gepotidacin + cimetidine

**Gepotidacin + cimetidine** is the co-administration of two pharmaceuticals: gepotidacin, a novel, first-in-class triazaacenaphthylene antibiotic, and cimetidine, a nonspecific organic cation transporter (OCT) and multidrug and toxic extrusion transporter (MATE) renal transport inhibitor. Gepotidacin acts by selective inhibition of bacterial DNA gyrase and topoisomerase IV, targeting the GyrA subunit and ParC subunit; this disrupts bacterial DNA replication, transcription, and cell division by binding within a DNA-enzyme pocket[4][5]. Gepotidacin is structurally and pharmacologically distinct from fluoroquinolone antibiotics and is bactericidal against major pathogens in uncomplicated urinary tract infections, including *Escherichia coli*, *Klebsiella pneumoniae*, *Citrobacter freundii* complex, *Staphylococcus saprophyticus*, and *Enterococcus faecalis*[4][5]. Cimetidine functions mainly as a histamine H2 receptor antagonist used to reduce stomach acid, but in this context, acts as an inhibitor of renal transporters (OCT2 and MATE1/MATE2), affecting the renal clearance of coadministered drugs like gepotidacin[1][2][3]. No clinically significant drug-drug interaction exists in terms of gepotidacin plasma pharmacokinetics when coadministered with cimetidine; however, biomarkers indicate partial OCT2 inhibition and extensive MATE inhibition (increased serum creatinine, reduced creatinine clearance)[1][2][3]. Gepotidacin was developed by GSK, while cimetidine is an established generic drug originally developed by SmithKline & French.

Other names

gepotidacin hydrochloridegepotidacin mesylate