phenotypes moreover

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Posters –
Immunology and Oncology
NAME OF THE PROJECT
NAME OF THE MAIN CONTACT
ORGANISATION NAME
ERK inhibitors for the treatment of RAF and RAS mutated cancers
Jean-Francois GUICHOU
AGV DISCOVERY
Technology
AGV Discovery and its academic partner, Inserm, have identified a new original series of
small molecules (“NCE”) that inhibit ERK kinase activity by using a Fragment-Based
approach. After a chemical optimization within AGV Discovery, the consortium obtained
selective ERK inhibitors with very high affinity and selectivity for their target. Moreover,
In vitro studies revealed promising anti- proliferative activities on Raf and Ras driven
cancer cell lines, especially resistant melanoma cell lines (better than available ERK
inhibitors that are currently in clinical trials). Our lead compound, CB745, shows good
ADMET profile and represents a promising drug candidate for the treatment of resistant
melanoma in monotherapy or in combination with other targeted therapies.
Customers / Target market
Selective ERK inhibitors, to be used in monotherapy or in combination, will be dedicated
for the treatment of RAF and RAS mutated cancers. Patients that correspond to these
phenotypes will be targeted. Studies will focus as a priority on the treatment of
metastatic melanoma (cancers mainly RAF-dependent) and pancreatic cancers (cancers
mainly RAS-dependent).
Industry and competitors
Financing need / Commercial
opportunity
IP – Patent situation
Future steps / Milestones
3 pharmaceutical companies have recently launched early clinical phases for ERK
inhibitors: Genentech (GDC-0994), Celgene (CC-90003) and BioMed Valley (BVD523). Several other companies have also active programs in preclinical stages.
AGV Discovery is searching either for a pharmaceutical company to acquire its Erk
inhibitors program by the end of 2016, or for a fundraising to achieve regulatory
preclinical development and to launch clinical phases.
Patent and worldwide all rights are owned by AGV Discovery and Inserm Transfert.
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Achieve preclinical development
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Out-license the program
Further reading
N/A
Contact person
Mr Jean-François GUICHOU, AGV Discovery, Chief Scientific Officer and founder of the
company, guichou@cbs.cnrs.fr
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