Elimusertib

Last updated

Elimusertib
Elimusertib.svg
Identifiers
  • (3R)-3-methyl-4-[4-(2-methylpyrazol-3-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridin-2-yl]morpholine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C20H21N7O
Molar mass 375.436 g·mol−1
3D model (JSmol)
  • C[C@@H]1COCCN1C2=NC3=C(C=CN=C3C4=CC=NN4)C(=C2)C5=CC=NN5C
  • InChI=1S/C20H21N7O/c1-13-12-28-10-9-27(13)18-11-15(17-5-8-23-26(17)2)14-3-6-21-20(19(14)24-18)16-4-7-22-25-16/h3-8,11,13H,9-10,12H2,1-2H3,(H,22,25)/t13-/m1/s1
  • Key:YBXRSCXGRPSTMW-CYBMUJFWSA-N

Elimusertib (Bay 1895344) is an experimental anticancer drug which acts as an inhibitor of ataxia telangiectasia and Rad3 related protein. This is involved in DNA repair following damage, and so inhibiting this protein causes cancer cells to become more vulnerable to other chemotherapy drugs. Elimusertib is in early stage clinical trials against advanced solid tumors. [1] [2] [3] [4]

References

  1. ↑ Lücking U, Wortmann L, Wengner AM, Lefranc J, Lienau P, Briem H, et al. (July 2020). "Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models". Journal of Medicinal Chemistry. 63 (13): 7293–7325. doi:10.1021/acs.jmedchem.0c00369. PMID   32502336.
  2. ↑ Wengner AM, Siemeister G, Lücking U, Lefranc J, Wortmann L, Lienau P, et al. (January 2020). "The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage-Inducing or Repair-Compromising Therapies in Preclinical Cancer Models". Molecular Cancer Therapeutics. 19 (1): 26–38. doi:10.1158/1535-7163.MCT-19-0019. PMID   31582533.
  3. ↑ Yap TA, Tan DS, Terbuch A, Caldwell R, Guo C, Goh BC, et al. (January 2021). "First-in-Human Trial of the Oral Ataxia Telangiectasia and RAD3-Related (ATR) Inhibitor BAY 1895344 in Patients with Advanced Solid Tumors". Cancer Discovery. 11 (1): 80–91. doi:10.1158/2159-8290.CD-20-0868. PMC   9554790 . PMID   32988960.
  4. ↑ Odhiambo DA, Pittman AN, Rickard AG, Castillo RJ, Bassil AM, Chen J, et al. (April 2024). "Preclinical Evaluation of the ATR Inhibitor BAY 1895344 as a Radiosensitizer for Head and Neck Squamous Cell Carcinoma". International Journal of Radiation Oncology, Biology, Physics. 118 (5): 1315–1327. doi:10.1016/j.ijrobp.2023.12.012. PMC   11294978 . PMID   38104870.
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