Vividion Therapeutics has dosed the first subject in a Phase I trial of an oral inhibitor, VVD-159642, aimed at treating rat sarcoma (RAS)-driven cancers.
This trial aims to assess VVD-159642’s tolerability, preliminary anti-tumour activity, pharmacokinetics, and safety as a monotherapy and in conjunction with trametinib or sotorasib in individuals with advanced solid tumours.
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According to the company, the therapy is the fourth clinical-stage programme derived from its chemoproteomics discovery platform.
It is designed to block the signalling pathway of the RAS-phosphatidylinositol 3-kinase alpha (PI3Kα), which plays an important role in the development and progression of solid tumours.
In addition to VVD-159642, the company is conducting other Phase I trials assessing an oral, Kelch-like, ECH-associated protein 1 (KEAP1) activator, as well as an oral signal transducer and activator of transcription 3 (STAT3) focusing on solid and haematologic malignancies.
Vividion Therapeutics’ chief medical officer Jenna Goldberg said: “Despite being a major driver in approximately 20% of cancers, the RAS gene has proven exceptionally difficult to target with drugs, largely due to its essential role in the RAS-PI3Kα signalling pathway, which is vital for healthy cell function.
“In addition to providing a more tolerable alternative to current therapies, we believe that VVD-159642 has the potential to treat a broad patient population, including in both RAS-mutant and HER2-overexpressed tumours, and may deliver increased efficacy in combination with other RAS/mitogen-activated protein kinase (MAPK) pathway inhibitors.”
As a ‘wholly owned’ Bayer subsidiary, Vividion uses discovery technologies to address ‘undruggable’ targets using therapeutics for cancers and immune disorders.
In February 2024, the company initiated subject dosing in a Phase I trial of VVD-130850, an investigational oral STAT3 inhibitor aimed at treating advanced solid and haematologic tumours.
