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AZD6244 (Selumetinib)

Last Updated: 09/18/18

Status: Currently a NF2 Clinical Trial


Chemical Structure, selumetinib

Trade Name: N/A
Synonyms: AZD 6244, 606143-52-6, AZD6244, AZD-6244,
ARRY-142886, CHEMBL1614701, NCGC00189073-01,
PubChem21092, Selumetinib (USAN/INN)
Pharmaceutical Company: N/A
Protein Target: MAPK/ERK Pathway
Legal Status: ℞ - Prescription/Under Clinical Trial
Administered By: Pill[3]
Formula: C17H15BrClFN4O3
ChemSpider: 8303141 (Accessed: 2018)
PubChem: CID 10127622

Selumetinib (AZD6244) is a drug being investigated for the treatment of various types of cancer, for example non-small cell lung cancer (NSCLC). [4}

Treatment Information

UK Treatments: The role of insulin-like growth factors signaling in merlin-deficient human schwannomas


NF2 Trial:

https://www.cincinnatichildrens.org/service/c/clinical-trials/studies/SEL-TH-1601

Also Treatment For[2]

  1. Solid Tumors
  2. Neurofibromatosis Type 1
    1. Plexiform Neurofibroma
    2. Optic Nerve Glioma
  3. Uveal Melanoma
  4. Malignant Peripheral Nerve Sheath Tumors
  5. Chronic Myeloid Leukemia
  6. Myelofibrosis
  7. Kaposi's Sarcoma
  8. Malignant Neoplasm of Breast
  9. Malignant Neoplasms of Digestive Organs
  10. Malignant Neoplasms of Female Genital Organs
  11. Malignant Neoplasms of Male Genital Organs
  12. Malignant Neoplasms of Thyroid and other Endocrine Gland
  13. Triple-Negative Breast Cancer
  14. Squamous Cell Lung Cancer
  15. Non-squamous Cell Lung Cancer with KRAS Mutations
  16. Non-squamous Cell Lung Cancer with Wild-type KRAS

Side Effects

Dermatologic side-effects [2,3]

Sources

  1. ChemSpider. "Selumetinib." http://www.chemspider.com/Chemical-Structure.8303141.html
  2. CinicalTrials.gov "Selumetinib Trials USA"
    https://clinicaltrials.gov/ct2/results?term=Selumetinib&Search=Apply&recrs=b&recrs=a&recrs=f&recrs=d&recrs=g&recrs=h&recrs=e&recrs=i&recrs=m&age_v=&gndr=&type=&rslt=
  3. Dombi, Eva, et al. "Activity of selumetinib in neurofibromatosis type 1-related plexiform neurofibromas." New England Journal of Medicine 375.26 (2016): 2550-2560.
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5508592/
  4. Balagula, Yevgeniy, et al. "Dermatologic side effects associated with the MEK 1/2 inhibitor selumetinib (AZD6244, ARRY-142886)." Investigational new drugs 29.5 (2011): 1114-1121.
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5691597/ DOI: https://doi.org/10.1007/s10637-010-9567-3
  5. Casaluce, Francesca, et al. "Selumetinib for the treatment of non-small cell lung cancer." Expert opinion on investigational drugs 26.8 (2017): 973-984.
    https://www.tandfonline.com/doi/abs/10.1080/13543784.2017.1351543 | DOI: https://doi.org/10.1080/13543784.2017.1351543
  6. Wallace, Eli M., et al. "Compositions comprising N3 alkylated benzimidazole derivatives as MEK inhibitors and methods of use thereof." U.S. Patent No. 8,193,231. (5 Jun. 2012).
    https://patents.google.com/patent/US8193231B2/en
  7. Wallace, Eli M., et al. "Method of treatment using N3 alkylated benzimidazole derivatives as MEK inhibitors." U.S. Patent No. 8,193,229. 5 Jun. 2012.
    https://patents.google.com/patent/US8193229B2/en