Fuzuloparib-Apatinib pharmacokinetic interaction

The Fuzuloparib-Apatinib pharmacokinetic interaction refers to the pharmacological interplay between fuzuloparib, a poly (ADP-ribose) polymerase (PARP) inhibitor, and apatinib, a selective vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor (PMID: 33155184). This interaction is primarily characterized by the potential for apatinib to alter the metabolic clearance and transport of fuzuloparib, often resulting in increased systemic exposure of the latter (PubChem CID: 6918837). Mechanistically, this is attributed to apatinib's role as an inhibitor of the CYP3A4 enzyme and the P-glycoprotein (P-gp) transporter, both of which are involved in fuzuloparib's disposition (PMID: 33155184). In clinical settings, this combination is used to treat various advanced solid tumors, including ovarian and gastric cancers, where the two drugs act synergistically to inhibit DNA repair and angiogenesis (ClinicalTrials.gov NCT03007069). However, the interaction necessitates careful dose titration to balance efficacy against cumulative toxicities such as bone marrow suppression and vascular side effects. Clinical studies have shown that co-administration can lead to a significant increase in the area under the curve (AUC) and maximum concentration (Cmax) of fuzuloparib compared to monotherapy. Consequently, monitoring for adverse events like anemia, neutropenia, and hypertension is essential when these drugs are used together. As such, this entry represents a complex drug-drug interaction profile rather than a discrete molecular target or receptor.

Other names

Fuzuloparib-Apatinib drug-drug interactionFuzuloparib-Apatinib DDISHR1214-SHR6390 interaction

Inhibition of Cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) by apatinib, which increases the systemic exposure and reduces the clearance of fuzuloparib.