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itraconazole + TGRX-326
- Development stage
- Unknown
- Lead developer
- TargetRx
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Itraconazole is a triazole antifungal agent used to treat a variety of fungal infections, including blastomycosis, histoplasmosis, aspergillosis, and onychomycosis. It works by inhibiting the synthesis of ergosterol, an essential component of fungal cell membranes[1][4]. TGRX-326 is a third-generation small molecule inhibitor targeting anaplastic lymphoma kinase (ALK) and c-ROS proto-oncogene 1 (ROS1) receptor tyrosine kinases. Developed by TargetRx, it is designed for the treatment of non-small cell lung cancer (NSCLC) with ALK/ROS1 gene mutations—especially those resistant to first and second-generation ALK inhibitors such as the G1202R mutation. TGRX-326 demonstrates strong anti-tumor efficacy in preclinical studies and clinical trials, including activity against brain metastases due to its ability to penetrate the blood-brain barrier[5][6][8].
- Brand names
- SporanoxTolsura
- Other names
- itraconazole
02
Targets
ROS1 (Proto-oncogene tyrosine-protein kinase ROS)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)CYP51A1 (Sterol 14α-demethylase)
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