Sapanisertib

Sapanisertib (also known as MLN0128, INK128 and TAK-228) is an experimental small molecule inhibitor of mTOR which is administered orally. It targets both mTORC1 and mTORC2.[1]

Sapanisertib
Identifiers
  • 5-(4-Amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
CAS Number
PubChem CID
UNII
KEGG
Chemical and physical data
FormulaC15H15N7O
Molar mass309.333 g·mol−1
3D model (JSmol)
  • CC(C)N1C2=C(C(=N1)C3=CC4=C(C=C3)OC(=N4)N)C(=NC=N2)N
  • InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
  • Key:GYLDXIAOMVERTK-UHFFFAOYSA-N

Developed by Millennium Pharmaceuticals,[2][3][4] and is in phase II clinical trials for breast cancer, endometrial cancer, glioblastoma, renal cell carcinoma, and thyroid cancer.[5] The drug has been well tolerated by patients with advanced solid tumours in Phase I trials.[6]

References
  1. Panchal II, Badeliya SN, Patel R, Patel A, Devaligar A (2019). "In silico Analysis and Molecular Docking Studies of Novel 4-Amino-3- (Isoquinolin-4-yl)-1H-Pyrazolo[3,4-d]Pyrimidine Derivatives as Dual PI3-K/mTOR Inhibitors". Current Drug Discovery Technologies. 16 (3): 297–306. doi:10.2174/1568009618666181102144934. PMID 30387396. S2CID 54344624.
  2. Guo N, Azadniv M, Coppage M, Nemer M, Mendler J, Becker M, Liesveld J (April 2019). "Effects of Neddylation and mTOR Inhibition in Acute Myelogenous Leukemia". Translational Oncology. 12 (4): 602–613. doi:10.1016/j.tranon.2019.01.001. PMC 6348338. PMID 30699367.
  3. Ouvry G, Clary L, Tomas L, Aurelly M, Bonnary L, Borde E, et al. (November 2019). "Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors". ACS Medicinal Chemistry Letters. 10 (11): 1561–1567. doi:10.1021/acsmedchemlett.9b00401. PMC 6862343. PMID 31749911.
  4. Arnold A, Yuan M, Price A, Harris L, Eberhart CG, Raabe EH (April 2020). "Synergistic activity of mTORC1/2 kinase and MEK inhibitors suppresses pediatric low-grade glioma tumorigenicity and vascularity". Neuro-Oncology. 22 (4): 563–574. doi:10.1093/neuonc/noz230. PMC 7158655. PMID 31841591.
  5. "Sapanisertib - Takeda Oncology". Adis Insight. Springer Nature Switzerland AG.
  6. Moore KN, Bauer TM, Falchook GS, Chowdhury S, Patel C, Neuwirth R, et al. (February 2018). "Phase I study of the investigational oral mTORC1/2 inhibitor sapanisertib (TAK-228): tolerability and food effects of a milled formulation in patients with advanced solid tumours". ESMO Open. 3 (2): e000291. doi:10.1136/esmoopen-2017-000291. PMC 5812400. PMID 29464110.
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