FIS103 / Fannin - LARVOL DELTA

[PREPRINT] FIS103, a Novel SULT1A1-dependent Prodrug, Demonstrates Potent Antitumor Activity in Renal Cell Carcinoma (medRxiv) - "We report that FIS103 displays potent antitumor activity in SULT1A1 over-expressing RCC cell lines (A498 and Caki-1). Contrarily, low SULT1A1 expressing RCC cells (786-O and ACHN) did not show any antitumor effects, which suggests low FIS103 toxicity in the absence of SULT1A1. In silico modeling validated the predicted SULT1A1-FIS103 interaction. Furthermore, FIS103 demonstrates potent SULT1A1-dependent antitumor activity in NU/J mouse xenografts injected with A498 cells. Remarkably, the flank tumors in mice regressed to non-measurable 14 days post-FIS103 treatment and did not regrow through the study conclusion. Additionally, SD rats treated with FIS103 once daily for 14 days demonstrated a promising liver toxicity profile with serum liver enzymes falling within the normal range and histopathology analysis indicated no difference between FIS103 or vehicle treated rats."

Preclinical • Preprint • Genito-urinary Cancer • Kidney Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor