Drug intelligence / Profile preview

itraconazole + IMP4297

Development stage
Phase 1
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of itraconazole and IMP4297**. - **Itraconazole** is a triazole antifungal agent used to treat a variety of fungal infections by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. It acts primarily as a potent inhibitor of the cytochrome P450 enzyme CYP3A4 and P-glycoprotein. - **IMP4297** is a small molecule **poly-(ADP-ribose) polymerase (PARP) 1/2 inhibitor** in clinical development for cancer indications such as ovarian, breast, and other solid tumors. It targets the PARP1 and PARP2 enzymes, pivotal in DNA repair, leading to synthetic lethality in tumor cells deficient in homologous recombination repair. - **The combination has been evaluated in phase I trials for potential drug-drug interactions.** Itraconazole, as a strong CYP3A4 inhibitor, increases the plasma concentration of IMP4297 when co-administered. The combination is generally well tolerated in healthy subjects, with the increased exposure to IMP4297 considered not clinically significant, though monitoring is needed.

02

Targets

CEBPB (CCAAT/enhancer-binding protein beta)CYP51A1 (Sterol 14α-demethylase)PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)

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