Noch ein Proteasome-Inhibitor in Entwicklung vom gleichen Hersteller von Velcade und Carfilzomib

Onyx is developing oprozomib (formerly ONX 0912), a novel oral proteasome inhibitor. In preclinical studies, oprozomib has been shown to inhibit the 20S proteasome that primarily targets chymotrypsin-like activity. Oprozomib 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, oprozomib is designed to provide prolonged proteasome inhibition and combinability with other available therapies with the convenience of an oral therapy.
Oprozomib has demonstrated preclinical anti-tumor activity and a broad therapeutic window in preclinical models. Oprozomib is currently being studied in two trials, including a Phase 1b/2 study evaluating oprozomib in hematologic malignancies including multiple myeloma. The second trial is a Phase 1 study in patients with recurrent or refractory solid tumors. From this early-stage study, data from this trial 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, although further study is required.