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Synonyms: Shaite® (China)
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). |
| References |
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1. Dhillon S. (2024)
Aponermin: First Approval. Drugs, 84 (4): 459-466. [PMID:38441805] |
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2. Fang F, Wang AP, Yang SF. (2005)
Antitumor activity of a novel recombinant mutant human tumor necrosis factor-related apoptosis-inducing ligand. Acta Pharmacol Sin, 26 (11): 1373-81. [PMID:16225761] |
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3. Leng Y, Hou J, Jin J, Zhang M, Ke X, Jiang B, Pan L, Yang L, Zhou F, Wang J et al.. (2017)
Circularly permuted TRAIL plus thalidomide and dexamethasone versus thalidomide and dexamethasone for relapsed/refractory multiple myeloma: a phase 2 study. Cancer Chemother Pharmacol, 79 (6): 1141-1149. [PMID:28500554] |
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4. Xia Z, Leng Y, Fang B, Liang Y, Li W, Fu C, Yang L, Ke X, Jiang H, Weng J et al.. (2023)
Aponermin or placebo in combination with thalidomide and dexamethasone in the treatment of relapsed or refractory multiple myeloma (CPT-MM301): a randomised, double-blinded, placebo-controlled, phase 3 trial. BMC Cancer, 23 (1): 980. [PMID:37838670] |
