Drug intelligence / Profile preview

talazoparib + itraconazole

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination** drug of talazoparib and itraconazole, for which no unique brand or combination name exists. - **Talazoparib** is a poly(ADP-ribose) polymerase (PARP) inhibitor, approved for HER2-negative, BRCA-mutant locally advanced or metastatic breast cancer, and in combination treatment for HRR-mutated metastatic castration-resistant prostate cancer[2][3]. - **Itraconazole** is a triazole antifungal agent indicated for deep and superficial fungal infections[4][1]. It is also a potent inhibitor of CYP3A4 enzymes and drug transporters P-glycoprotein and BCRP, which leads to significant pharmacokinetic interactions with many other drugs, including talazoparib[1][4]. - The combination **lacks formal approval as a fixed product** and co-administration is primarily referenced for drug-drug interaction studies: itraconazole can **increase the serum concentration of talazoparib** via CYP3A4 inhibition, potentially raising risk of talazoparib toxicity (myelosuppression, anemia, neutropenia, etc.)[3][4]. - Concomitant use is generally not approved due to safety/interaction concerns unless carefully justified.

02

Targets

ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)PARP1 (Poly (adp-ribose) polymerase 1)CYP51A1 (Sterol 14α-demethylase)

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