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Preclinical development of squalenic acid and gemcitabine squalene nanomedicine

Objective

"In the course of the ERC Advanced Grant TERNANOMED, we have discovered that the linkage of squalene (a natural lipid) to many drugs, confers to the resulting bioconjugates the remarkable property to self-assemble as nanoparticles, due to the folded molecular conformation of squalene. This approach is unique and has never been used before. The so called ""squalenoylation"" technology may be considered as a generic platform to construct nanomedicines with high drug loading and targeted drug release triggered by the spacer between the drug and the squalene moiety. Remarkably, it was shown that these nanomedicines were more efficient and less toxic than the parent drugs. The gemcitabine-squalene (Gem-SQ) nanomedicine, our first candidate for further pharmaceutical developments, was shown not only to display an impressive anticancer activity in experimental tumors but also to overcome drug resistance, thus addressing a major challenge in tumor therapy. These pre-clinical data deserve further development towards translation into the clinic for the treatment of the pancreatic cancer, a devastating disease. However, the squalenic acid (SQCO2H), the chemical template essential for the synthesis of the Gem-SQ bioconjugate, is currently obtained through the Van Tamelen reaction which cannot be employed for the preparation of a clinical sample of Gem-SQ, because of the use of CrO3 (a toxic compound) and the poor yield of the reaction. Therefore, the synthesis of SQCO2H represents a lock for further clinical development of our Gem-SQ nanomedicine. The goals of the present proposal are : (i) to perform the total synthesis of SQCO2H through a new « green » chemistry way (which represents in itself a real innovation) allowing (ii) further regulatory acceptable preparation of Gem-SQ nanoparticles. Incidentally, the total synthesis of SQCO2H will avoid environmental concern due to excessive shark hunting and represents by itself some economical value as excipient for the cosmetics."

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Programme(s)

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Topic(s)

Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.

Funding Scheme

Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.

ERC-POC - Proof of Concept Grant

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Call for proposal

Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.

(opens in new window) ERC-2014-PoC

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Host institution

UNIVERSITE PARIS-SACLAY
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 145 000,00
Address
BATIMENT BREGUET - 3 RUE JOLIOT CURIE
91190 Gif-Sur-Yvette
France

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Region
Ile-de-France Ile-de-France Essonne
Activity type
Higher or Secondary Education Establishments
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Total cost

The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.

€ 150 000,00

Beneficiaries (2)

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