A Comprehensive Clinical and Pharmacological Monograph on Hexaminolevulinate (DB06261)

Executive Summary

Hexaminolevulinate is a small molecule optical imaging agent that represents a significant advancement in the diagnosis and management of non-muscle invasive bladder cancer (NMIBC). Administered intravesically, it functions as a prodrug that is selectively metabolized by neoplastic cells into the fluorescent compound protoporphyrin IX (PpIX). When illuminated with blue light during a procedure known as Blue Light Cystoscopy (BLC), cancerous lesions, which preferentially accumulate PpIX, fluoresce a distinct bright pink or red, creating a high-contrast image against the dark blue background of healthy urothelium. This technology, marketed as Cysview® in North America and Hexvix® in Europe, is used as an adjunct to standard White Light Cystoscopy (WLC).

A robust body of evidence from pivotal Phase III clinical trials demonstrates that BLC with Hexaminolevulinate offers superior detection rates for NMIBC lesions compared to WLC alone. The diagnostic advantage is most pronounced for aggressive, flat lesions such as carcinoma in situ (CIS), which are frequently missed by conventional cystoscopy. This improved intraoperative visualization allows for a more complete and accurate transurethral resection of bladder tumors (TURBT).

The clinical benefits of enhanced detection extend to significant improvements in long-term patient outcomes. Studies with long-term follow-up have shown that the use of Hexaminolevulinate-guided BLC is associated with a statistically significant reduction in tumor recurrence rates and a prolonged time to first recurrence. Furthermore, there is an emerging trend toward delayed disease progression and improved bladder preservation. The agent possesses a well-established and favorable safety profile, with most adverse events being mild, transient, and related to the cystoscopy procedure itself.