21 September 2020 - - US-based biopharmaceutical company OnKure, Inc., a developer next generation histone deacetylase inhibitors, has entered into a clinical trial collaboration and supply agreement with US-based pharmaceutical company Pfizer Inc. (NYSE: PFE) to support the clinical proof of concept study for Mektovi (binimetinib) in combination with OKI-179, a highly potent and tolerable Class I HDAC inhibitor currently in Phase I for the treatment of NRAS melanoma, the company said.

Activating NRAS mutations occur in approximately 20% of melanomas, representing the second most common oncogenic driver mutation in melanoma after BRAF mutations.

An unmet medical need remains for targeted therapy in metastatic patients harboring an NRAS mutation.

Binimetinib, a mitogen-activated protein kinase inhibitor that Pfizer has exclusive rights to in the US and Canada, has been approved for use in combination with encorafenib for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation.

Based on a recent study by Maertens et al. reported in Cancer Discovery, as well as preclinical combination studies conducted by OnKure, the rational combination of these two agents may enhance clinical benefit of MAPK inhibition in NRAS melanomas.

OnKure and Pfizer will form a Joint Development Committee to review clinical trial results from the OnKure-sponsored study.

OnKure, Inc. is a biopharmaceutical company focused on the discovery and development of targeted small molecule drugs to improve the outcomes of patients afflicted with cancer.

OnKure's drug candidates aim to treat patients by targeting malignant cells directly, by working in combination with other small molecule therapies and by priming the tumor microenvironment such that checkpoint inhibition is optimised.