Products and
Pipeline

Overview^1-3

- SUMOylation is a reversible post-translational modification that regulates protein function by covalent attachment of small ubiquitin-like modifier (SUMO) proteins to protein substrates

- TAK-981 is a first-in-class, small molecule inhibitor of SUMO Activating Enzyme (SAE)

- SUMOylation has been reported to play a key role in inhibiting Type I interferon (IFN) responses

- Inhibition of SUMOylation by TAK-981 promotes Type I IFN dependent innate and adaptive antitumor immune responses

MOA²

- TAK-981 is a small molecule that binds covalently to SUMO and inhibits SAE2 (an E1 activating enzyme) and the downstream SUMOylation of targeted substrates

- Inhibition of SUMOylation has diverse biological consequences, including potential effects on the innate and adaptive immune system

Clinical Trials

Study Name

A Phase 1b/2 Study of TAK-981 Plus Pembrolizumab to Evaluate the Safety, Tolerability, and Antitumor Activity of the Combination in Patients With Select Advanced or Metastatic Solid Tumors

Study Name

Phase 1/2 Study of TAK-981 in Combination With Rituximab in Patients With Relapsed/Refractory CD20-Positive Non-Hodgkin Lymphoma

Study Name

A Phase 1b/2 Open-Label, Multicenter Study to Evaluate the Safety and Efficacy of TAK-981 in Combination With Monoclonal Antibodies in Adult Patients With Relapsed and/or Refractory Multiple Myeloma

Study Name

An Open Label, Dose-Escalation, Phase I Study to Evaluate the Safety, Tolerability and Pharmacokinetics of TAK-981 in Adult Patients With Advanced or Metastatic Solid Tumors or Relapsed/Refractory Hematologic Malignancies and in a Subset With Coronavirus Disease 2019

References

1. He X, et al. PLoS One. 2015;10:e0123882,

2. Assouline SE, et al. Blood. 2019;134(Supplement_1):768.

3. Mi Z, et al. Protein Cell. 2010;1:275-283.