Sulanemadlin

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Sulanemadlin
Sulanemadlin.svg
Clinical data
Other namesALRN-6924
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
DrugBank
UNII
Chemical and physical data
Formula C95H140N20O23
Molar mass 1930.282 g·mol−1

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. 1 2 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.
  2. ↑ Sallman D (17 December 2018). "Stapled peptide sulanemadlin for AML and MDS". The Video Journal of Hematological Oncology (VJHemOnc). Magdalen Medical Publishing (MMP).
  3. ↑ "MDM2/MDMX inhibitor ALRN-6924". NCI Drug Dictionary. National Cancer Institute.
  4. ↑ 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).
  5. ↑ "Phase 1b Trial of ALRN-6924 for p53-Mutated Breast Cancer Terminated". Targeted Oncology. 22 February 2023. Retrieved 18 April 2024.
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