| Primary information |
|---|
| ThPP ID | Th1156 |
| Therapeutic Peptide/Protein Name | Abarelix |
| Sequence | N.A. view full sequnce in fasta |
| Functional Classification | IIIc |
| Molecular Weight | 1416.063 |
| Chemical Formula | C72H95ClN14O14 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | 13.2 ± 3.2 days |
| Description | Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market. |
| Indication/Disease | For palliative treatment of advanced prostate cancer. |
| Pharmacodynamics | Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis |
| Mechanism of Action | Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion |
| Toxicity | The maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix. |
| Metabolism | In vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo. |
| Absorption | Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Anti-Testosterone Agents |
| Patents Number | US5968895 |
| Date of Issue | 11/12/96 |
| Date of Expiry | 11/12/13 |
| Drug Interaction | Tacrolimus, Thiothixene, Toremifene, Trimipramine, Voriconazole, Vorinostat, Ziprasidone, Zuclopenthixol- All above drugs cause Additive QTc Prolongation and increases the risk of severe ventricular arrythmias |
| Target | Gonadotropin-releasing hormone receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Plenaxis |
| Company | Speciality european pharma |
| Brand Discription | Plenaxis is a synthetic decapeptide with potent antagonistic activity against naturally occurring gonadotropin releasing-hormone (GnRH). Plenaxis inhibits gonadotropin and related androgen production by directly and competitively blocking GnRH receptors in the pituitary. |
| Prescribed for | Plenaxis is indicated for the palliative treatment of men with advanced symptomatic prostate cancer, in whom LHRH agonist therapy is not appropriate and who refuse surgical castration, and have one or more of the following: (1) risk of neurological compromise due to metastases, (2) ureteral or bladder outlet obstruction due to local encroachment or metastatic disease, or (3) severe bone pain from skeletal metastases persisting on narcotic analgesia. |
| Chemical Name | Abarelix is chemically described as acetyl-D-β-naphthylalanyl-D-4-chlorophenylalanyl- D-3-pyridylalanyl-L-seryl-L-N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(ε)-isopropyllysyl- L-prolyl-D-alanyl-amide. |
| Formulation | The single-dose vial contains 113 mg of anhydrous free base abarelix peptide (net) supplied in an abarelix CMC complex. This complex also contains 19.1 to 31 mg of CMC. After the vial is reconstituted with 2.2 mL of 0.9% sodium chloride injection |
| Physcial Appearnce | Abarelix for injectable suspension is supplied as a white to off-white sterile dry powder |
| Route of Administration | Intramuscular Injection |
| Recommended Dosage | The recommended dose of Plenaxis is 100 mg administered intramuscularly to the buttock on Day 1, 15, 29 (week 4) and every 4 weeks thereafter. |
| Contraindication | Plenaxis is not indicated in women or pediatric patients. In addition, Plenaxis may cause fetal harm if administered to a pregnant woman. |
| Side Effects | Diarrhea, Dizziness, Flushing of Skin, Headache, Constipation, Sleep Disturbance |
| Useful Link | http://www.rxlist.com/plenaxis-drug.htm |
| PubMed ID | 21904569 |
| 3-D Structure | N.A. |