ONX 0912

Onyx is developing ONX 0912, a novel oral proteasome inhibitor. ONX 0912 inhibits the 20S proteasome that primarily targets chymotrypsin-like activity. ONX 0912 is distinct from carfilzomib, although the compound is based on the same chemistry that is employed to selectively target the proteasome. As an orally-dosed agent, ONX 0912 is designed to provide prolonged proteasome inhibition and combinability with other available therapies with the convenience of an oral therapy.

ONX 0912 has demonstrated preclinical anti-tumor activity and a broad therapeutic window in preclinical models. ONX 0912 is currently in Phase 1 clinical development in a solid tumor study in the United States. Early data have shown that two-thirds of patients at the 90 mg dose or above achieved a level of proteasome inhibition comparable to what has been observed with carfilzomib. A Phase 1b/2 trial evaluating ONX 0912 in hematologic malignancies is expected to commence in 2011.

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