Tecnologies per llicenciar

PHX: light-regulated lead compound for the treatment of psoriasis

Advantages

PHX pharmacologic action can be reversibly photoregulated. Our approach can potentially address many limitations of classical PDT, which is based on the chemical cytotoxicity of photogenerated species: (1) PDT is not directed to a specific pharmacological target, (2) it requires oxygen as a precursor, which is depleted in hyperproliferative tissues, and (3) irreversibly photogenerated toxic species diffuse to other tissues, causing adverse effects including pain. PHX can be activated locally using clinically-approved PDT lamps, and would self-inactivate upon diffusion away from the illuminated site. Importantly, by taking the inactivated PHX and only activating it in the skin, we envisage that the treatment will be accompanied with low side-effects.

Goal

Licensing and/or co-development.

Intellectual Property

European patent application filed.

Reference

UBTT0332-E

Contact

Inma Íñiguez
Email: iiniguez@fbg.ub.edu
Tel: +34 934 039798

Introduction

Severe hyperproliferative diseases of the skin and other tissues (where cells grow without control) are often treated with high doses of antiproliferative drugs like methotrexate. They must be administered systemically and cause important off-target toxicity and adverse effects that reduce their therapeutic efficacy and tolerated doses. Alternatively, therapeutic effects can be localized using light to photogenerate cell-killing oxygen species (photodynamic therapy, PDT). Although the interest in PDT is on the rise in dermatology and oncology (with an expected market growth above 7% until 2022), the lack of pharmacological specificity of PDT photosensitizers has limited their advantages.

Description

A research group has developed PHX, a light-regulated, target-specific antiproliferative compound (including a wide range of analogs). PHX is based on an antiproliferative drug approved against psoriasis and several cancers. It is designed to be constitutively inactive in its thermodynamically stable configuration, while it can be activated with light to locally provide the specific pharmacological effects of the reference drug.

The light-dependent antiproliferative efficacy of PHX has been assessed. The results in vitro show inhibition of enzymatic activity and arrest of cell growth under illumination at nanomolar PHX concentration, while no antiproliferative effects are observed in the absence of light for a wide range of concentrations.

In zebrafish larvae, the inactive PHX form behaves as the control, whereas light-activated PHX shows effects equivalent to a reference antiproliferative.

Current stage of development

Currently PoC in vivo with lead compound.

 

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Tags: Life Sciences, Salut i ciències de la vida