Synonyms: Example 133 [WO2016004136A1] | I-263a [WO2016004136A1] | subasumstat (proposed INN) | TAK981
Compound class:
Synthetic organic
Comment: TAK-981 is an inhibitor of the protein post-translational modification, SUMOylation. SUMO is a small ubiquitin-like modifier that is attached to proteins by enzymes of the SUMOylation complex (sumo activating enzyme, SAE) [2], and its attachment regulates protein function. SUMOylation has emerged as an important pathway in oncogenic processes, making SAE an oncology drug target. TAK-981 inhibits SUMOylation and has been shown to induce anti-tumour immunity in preclinical models. The precise molecular target for TAK-981 has not been disclosed.
The chemical structure that was submitted to the WHO for the INN subasumstat is identical to the chemical structure of TAK-981 that is held by PubChem, and is claimed in patent WO2016004136A1 by a team from Millennium Pharmaceuticals. |
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No information available. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT04065555 | Intratumoral Microdosing of TAK-981 in Head and Neck Cancer | Early Phase 1 Interventional | Presage Biosciences | ||
NCT03648372 | A Study to Evaluate the Safety, Tolerability and Pharmacokinetics (PK) of TAK-981 in Adult Participants With Advanced or Metastatic Solid Tumors or Relapsed/Refractory Hematologic Malignancies and in a Subset With Coronavirus Disease 2019 (COVID-19) | Phase 1 Interventional | Takeda | ||
NCT04074330 | A Study of TAK-981 in Combination With Rituximab in Participants With Relapsed/Refractory (r/r) CD20-positive (CD20+) Non-Hodgkin Lymphoma (NHL) | Phase 1/Phase 2 Interventional | Takeda | ||
NCT04381650 | A Safety and Efficacy Study of TAK-981 Plus Pembrolizumab in Participants With Select Advanced or Metastatic Solid Tumors | Phase 1/Phase 2 Interventional | Takeda |