Chemistry:Sulanemadlin
From HandWiki
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]
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
Sulanemadlin 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
- ↑ 1.0 1.1 "Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development". Journal of Medicinal Chemistry 66 (14): 9401–9417. July 2023. doi:10.1021/acs.jmedchem.3c00623. PMID 37439511.
- ↑ "Stapled peptide sulanemadlin for AML and MDS". The Video Journal of Hematological Oncology (VJHemOnc). Magdalen Medical Publishing (MMP). 17 December 2018. https://www.vjhemonc.com/video/tv6oq8c3x2q-stapled-peptide-alrn-6924-for-aml-and-mds/.
- ↑ "MDM2/MDMX inhibitor ALRN-6924". NCI Drug Dictionary. National Cancer Institute. https://www.cancer.gov/publications/dictionaries/cancer-drug/def/sulanemadlin.
- ↑ "The Stapled Peptide That Made It Furthest". In The Pipeline, Science Magazine. American Association for the Advancement of Science (AAAS). July 27, 2023. https://www.science.org/content/blog-post/stapled-peptide-made-it-furthest.
- ↑ "Phase 1b Trial of ALRN-6924 for p53-Mutated Breast Cancer Terminated" (in en). 22 February 2023. https://www.targetedonc.com/view/phase-1b-trial-of-alrn-6924-for-p53-mutated-breast-cancer-terminated.
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