Drug intelligence / Profile preview

copanlisib + itraconazole

Development stage
Unknown
Lead developer
Bayer
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This item represents the **co-administration of copanlisib and itraconazole**, not a fixed-dose combination product. **Copanlisib** is a small molecule, intravenous, pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor, with predominant activity against PI3K-alpha and delta isoforms. It is primarily indicated for relapsed follicular lymphoma and other indolent non-Hodgkin lymphomas. **Itraconazole** is a triazole antifungal agent that is a strong inhibitor of CYP3A4. When these drugs are co-administered, itraconazole can significantly affect copanlisib pharmacokinetics by inhibiting its metabolism, potentially increasing copanlisib exposure. This combination is not an approved therapy and is of interest primarily in the context of a drug-drug interaction or for clinical pharmacology considerations, such as the need for copanlisib dose adjustment when co-administered with strong CYP3A4 inhibitors like itraconazole[1][3].

02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)CYP3A4 (Cytochrome P450 3A4)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)

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