ValiRxOpportunity Contact
Mark Treharne, Head of Corporate Development
London, United Kingdom

ValiRx Website
Therapeutic Pharmalicensing.com

VAL401 is the reformulation of the anti-psychotic drug Risperidone in a lipid-based capsule which enables anti-cancer biology that is not seen in the conventional formulation.

Introduction/Background
The proprietary formulation contains a specific ratio of Risperidone to a plant-derived conjugated linoleic acid.

This has been subject to a pilot phase 2 clinical trial, demonstrating improvements in Quality of Life in patients, and an improvement in Overall Survival compared to case-matched control patient data.  The clinical trial was conducted with end-stage non-small cell lung cancer patients as a monotherapy.  Further trials are proposed to include patients with pancreatic ductal adenocarcinoma, having identified improvements in pain, nausea and appetite in the pilot study.

Description of Technology
A chemical genomics screen identified that the anti-psychotic drug Risperidone, inhibits both the oxidative and reductive activities of mitochondrial enzyme HSD10 (hydroxy-steroid dehydrogenase type 10).  In healthy cells, this enzyme is found predominantly in the mitochondria, however in many adenocarcinomas it is found to be greatly over-expressed and located in the cytoplasm of the cell; it is believed to e contributing to cancerous cell metabolism.

By inhibiting HSD10, we believe that Risperidone can provide an effective anti-cancer treatment, either alone or as a combination therapy. 

Conventional Risperidone interacts with a number of GPCR cell surface receptors, including dopamine, serotonin and adrenergic receptors.  It has no reason to enter the cell for effective anti-psychotic activity.  Our formulation is believed to alter the lipophilicity of the molecule, forming an ion-paired structure due to the restricted structural confirmation of the conjugated linoleic acid, allowing the Risperidone to enter the cell and interact with the HSD10 in the cytoplasm.

This mechanism provides the selectivity between cancerous and healthy cells, as the Risperidone will remain unable to enter the mitochondria and interfere with healthy HSD10.

Advantages
VAL401 has competitive advantages from both commercial and scientific viewpoints.

As the reformulation of a generic drug that has been in clinical use for over 20 years, there is already a lot of knowledge about the drug activity in the open literature.  Expected side effects, contraindications and special population are well characterised.  Our pilot clinical trial demonstrated that the exposure to active Risperidone from VAL401 administration was within the safety parameters defined by conventional usage, and no unexpected additional side effects were observed.

The scientific advantage is presented by the current off-label use for risperidone and similar anti-psychotics in cancer patients to mitigate the effects of traditional chemotherapy.  For example it is reported as used to treat opioid induced nausea, chemotherapy induced delirium and to boost appetite.  Although our new formulation changes the cellular distribution of a portion of the drug administered to enable the anti-cancer activity, some remains available in the blood stream and achieves these palliative effects.

The patent portfolio of VAL401 defines the competitive advantage, and includes granted patents covering the method of use for treating adenocarcinoma and for the composition of the formulation.

Clinical Trials
ClinicalTrials.gov Identifier: NCT02875340

The pilot Phase 2 clinical trial dosed 8 end-stage non-small cell lung cancer patients for up to 3 months.

Type of Business Relationship Sought
Out license, Partnership

Patent Information

AUAU 2013,322,612
ILIL 62,081
EUEU 2,900,270
MXMX 15/003,899
JPJP 6,434,410
NZNZ 706,067
NZNZ 726,050
USUS 9,808,462
USUS 10,111,877
USUS 9,585,890
USUS 9,585,887
USUS 9,375,433
USUS 9,072,743
CNCN104797271B
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