Abarelix

Last updated
Abarelix
Abarelix.svg
Clinical data
Trade names Plenaxis
AHFS/Drugs.com Monograph
Routes of
administration 		Intramuscular injection
Drug class GnRH analogue; GnRH antagonist; Antigonadotropin
ATC code
Pharmacokinetic data
Protein binding 96–99%
Identifiers
  • N-acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparagyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide [1]
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C72H95ClN14O14
Molar mass 1416.09 g·mol−1
3D model (JSmol)
  • CC(C)C[C@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H](NCc5ccc4ccccc4c5)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N6CCC[C@H]6C(=O)N[C@H](C)C(N)=O
  • InChI=1S/C72H95ClN14O14/c1-41(2)32-54(64(93)80-53(17-10-11-30-77-42(3)4)72(101)87-31-13-18-60(87)69(98)78-43(5)63(75)92)81-68(97)58(38-62(74)91)84-70(99)61(37-46-22-27-52(90)28-23-46)86(7)71(100)59(40-88)85-67(96)57(36-48-14-12-29-76-39-48)83-66(95)56(34-45-20-25-51(73)26-21-45)82-65(94)55(79-44(6)89)35-47-19-24-49-15-8-9-16-50(49)33-47/h8-9,12,14-16,19-29,33,39,41-43,53-61,77,88,90H,10-11,13,17-18,30-32,34-38,40H2,1-7H3,(H2,74,91)(H2,75,92)(H,78,98)(H,79,89)(H,80,93)(H,81,97)(H,82,94)(H,83,95)(H,84,99)(H,85,96)/t43-,53+,54+,55-,56-,57-,58-,59+,60+,61+/m1/s1 Yes check.svgY
  • Key:AIWRTTMUVOZGPW-HSPKUQOVSA-N Yes check.svgY
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Abarelix, sold under the brand name Plenaxis, is an injectable gonadotropin-releasing hormone antagonist (GnRH antagonist) which is marketed in Germany and the Netherlands. It is primarily used in oncology to reduce the amount of testosterone made in patients with advanced symptomatic prostate cancer for which no other treatment options are available. [2] [3]

It was originally marketed by Praecis Pharmaceuticals as Plenaxis, [2] and is now marketed by Speciality European Pharma in Germany [4] after receiving a marketing authorization in 2005. The drug was introduced in the United States in 2003, but was discontinued in this country in May 2005 due to poor sales and a higher-than-expected incidence of severe allergic reactions. [5] It remains marketed in Germany and the Netherlands however. [6]

See also

References

  1. ↑ "Abarelix". PubChem. 2017-07-29.
  2. 1 2 "Abarelix". Drugs.com. Archived from the original on 2018-02-10. Retrieved 2018-01-23.
  3. ↑ Boccon-Gibod L, van der Meulen E, Persson BE (June 2011). "An update on the use of gonadotropin-releasing hormone antagonists in prostate cancer". Therapeutic Advances in Urology. 3 (3): 127–40. doi:10.1177/1756287211414457. PMC   3159401 . PMID   21904569.
  4. ↑ Pharmazeutische Zeitung online: Abarelix (in German)
  5. ↑ Minev B (13 January 2011). Cancer Management in Man: Chemotherapy, Biological Therapy, Hyperthermia and Supporting Measures. Springer Science & Business Media. pp. 182–. ISBN   978-90-481-9704-0.
  6. ↑ "Abarelix". Drugs.com. Archived from the original on 2019-08-29. Retrieved 2018-08-27.


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