Drug intelligence / Profile preview

iodofalan + lomustine

Development stage
Unknown
Lead developer
Telix Pharmaceuticals
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous (iodofalan), Oral (lomustine)
01

Overview

**Iodofalan + lomustine** is a combination regimen consisting of iodofalan (TLX101), an investigational radiopharmaceutical agent, and lomustine, a nitrosourea-class alkylating agent used in chemotherapeutic protocols. The combination is being explored primarily for recurrent glioblastoma, with iodofalan delivering targeted radiation to tumor cells and lomustine causing DNA alkylation and cross-linking, resulting in cytotoxicity. TLX101 is a small molecule that targets the LAT-1 (L-type amino acid transporter 1) highly expressed in malignant glioma cells, thereby delivering radioactive iodine directly into tumor tissue. This combination aims to achieve synergistic anti-tumor effects by leveraging both targeted radiotherapy (via TLX101) and systemic chemotherapeutic cytotoxicity (via lomustine).

Brand names
TLX101-TxTLX-101-TxTLX 101-Tx
Other names
iodofalan + lomustineTLX101 + lomustine
02

Targets

DNASLC7A5 (Large neutral amino acid transporter small subunit 1)

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