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TAK-580: An Oral Pan-RAF Kinase Inhibitor

TAK-580 (formerly called MLN2480) is an oral pan-RAF kinase inhibitor with a distinct molecular signature which has exhibited a promising preclinical profile. TAK-580 was identified through a pan-RAF inhibitor discovery program that was originally initiated under a collaboration agreement between Sunesis and Biogen Idec. TAK-580 is currently being developed by Takeda Pharmaceutical Company Limited through an exclusive license from Sunesis, which includes an option for co-development by Sunesis. In September 2017, Takeda presented results from the dose-expansion cohorts of a single-agent, first-in-human study of TAK-580 in patients with metastatic melanoma (NCT01425008). The Maximum Tolerated Doses of TAK-580 identified during dose escalation and used for the dose-expansion cohorts were 200 mg dosed every other day and 600 mg dosed weekly. Results suggested that the weekly dosing regimen was better tolerated.

Based on results from this study, Takeda has initiated a multi-arm, open-label Phase 1B Study of TAK-580 in combination with MLN0128, an oral mTORC 1/2 inhibitor; alisertib, an oral aurora A kinase inhibitor; or paclitaxel, in adult patients with advanced nonhematologic malignancies.

Under the license agreement, we may in the future receive pre-commercialization, event-based payments related to the development by Millennium of the first two indications for each of the licensed products directed against the RAF target, and royalty payments depending on related product sales.

For more information about TAK-580 clinical trials, please click here.


Download presentations that have been given at recent conferences and meetings.
TAK-580 (RAF) Presentations