Sulanemadlin (development code ALRN-6924) is an experimental drug for the treatment of cancer.[1] It is under development by Aileron Therapeutics, and has been studied in clinical trials for myelodysplastic syndrome and acute myeloid leukemia.[2]
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| Other names | ALRN-6924 |
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| Formula | C95H140N20O23 |
| Molar mass | 1930.282 g·mol−1 |
Sulanemadlin is a stapled peptide that mimics the N-terminal domain of p53, a tumor suppressor protein. As such, it binds to MDM2 and MDMX, leading to tumor cell apoptosis.[3]
Clinical trials
editSulanemadlin is notable as the first stapled peptide, a novel pharmaceutical strategy, to enter clinical trials.[1][4]
Despite its preclinical promise, concerns about side effects, including severe neutropenia, have terminated Phase 1B clinical trials early in at least one trial.[5]
References
edit- ^ a b Guerlavais V, Sawyer TK, Carvajal L, Chang YS, Graves B, Ren JG, et al. (July 2023). "Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development". Journal of Medicinal Chemistry. 66 (14): 9401–9417. doi:10.1021/acs.jmedchem.3c00623. PMID 37439511.
- ^ Sallman D (17 December 2018). "Stapled peptide sulanemadlin for AML and MDS". The Video Journal of Hematological Oncology (VJHemOnc). Magdalen Medical Publishing (MMP).
- ^ "MDM2/MDMX inhibitor ALRN-6924". NCI Drug Dictionary. National Cancer Institute.
- ^ Lowe D (July 27, 2023). "The Stapled Peptide That Made It Furthest". In The Pipeline, Science Magazine. American Association for the Advancement of Science (AAAS).
- ^ "Phase 1b Trial of ALRN-6924 for p53-Mutated Breast Cancer Terminated". Targeted Oncology. 22 February 2023. Retrieved 18 April 2024.