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aponermin   Click here for help

GtoPdb Ligand ID: 13293

Synonyms: Shaite® (China)
Approved drug
aponermin is an approved drug (China (2023))
Compound class: Peptide
Comment: Aponermin is an engineered tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) peptide mimetic that was designed to promote apoptosis in tumours by interacting with death receptors (DR) 4 and 5 on the surface of tumour cells [2], whilst sparing normal cells/tissues. This peptide construct comprises the extracellular (soluble) portion of TRAIL and it organises into stable homotrimers in solution. Aponermin has higher binding affinity for DR4/5 and a longer half-life (in rodents and humans) than endogenous wild type TRAIL [1,3].
In the absence of a declared amino acid sequence for aponermin, we generated the sequence presented here from information in [1] and the Uniprot entry for human TRAIL (P50591).
No information available.
Summary of Clinical Use Click here for help
Efficacy results from phase 2 and 3 clinical trials carried out in China have been published [3-4]. Aponermin was issued first approval in China in November 2023 [1]. It is indicated to treat relapsed/refractory multiple myeloma in combination with thalidomide and dexamethasone.