title: Triptorelin embonate (6-month formulation).
abstract: A 6-month formulation of the gonadotropin-releasing hormone agonist triptorelin embonate (designed to deliver 22.5 mg of triptorelin over a 6-month period) has been developed for use in the treatment of advanced prostate cancer. Following intramuscular administration of the 6-month formulation of triptorelin embonate 22.5 mg to men with advanced prostate cancer (subset of 15 patients from the pivotal clinical trial), serum testosterone levels initially increased, followed by a rapid, sustained decrease. Castrate serum testosterone levels (i.e. < or =1.735 nmol/L) were achieved in a geometric mean time of 18.8 days. The 6-month formulation of triptorelin embonate achieved and maintained castrate serum testosterone levels in patients with advanced prostate cancer (n = 120), according to the results of the pivotal, noncomparative, multicentre trial (patients received intramuscular triptorelin embonate 22.5 mg on day 1 and at month 6 [week 24]). By day 29, 97.5% of patients had castrate serum testosterone levels. Castrate serum testosterone levels were maintained from months 2 to 12 in 93.0% of patients. Prior to the second injection at month 6, 98.3% of patients had castrate serum testosterone levels, and 98.3% of patients had castrate serum testosterone levels at study completion. The 6-month formulation of triptorelin embonate 22.5 mg was generally well tolerated in patients with advanced prostate cancer; adverse events were of mild severity in the majority of patients. Drug-related adverse events (e.g. hot flushes) were consistent with the pharmacological action of triptorelin. Injection-site reactions occurred in 6.7% of triptorelin embonate recipients.
authors.affiliation: Adis, a Wolters Kluwer Business, Auckland, New Zealand. demail@adis.co.nz
authors.forename: Gillian M
authors.initials: GM
authors.lastname: Keating
mesh_terms: D018931:Antineoplastic Agents, Hormonal / Q000627:therapeutic use*; D015507:Drugs, Investigational / Q000627:therapeutic use*; D007987:Gonadotropin-Releasing Hormone / Q000819:agonists*; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D017329:Triptorelin Pamoate / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D018931:Antineoplastic Agents, Hormonal; D015507:Drugs, Investigational; D017329:Triptorelin Pamoate; D007987:Gonadotropin-Releasing Hormone