Nicox Selects Development Candidate in a New Class of NO-mediated Intraocular Pressure (IOP) Lowering Agents

• Nicox expands internal pipeline with third innovative program

• The new class of compounds combines two converging cellular mechanisms with the aim of achieving an effective and sustained control of intraocular pressure (IOP) in glaucoma patients

• Previously disclosed^1,2 data demonstrate the potential of this new class for lowering IOP

Sophia Antipolis, France

Nicox SA (Euronext Paris: FR0013018124, COX), an international ophthalmology company, today announced that it has selected a new development candidate, NCX 1728, from its proprietary research program focused on nitric oxide (NO)-mediated IOP lowering agents.  An analog of this molecule has demonstrated¹ positive results in ocular hypertensive non-human primates compared to travoprost 0.1%, a prostaglandin analog.  Prostaglandin analogs are the standard of care for IOP lowering therapies.

Nicox owns all exclusive worldwide rights to NCX 1728.  Further optimization of the ophthalmic formulations of NCX 1728 will continue prior to initiating formal pre-Investigational New Drug (IND) tests required for the filing of an IND application.

Michele Garufi, Chairman and Chief Executive Officer of Nicox commented “We are very proud to announce the selection of this new drug candidate, NCX 1728, which becomes our third in-house development program.  NCX 1728 is the first in a new class of molecules combining the clinically proven effects of nitric oxide with phosphodiesterase-5 inhibition, which has been shown to enhance the efficacy and the duration of nitric oxide-mediated effects.”

NCX 1728 was invented in Nicox’s Bresso (Milan, Italy) Research Laboratories using the Company’s proprietary NO-donating research platform, which has enabled the development of a leading scientific and strategic position in the therapeutic application of NO-donating compounds.

NO-mediated IOP lowering agents

It has been established that NO plays a key role in the regulation of IOP and can be linked with other pharmaceutical agents, as is the case with our lead clinical development candidate NCX 470, a second generation NO-donating prostaglandin analog, and the first generation product, VYZULTA^® (latanoprostene bunod ophthalmic solution), 0.024%.  VYZULTA is exclusively licensed worldwide to our partner Bausch + Lomb, who is commercializing it in the U.S. and Canada.  The effect of NO on IOP lowering may be further increased or prolonged by phosphodiesterase-5 (PDE5) inhibitors, which inhibit the degradation of cyclic guanosine monophosphate (cGMP), a key intracellular messenger that is produced as a result of stimulation by NO.

NCX 1728 is the first in a new class of compounds where NO-mediated effects are enhanced by concomitant action of PDE5 inhibition within the same molecule.  Data presented² on this class at the 2019 Annual Meeting of the Association for Research in Vision and Ophthalmology (ARVO) show statistically significant IOP changes compared to vehicle in laser-induced ocular hypertensive non-human primates.  Additional data recently published¹ showed that a molecule of this class reduces IOP to a similar extent but with a faster onset of action when compared to travoprost.

Nicox is terminating the research collaboration with Novaliq GmbH concerning their water-free enabling EyeSol^® technology since NCX 1728 has been selected and will be developed using an in-house, proprietary formulation.

References:

1. Impagnatiello F., Navratil T., Toris C.B., Bergamini M.V.W., et al., Intraocular pressure (IOP) reduction elicited with NCX 1741, a dual acting nitric oxide (NO) and phosphodiesterase type-5 (PDE5) inhibitor or travoprost in a non-human primate model of ocular hypertension and glaucoma Investigative Ophthalmology & Visual Science 2020, Vol.61, 2786
2. Impagnatiello F., Bastia E., Toris CB et al., NCX 1741, a novel NO-donating derivative of the phosphodiesterase-5 inhibitor avanafil, reduces IOP in models of ocular hypertension and glaucoma”, Impagnatiello F., Bastia E., Toris C., Fan S., Brambilla S., Galli C., Almirante N., Bergamini M.V.W. Investigative Ophthalmology & Visual Science 2019, Vol.60, 3770.

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