Gepotidacin tissue distribution
Description: Demonstrating penetration of gepotidacin in tonsillar and prostate tissues.
Mode of Action (MoA): Topoisomerase type II inhibitor.
ERA4TB-01
Description: Molecule targeting mycobacterial cholesterol cycle.
Mode of Action (MoA): Cholesterol catabolism.
ERA4TB-02
Description: Compound targeting Mycobacterium tuberculosis tryptophan synthase, an enzyme that catalyses the final two steps in tryptophan biosynthesis.
Mode of Action (MoA): M. tuberculosis tryptophan synthase.
ERA4TB-03
Description: Compounds targeting energy metabolism.
Mode of Action (MoA): Electron chain transport.
ERA4TB-04
Description: Compound targeting lysine transfer RNA synthase (Rv3598c), which is an essential gene as assessed by transposon mutagenesis.
Mode of Action (MoA): Lysine transfer RNA synthase.
ERA4TB-06
Description: Potent in vitro inhibitory and bactericidal activity against Mycobacterium tuberculosis.
Mode of Action (MoA): Mycobacterial membrane protein Large 3 (Mmpl3)
ERA4TB-09
Description: Natural product analogs active against Mycobacterium tuberculosis.
Mode of Action: Unknown.
ERA4TB-10
Description: Derivative of piperazinobenzothiazinone that acts as an anti-mycobacterial compound.
Mode of Action: Targets and covalently inhibits the enzyme Decaprenyl-phosphoryl-ribose 2'-epimerase (DprE1).
ERA4TB-11
Description: Small molecule oxaborole.
Mode of Action (MoA): Inhibits leucyl tRNA synthetase (LeuRS)
ERA4TB-13
Description: Targets cholesterol cycle in Mycobacterium tuberculosis.
Mode of Action (MoA): Cholesterol catabolism.
ERA4TB-14
Description: Small molecule compound that leads to the depletion of ATP in three mycobacterial species, M. tuberculosis, M. leprae, and M. ulcerans.
Mode of Action (MoA): Inhibits the mycobacterial cytochrome bc1 complex in the cellular respiration pathway.
ERA4TB-15
Description: A novel class of small-molecule antibiotics shown to inhibit new targets within the M. tuberculosis mycolic acid biosynthesis pathway.
Mode of Action (MoA): Covalently inhibits the acyl transferase domain of Mtb Pks13, a polyketide synthase involved in mycolic acid biosynthesis via a novel mode of inhibition.
ERA4TB-16
Description: A novel class of small-molecule antibiotics shown to inhibit new targets within the M. tuberculosis mycolic acid biosynthesis pathway.
Mode of Action (MoA): Covalently inhibits the acyl transferase domain of Mtb Pks13, a polyketide synthase involved in mycolic acid biosynthesis via a novel mode of inhibition.
ERA4TB-17
Description: A novel class of small-molecule antibiotics that targets several Mtb biosynthesis pathways.
Mode of Action (MoA): Inhibits FadD32, a key enzyme at the interface between the fatty acid synthase and polyketide synthase biosynthetic pathways and is involved in mycolic acid biosynthesis.
ERA4TB-18
Description: A novel class of small-molecule antibiotics that targets several Mtb biosynthesis pathways.
Mode of Action (MoA): Inhibits FadD32, a key enzyme at the interface between the fatty acid synthase and polyketide synthase biosynthetic pathways and is involved in mycolic acid biosynthesis.
Gepotidacin
Description: Gepotidacin is a first-in-class triazaacenaphthylene antibiotic that inhibits bacterial DNA replication by a novel mechanism of action and binding site by inhibiting two different Type II topoisomerase enzymes. Thanks to positive PhIII results for other indications (uUTI & gonorrhoea), gepotidacin is investigated by GNA NOW for its suitability to treat severe enteric infections in low- and middle-income countries.
Mode of Action (MoA): Topoisomerase type II inhibitor
BC1 back up
Description: Lead optimisation program on BC1 inhibitors.
Mode of Action (MoA): Cytochrome bc1 complex in the cellular respiration pathway.
MenG
Description: H2L medChem for novel menaquinone biosynthesis inhibitors.
Mode of Action (MoA): Inhibits menG, a product of which catalyses methylation of demethylmenaquinone.
BDQ LAI
Description: Novel long-acting injectable formulation of bedaquiline for Tb preventive therapy.
Mode of Action (MoA): ATPase.
PASA
Description: Novel para-Aminosalicylic acid (PAS) analogues.
Mode of Action (MoA): Dihydrofolate reductase (DHFR).
HDT
Description: Exploring known host-directed therapies for TB treatment.
Mode of Action(MoA): Various.
Mtr
Description: Exploring known host-directed therapies for TB treatment.
Mode of Action (MoA): Various.
TBA
Description: Novel assets (one first-in-human start) that may synergise with bedaquiline and cytochrome bc1 drugs.
Mode of Action (MoA): Unknown.
Alpibectir
Description: Boosts ethionamide efficacy and lowers the dose with small molecule transcriptional modulators to overcome multi-drug resistant tuberculosis infections.
Mode of Action (MoA): Bacterial transcriptional regulation.
GSK656
Description: A first-in-class investigational antitubercular agent is being developed to treat tuberculosis as part of a future combination regimen.
Mode of Action (MoA): Suppresses protein synthesis in Mycobacterium tuberculosis by inhibiting the enzyme leucyl t-RNA synthetase (LeuRS).
BTZ-043
Description: A first-in-class investigational antitubercular agent is being developed to treat tuberculosis as part of a future combination regimen.
Mode of Action (MoA): Inhibits an essential enzyme for cell wall synthesis in Mycobacteria tuberculosis.
