Vivesto AB products

Many intravenously delivered Active Pharmaceutical Ingredients (APIs) are insoluble or poorly soluble in water. This can be a major hurdle in pharmaceutical development and may cause promising drugs to fail during the development process and may limit the application of approved drugs because of poor solubility. According to some estimates, between 70 and 90% of drugs in the development pipeline are classified as poorly soluble, with approximately 40% of approved drugs similarly affected. Techniques to improve i.v. drug solubility, such as the use of solvents in the form of polymers or polyoxyl oil derivatives and ethanol, may give rise to acute and delayed adverse effects that can be severe. Adverse effects caused by carriers have been seen as an unpleasant trade off in cancer treatment and may necessitate the routine use of corticosteroid as premedication and slow infusions that limit patient flow in the busy chemotherapy suites.

Apealea (paclitaxel micellar) is a patented solvent-free formulation: it applies paclitaxel – a cornerstone within chemotherapy for many different forms of cancer – through Vivesto’s XR-17 technology platform. Apealea is approved by the European regulatory authority EMA for use in combination with carboplatin for the treatment of adult patients with first relapse of platinum-sensitive epithelial ovarian cancer, primary peritoneal cancer and fallopian tube cancer. Apealea has also received orphan drug designation from the US regulatory authority FDA for the treatment of epithelial ovarian cancer, which could entail several potential benefits, including seven years of market exclusivity.

Cantrixil is a product candidate in clinical stage being developed for the treatment of ovarian cancer. Cantrixil consists of the active molecule, a potent and selective third generation benzopyran SMETI inhibitor named TRXE-002-01, encapsulated in a cyclodextrin. It is believed to target a wide spectrum of cancer cells, including chemotherapy-resistant tumor-initiating cells that are thought to be responsible for disease relapse. In December 2020, top-line results of a Phase I open-label study (NCT02903771), conducted at sites in the USA and Australia, were released. The Phase I study met its primary endpoints, establishing clinical proof of concept, subject to further clinical evaluation and confirmation. The results from the Phase I study were published in Cancers, a peer reviewed, open access journal of oncology. A Phase II study with Cantrixil is expected to be initiated in the second half of 2022.

Docetaxel micellar is a product candidate in early clinical development and is a novel formulation that combines XR-17 with docetaxel - a well-established cytotoxin, currently administered intravenously and containing ethanol. In June 2020, Vivesto partnered with the Swiss Group for Clinical Cancer Research (SAKK) with the aim of conducting the first clinical study on the treatment of metastasized prostate cancer with Vivesto’s Docetaxel micellar formulation. In June 2021 the first patient was dosed in an investigator-initiated Phase 1b clinical trial in patients with advanced prostate cancer. It is an open-label, multicenter, single-stage study conducted by SAKK at major hospitals in Switzerland, recruiting 18 chemotherapy-naïve patients with metastatic castration resistant prostate cancer (mCRPC) with adequate bone marrow, liver and renal function.

XR-18 is a research effort based on the XR-17 technology platform intended to provide enhanced properties that improve clinical formulations and applications of active pharmaceutical ingredients (APIs) for cancer treatment. This effort has recently generated promising data including: Addition of components to existing XR-17 formulation improving certain properties. Synthesis of novel excipients exhibiting XR-17-like properties with enhanced stability characteristics. These modifications will be evaluated for feasibility in various drug formulations.