Synonyms: BIIB024 | example 10Da [US20090036419] | MLN-2480 | MLN2480 | TAK-580 | TAK580
Compound class:
Synthetic organic
Comment: TAK-580 (MLN2480) is an investigational pan-RAF kinase inhibitor that was developed for anti-tumour potential against solid tumours, including gliomas, and common adult RAF mutant tumours (harbouring BRAF and CRAF fusions and mutations) that metastasise to the brain. It has been optimised for CNS penetration [2]. The chemical structure is claimed as example 10Da in patent US20090036419A1 [1]. Day One Biopharmaceuticals licensed this inhibitor from Sunesis Pharma in 2019, at which point it was re-named DAY101. The chemical structure of TAK-580 is identical to that which was submitted to the WHO for the INN tovorafenib (proposed INN list 126, Jan 2022).
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Phase 1 clinical trials are underway to evaluate TAK-580 (MLN2480) efficacy in melanoma, glioma and other non-hematological cancers, either as monotherapy or in combination with other antineoplastic agents. Click here to link to ClinicalTrials.gov's full list of registered TAK-580 studies. Day One Biopharmaceuticals have licensed this inhibitor, and they plan to develop it (as DAY101) for childhood recurrent or progressive low-grade glioma with BRAF alterations, and for adults with RAF-altered solid tumours for which there are no other treatment options. The FDA granted DAY101 Orphan Drug Designation for the treatment of malignant glioma in September 2020. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT03429803 | TAK-580 In Gliomas and Other Tumors | Phase 1 Interventional | Dana-Farber Cancer Institute | ||
NCT02327169 | A Study MLN2480 in Combination With MLN0128 or Alisertib, or Paclitaxel, or Cetuximab, or Irinotecan in Adult Participants With Advanced Nonhematologic Malignancies | Phase 1 Interventional | Takeda | ||
NCT01425008 | Study of MLN2480 in Participants With Relapsed or Refractory Solid Tumors Followed by a Dose Expansion in Participants With Metastatic Melanoma | Phase 1 Interventional | Takeda |