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VPC51299

Catena’s lead compound, VPC51299, targets LPA G-protein coupled receptors (GPCRs) with high potency.  These GPCRs elicit a signaling cascade upon LPA binding the receptor leading to LPA’s biological effects, such as proliferation, migration, angiogenesis and so on.  VPC51299 antagonizes (blocks) this signaling cascade.  Affecting GPCRs is a classic, validated approach to drug therapy—about one third of marketed drugs target GPCR’s, and GPCR modulators have included several multi-billion dollar drugs, such as  Eli Lilly’s Zyprexa, GlaxoSmithKline’s Zantac, Sanofi-Aventis’s Plavix and many more.

 

In rodent experiments, VPC51299 slowed tumor growth and extended lifespan in an aggressive melanoma cancer model, and decreased the size of breast cancer tumor metastases to bone by nearly 70%.  Furthermore, experiments have demonstrated that VPC51299 is orally bioavailable and does not cause overt animal toxicity.  Collectively, these data indicate VPC51299 is a highly promising treatment for cancer, particularly those tumors that metastasize to bone (breast cancer and prostate cancer) or are strongly linked to LPA levels (ovarian cancer).  Investigations are also underway to assess the value of VPC51299 in animal models of organ fibrosis.

 

 

VPC8 Series

Catena controls proprietary chemistry targeted at the synthesis enzyme for LPA, known as Autotaxin (ATX; a.k.a. LysoPLD).  Catena believes that by inhibiting the prodction of LPA, overall signaling of LPA could be reduced, which may provide therapeutic benefits different than those from the targeted signal interruption offered by VPC51299.  Catena’s lead LPA synthesis inhibitor is among the VPC8 Series of chemistry.  Compounds within the VPC8 Series have been identified to be highly potent inhibitors of Autotaxin, functional ex vivo, and without observed toxicity.  Lead optimization is the next step for VPC8 Series of LPA synthesis inhibitors.  Investigations are underway on the promise of this approach in animal models of both cancer and organ fibrosis.

 

 

 

 

 

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