Drug intelligence / Profile preview

LY3484356 + itraconazole

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY3484356 + itraconazole refers to a **combination regimen of two drugs**: - **LY3484356** is a novel, investigational oral selective estrogen receptor degrader (SERD) under clinical development for hormone receptor positive breast cancer. It acts by binding and promoting degradation of the estrogen receptor, antagonizing estrogen-driven cellular proliferation. - **Itraconazole** is a triazole antifungal agent used for systemic and superficial fungal infections. It inhibits fungal cytochrome P450-dependent enzyme 14α-demethylase, disrupting cell membrane synthesis. It is also a potent inhibitor of CYP3A4 and P-glycoprotein, often used in drug-drug interaction studies as a "strong CYP3A4 inhibitor" to study pharmacokinetics of drugs metabolized by CYP3A4[1][2]. The combination is **not approved as a therapeutic regimen** but is commonly used in clinical pharmacology studies to assess CYP3A4-mediated metabolism and drug-drug interaction potential for investigational drugs like LY3484356.

02

Targets

ESR1 (ERα)

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