552-38-7
Abarelix (trade name: Plenaxis ®) is a drug from the group of GnRH antagonist, which is used for the treatment of advanced or metastatic hormone-dependent prostate cancer.
Pharmacological properties
Abarelix is administered by intramuscular injection, and via the working principle of competitive inhibition of receptors to rapid but reversible disruption of testosterone production. In contrast to treatment with an LHRH analogue, it comes under Abarelix not a testosterone flooding (increase in testosterone levels ), which can trigger an exacerbation of the disease under certain circumstances. A combination with anti-androgens for the prevention of the effect of testosterone - flooding is not necessary.
Clinical studies have shown that under a Abarelix treatment both in comparison with an LHRH analogue treatment ( eg, leuprolide, goserelin, buserelin ), as well as compared with a maximum androgen blockade ( LHRH analogue antiandrogen ) testosterone and PSA decreased faster be. After discontinuation of treatment with Abarelix the drug is washed out and testosterone can be re- produced by the organism, which subside the side effects of testosterone withdrawal. If necessary, treatment can be restarted again.
Side effects
Abarelix may cause anaphylactoid reactions ( in clinical trials in 1.1% of treated patients, but in 3.7% of patients with advanced prostate cancer). For this reason, it is necessary to monitor 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. A drug with fewer allergic effects should be degarelix.
Other Information
Plenaxis was approved in the U.S. in 2003 by the FDA; the former manufacturer, Praecis Pharmaceuticals, but refrained from 2005 to the further commercialization. Granted in 2005, the BfArM approval for Germany, without the product was put on the market. In 2007 the company Speciality European Pharma, founded in 2006 acquired the rights to the drug, in February 2008 it is sold in Germany. An authorization in other EU Member States or Switzerland does not exist yet.