Metirosine is an inhibitor of catecholamine synthesis used to ameliorate catecholamine-induced symptoms of patients with pheochromocytoma/paraganglioma (PPGL), approved by the United States Food and Drug Administration in 1979. This clinical trial was conducted in accordance with the principles of the Declaration of Helsinki and the Guideline for Good Clinical Practice to receive regulatory approval of metirosine in Japan (JAPIC CTI-152999).
Objective:
The aim of this study was to investigate the efficacy and safety of metirosine in PPGL in a multicenter, open-label clinical trial in accordance with the principles of the Declaration of Helsinki and Good Clinical Practice in Japan (MCAP-J Study).
Patients:
PPGL patients aged≥12 years requiring preoperative or chronic treatment, with baseline urinary metanephrine (uMN) or normetanephrine (uNMN) levels≥3 times the upper limit of normal values; being treated with α-blockers; and with symptoms associated with excess catecholamine.
Results:
Sixteen patients aged 12-86 years participated, 11 males. After 12-week treatment, the proportion of patients who achieved at least 50% reduction of uMN or uNMN from baseline as the primary endpoint was achieved in 31.3% of all patients, 23.1% under chronic treatment, and 66.7% under preoperative treatment at the last evaluation of efficacy. The changing rate for uMN and uNMN were -46.8±24.3% and -42.3±17.5%, respectively. During 24-week treatment, commonly reported adverse events (AEs) related to metirosine were sedation and somnolence in 15 patients (mild in 12, moderate in 2 and severe in 1). Serious AEs related to metirosine were sedation, anemia, and death in 1 patient each. Sedation and anemia were resolved after cessation of metirosine. The cause of death was considered by the investigator to be possibly due to the underlying unresectable pheochromocytoma.
Conclusions:
Metirosine was shown to be effective and tolerated in relieving symptoms by reducing excess catecholamine in PPGL patients under both preoperative and chronic treatment.