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NAICONS' PIPELINE

other leads


Several structurally unique compounds have been identified by Naicons and are under evaluation for further development.  Published compounds include: Antibacterial Paramagnetic Quinones and Allocyclinones from Actinoallomurus; NAI-802, a variant of actagardine with improved antibacterial activity; orthoformimycin, a structurally and mechanistically unusual inhibitor of bacterial protein synthesis. Other structurally unique compounds have not yet been disclosed.


Read more: Selected bibliography

PUM (Pseudouridimycin)               Producer strain: Streptomyces sp.


a novel class of RNA polymerase inhibitors with extremely low frequency of resistance selection. Active against Gram-positive and Gram-negative pathogens,including antibiotic-resistant isolates, with efficacy in animal models of infection.  


Read more: Selected bibliography

NAI-112                          Producer strain: Actinoplanes DSMZ24059


a lanthipeptide with efficacy in animal models of nociceptic and inflammatory pain. Likely to act through the vanilloid pathway by a novel target. It can be developed for the treatment of neuropathic pain.


Read more: Selected bibliography

NAI-603                Producer strain: Actinoplanes sp. ATCC 33076


a semi-synthetic derivative of ramoplanin highly active against aerobic and anareobic Gram-positive pathogens, including all antibiotic-resistant strains (e.g. MRSA and VRE); rapidly bactericidal, well-tolerated and efficacious in experimental models of infection. It can be developed for iv or topical use for several indications. Favorable toxicological profile.


Read more: Selected bibliography

NAI-107 (and related lantibiotics)        

                                                            Producer strain: Microbispora sp. 107891


a family of related lantibiotics highly active against aerobic and anaerobic Gram-positive pathogens, including all antibiotic-resistant strains (e.g. MRSA and VRE); rapidly bactericidal and highly efficacious in experimental models of infection (septicemia, endocarditis, granuloma pouch), with favorable PK/PD properties. The compound inhibits cell wall synthesis by binding to lipid II. It is being developed for iv treatment of serious infections by gram-positive bacteria. The most advanced compound has a favorable toxicological profile.


Read more: Selected bibliography

NAI-Acne                          Producer strain: Planobispora rosea


a semi-synthetic thiopeptide highly selective against Propionibacterium acnes, including antibiotic-resistant strains. No activity against other skin flora. The compound targets elongation factor Tu in protein synthesis. It is being developed for the topical treatment of moderate-severe acne and has completed a phase I/IIa study in healthy volunteers. Recently licensed to Cassiopea SpA, it has completed a phase II proof of concept clinical study. read more>


Read more: Selected bibliography