VNRX-14079

VNRX-14079 is a novel non‑β‑lactam cyclic boronate penicillin‑binding protein inhibitor that selectively targets penicillin‑binding protein 2 (PBP2) in Neisseria gonorrhoeae, including multidrug‑resistant strains with mosaic penA alleles conferring ceftriaxone resistance.[3][4][5][7] Discovered and developed by Venatorx Pharmaceuticals as part of a benzoxaborinine (boro‑PBPi) series, it achieves potent in vitro antibacterial and bactericidal activity against both wild‑type and ceftriaxone‑resistant N. gonorrhoeae through high‑affinity binding to PBP2, with low frequency of resistance, favorable selectivity, and a preclinical pharmacokinetic profile compatible with parenteral dosing.[1][3][4][7] In murine vaginal infection models with ceftriaxone‑resistant N. gonorrhoeae, VNRX-14079 demonstrated strong in vivo efficacy, supporting its further preclinical development as a first‑in‑class PBP2‑targeted agent for the treatment of gonorrhea, particularly infections caused by drug‑resistant strains.[1][4]