Table 8 New antibacterial pharmacophores, separated into major MoA classes, including compound name, phase, antibacterial class, lead source, activity, MoA and administration
From: Antibiotics in the clinical pipeline as of December 2022
Name – phase | Class (lead source) | Mode of actiona (target) - administration |
|---|---|---|
taniborbactam (62) – III | bicyclic bornonate (S) | cell wall (BLIs) – IV |
xeruborbactam (67) – I | bicyclic bornonate (S) | cell wall (BLIs) – IV and po (prodrug) |
ledaborbactam etzadroxil (73) – I | bicyclic bornonate (S) | cell wall (BLIs) – po (prodrug) |
afabicin (21) – II | benzofuran naphthyridine (S) | cell wall, fatty acid biosynthesis (FabI) – IV and po (prodrug) |
quabodepistat (35) – II | 3,4-dihydrocarbostyril (S) | cell wall (DprE1) – po |
BTZ-043 (34) – II | benzothiazinone (BTZ) (S) | cell wall (DprE1) – po |
macozinone (53) – I | benzothiazinone (BTZ) (S) | cell wall (DprE1) – po |
TBA-7371 (37) – I | azaindole (S) | cell wall (DprE1) – po |
TXA709 (50) – I | FtsZ benzamide (S) | cell wall (FtsZ) – po (prodrug) |
murepavadin (49) – I | “protegrin” (P) | cell wall (LptD) – IV & inhalation |
RG6319 – I | “arylomycin”b (NP) | cell wall, protein transport (SPase 1) – not disclosed |
exeporfinium (17) – II | porphyrin (NP) | cell wall/membrane perturbation – topical |
cannabidiol (18) – II | cannabidiol (NP) | cell wall/membrane perturbation – topical |
peceleganan (23) - II | cationic peptide (P) | cell wall/membrane perturbation – topical |
PLG0206 (47) – I | cationic peptide (P) | cell wall/membrane perturbation – topical/IV |
PL-18 (48) – I | cationic peptide (P) | cell wall/membrane perturbation – topical |
Recce-347 – I | polymer (S) | cell wall/membrane perturbation – topical/IV |
gepotidacin (10) – III | triazaacenaphthylene (S) | DNA (GyrA) – IV/po |
zoliflodacin (11) – III | spiropyrimidinetrione (S) | DNA (GyrB) – po |
MGB-BP-3 (16) – II | distamycin (NP) | DNA (minor groove binding) – po topical |
ibezapolstat (27) – II | dichlorobenzyl guanine (S) | DNA (DNA polymerase IIIC) – po topical |
fobrepodacin (32) – II | “ethyl urea benzimidazole” (S) | DNA (GyrB and ParE) – po (prodrug) |
BWC0977 (52) – I | “oxazolidinone containing NBTI” (S) | DNA (DNA gyrase and topoisomerase IV) - I and po |
epetraborole (13) – II/III | oxaborole (S) | protein synthesis (leucyl-tRNA synthetase) – po |
GSK3036656 (36) – II | oxaborole (S) | protein synthesis (leucyl-tRNA synthetase) – po |
CRS3123 (28) – II | “diaryldiamine” (S) | protein synthesis (methionyl-tRNA synthetase) – po topical |
Antibacterials with other MoA | ||
telacebec (31) – II | imidazo[1,2-a]pyridine amide (S) | oxidative phosphorylation (respiratory complex bc1) – po |
GSK2556286 (57) – I | “uracil aryloxypiperidine” (S) | cholesterol catabolism (adenylyl cyclase Rv1625c) – po |
RG6006 – I | macrocyclic peptide (S) | not disclosed - IV |
dovramilast (42) – II | “3-oxo-1H-isoindol-4-yl” (S) | anti-inflammatory (PDE4 inhibitor) – po |
fluorothyazinone (40) – II | thyazinone (S) | antivirulence (type III secretion system) – po |
GSK3882347 – I | mannose-derived (S) | antivirulence (FimH antagonist) – po |
ALS4 – I | not disclosed (S) | antivirulence (4,4ʹ-diapophytoene desaturase, CrtN) – po |
BVL-GSK098 (58) – I | spiroisoxazoline (S) | resistance reversal (inactivation of TetR-like repressor) - po |
