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L’invenzione riguarda due nuovi peptidi e relative composizioni farmaceutiche per il trattamento di malattie e condizioni patologiche associate all’alterata motilità, migrazione ed adesione cellulare come angiogenesi, invasione e metastasi tumorali. In particolare viene proposto l’uso di peptidi capaci di inibire la migrazione cellulare, impedendo la formazione di metastasi tumorali. Si tratta di un decapeptide lineare e della sua forma opportunamente ciclizzata.

Patent Status

SUBMITTED

Priority Number

IT-102018000010511

Priority Date

22/11/2018

License

INTERNATIONAL

Problem

Anti-neoplastic therapies target cancer cells, slowing or blocking their proliferation. However, in solid neoplasias, the tumor mass is surrounded by normal cells that support it, promoting its growth and dissemination.
Blocking the pro-tumoral effect of the (non-tumor) cells surrounding solid neoplasms: the case of fibroblasts or CAFs.

Current Technology Limits

-Anti-neoplastic chemotherapics are chemicals capable of hindering and / or stopping the cell multiplication of tumor masses.

-They are administered for the purpose of eliminating cancer cells and preventing their proliferation.

-However, in many cases they are only partially effective. One reason is that the cells surrounding solid tumor masses (stromal cells, including fibroblasts or CAFs) play a critical role in supporting tumor growth and dissemination. They are not targeted by the conventional therapies.

-A possible solution is to adopt the strategy of co-targeting in which the tumor cells are directly affected, and indirectly, by counteracting the stromal component that supports them.

-Here a new molecule is presented that is able to counteract both the tumor component and the fibroblasts CAFs surrounding and supporting the tumor.

Killer Application

Novel cyclic decapeptide uPACYCLIN: reduces lung metastases by 75% in a mouse model of metastatic dissemination

-Acts at pico / nanomolar concentrations.
-Blocks the avb5 integrin.
-Inhibits migration / invasion of breast, lung, prostate, glioma cancer cells.
-Blocks the pro-tumor activity of primary CAFs from breast carcinomas.

Our Technology and Solutions

New decapeptides with anti-tumor and anti-metastatic properties to block tumor cells and CAFs. The new decapeptides can be a reference for new and more effective anti-neoplastic strategies. They counteract tumor invasiveness both directly and by acting on the peritumor fibroblasts (CAF) and blocking their pro-tumor activity.

The new decapeptides, in particular uPACYCLIN:
-inhibit migration and invasion of tumor cells at picomolar concentrations.
-reduce the formation of lung metastases by 75% in a mouse model of tumor dissemination.
- they block the pro-tumor activity of peritumoral fibroblasts of patients with breast tumors.

Scheduled:
- continue in animal experimentation, with stability and pharmacokinetic tests of the peptides.

- test the new peptides in particular uPAcyclin for use as remedies for inflammatory skin and eye diseases and in formulations for topical use that require reduced testing times.

Advantages

The new compounds:
- they are potentially useful in human pathological conditions resulting from an altered or excessive cell migration / invasiveness, including neoplasms (acting on the peritumor component), angiogenesis, ocular and cardiovascular diseases. Because:
- they have a high affinity for potency and stability at pico-nanomolar concentrations.
- inhibited lung metastases in a mouse model by 75%.
- no toxicity effects were observed in vivo.

Roadmap

We are looking for Companies interested to:
- collaborate with us to continue animal experiments, further testing stability and pharmacokinetics of the cyclic peptide.

-joint experimentation in animal models for the use of these new peptide compounds in formulations for topical use, as remedies for inflammatory skin and eye diseases, for reduced testing and development times.

Review the Technology
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TRL 1
Basic Principles
Basic principles tested
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Formulation
Technology concept formulated
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Proof of concept
Experimental proof of concept
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Laboratory Prototype
Technology validated in lab
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Prototype tested on pilot-scale/large-scale
Technology validated in relevant environment (industrially relevant environment in the case of key enabling technologies)
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Commercial prototype
Technology demonstrated in relevant environment (industrially relevant environment in the case of key enabling technologies)
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Real world validation
System prototype demonstration in operational/real-world environment
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First complete and commercial product
System complete and qualified
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Full commercial application
Actual system proven in commercial environment (competitive manufacturing in the case of key enabling technologies; or in space)

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